{"id":42632,"date":"2018-09-14T01:00:00","date_gmt":"2018-09-17T07:06:34","guid":{"rendered":"http:\/\/www.05921.net\/index.php\/2018\/09\/17\/%e3%80%90bioworld-science%e3%80%912018%e5%b9%b48%e6%9c%88%e8%8d%af%e7%89%a9%e5%bf%ab%e8%ae%af_%e5%b8%ae%e5%8a%a9%e6%82%a8%e5%8f%8a%e6%97%b6%e6%8a%8a%e6%8f%a1%e8%8d%af%e7%89%a9%e7%a0%94%e5%8f%91\/"},"modified":"2018-09-17T15:06:38","modified_gmt":"2018-09-17T07:06:38","slug":"%e3%80%90bioworld-science%e3%80%912018%e5%b9%b48%e6%9c%88%e8%8d%af%e7%89%a9%e5%bf%ab%e8%ae%af_%e5%b8%ae%e5%8a%a9%e6%82%a8%e5%8f%8a%e6%97%b6%e6%8a%8a%e6%8f%a1%e8%8d%af%e7%89%a9%e7%a0%94%e5%8f%91","status":"publish","type":"post","link":"https:\/\/www.05921.net\/index.php\/42632\/","title":{"rendered":"\u3010BioWorld Science\u30112018\u5e748\u6708\u836f\u7269\u5feb\u8baf_\u5e2e\u52a9\u60a8\u53ca\u65f6\u628a\u63e1\u836f\u7269\u7814\u53d1\u52a8\u6001"},"content":{"rendered":"
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    2018\u5e748\u670831\u65e5\uff0c\u8f89\u745e\u516c\u53f8\u7ec8\u6b62\u4e86\u4e24\u9879\u4f7f\u7528domagrozumab\u5355\u6297\u6cbb\u7597DMD\u7684\u4e34\u5e8a\u7814\u7a76  <\/span> <\/span><\/p>\n<\/li>\n<\/ul>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n

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      2018\u5e748\u670830\u65e5\uff0cAstellasPharma\u53d1\u8868\u65b0\u7ed3\u6784\u7684KRAS Gly12Cys\u7a81\u53d8\u6291\u5236\u5242<\/span><\/p>\n<\/li>\n

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      2018\u5e748\u670829\u65e5\uff0cCelgene\u548cEpizym\u516c\u53f8\u53d1\u5e03pinometostat\u7528\u4e8e\u6cbb\u7597\u6025\u6027\u665a\u671f\u767d\u8840\u75c5\u7684\u5b89\u5168\u6027\u548c\u6709\u6548\u6027\u6570\u636e     <\/span><\/p>\n<\/li>\n

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      2018\u5e748\u670823\u65e5\uff0cBYL-719\u7528\u4e8e\u6cbb\u7597\u4e73\u817a\u764c\u4e2d\u7684III\u671fSOLAR-1\u7814\u7a76\u8fbe\u5230\u4e3b\u8981\u7ec8\u70b9PFS  <\/span><\/p>\n<\/li>\n

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          2018\u5e748\u670823\u65e5\uff0cNuevolution\u516c\u53f8\u62a5\u9053IL-17A\u5c0f\u5206\u5b50\u6291\u5236\u5242\u7684\u7814\u7a76\u8fdb\u5c55<\/span><\/p>\n<\/li>\n<\/ul>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n

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                2018\u5e748\u670830\u65e5\uff0c\u6297\u759f\u5019\u9009\u65b0\u836fGSK-701\u5177\u6709\u826f\u597d\u7684\u53e3\u670d\u751f\u7269\u6709\u6548\u6027<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/li>\n<\/ul>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n

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                  2018\u5e748\u670810\u65e5\uff0c\u963f\u65af\u5229\u5eb7\u53d1\u73b0\u65b0\u578bJAK1\u6291\u5236\u5242<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/li>\n<\/ul>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n


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                  \u57fa\u56e0\u6cf0\u514b\u516c\u53f8\u62a5\u9053\u4e86\u4e0eXenon Pharmaceuticals\u516c\u53f8\u5408\u4f5c\u5f00\u53d1\u7684\u4e00\u79cdNav1.7\u901a\u9053\u6291\u5236\u5242\uff0c\u6709\u671b\u7528\u4e8e\u6cbb\u7597\u75bc\u75db\uff0c\u5982\u9057\u4f20\u6027\u7ea2\u6591\u6027\u80a2\u75db\u75c7\uff0c\u4e00\u79cd\u7531Nav1.7\u9519\u4e49\u7a81\u53d8\u5f15\u8d77\u7684\u75bc\u75db\u7efc\u5408\u5f81\u3002<\/p>\n


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                  \u7814\u7a76\u4eba\u5458\u4ece\u4e00\u4e2a\u6700\u8fd1\u62a5\u9053\u7684\u82b3\u57fa\u78fa\u80fa\u7c7bNav1.7\u6291\u5236\u5242GX-936\u51fa\u53d1\uff0c\u901a\u8fc7\u82b3\u57fa\u78fa\u80fa\u7247\u6bb5\u4e0e\u7535\u538b\u4f20\u611f\u5668\u57dfVSD4\u7684\u7ed3\u5408\uff0c\u4f7f\u901a\u9053\u7a33\u5b9a\u5728\u975e\u6d3b\u6027\u72b6\u6001\u4e0b\u3002\u901a\u8fc7\u4e00\u7cfb\u5217\u7ed3\u6784\u6539\u9020\u4f18\u5316\u4e86\u5316\u5408\u7269\u7684\u6d3b\u6027\u548c\u9009\u62e9\u6027\uff0c\u6700\u7ec8\u53d1\u73b0\u4e86\u5019\u9009\u5316\u5408\u7269GNE-616\u3002\u8be5\u5316\u5408\u7269\u5bf9Nav1.7\u901a\u9053\u7684Ki\u4e3a1.8 nM\uff0c\u5bf9Nav1.5\u901a\u9053\u5177\u6709\u826f\u597d\u7684\u9009\u62e9\u6027\u548c\u7c7b\u836f\u6027\uff08logD = 1.4, logP = 2.8\uff09\u3002<\/p>\n


                  <\/p>\n

                  \u5b83\u5728\u4f53\u5916\u7ea2\u6591\u6027\u80a2\u75db\u6a21\u578b\u4e2d\u663e\u793a\u4e86\u826f\u597d\u7684\u6548\u679c\uff08IEM EC50 = 0.74 mcM, EC50 = 9.6 nM\uff09\u3002\u5316\u5408\u7269\u5177\u6709\u826f\u597d\u7684\u4f53\u5185\u836f\u6548\u548c\u836f\u4ee3\u52a8\u529b\u5b66\u7279\u5f81\uff0c\u662f\u4e00\u79cd\u6709\u671b\u7528\u4e8e\u6cbb\u7597Nav1.7\u4ecb\u5bfc\u7684\u75bc\u75db\u975e\u963f\u7247\u7c7b\u5019\u9009\u836f\u7269\u3002(McKerrall, S. et al. 256th Am ChemSoc (ACS) Natl Meet (August 19-23, Boston) 2018, Abst MEDI 278\uff0c\u8be6\u89c1\u4e13\u5229WO 2017058821)\u3002<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  Anavex Life Sciences\u516c\u53f8\u6cbb\u7597\u65e9\u671f\u963f\u5c14\u8328\u6d77\u9ed8\u75c5\u7684\u5019\u9009\u65b0\u836fAnavex 2-73\uff08AN2\/AVex-73\uff09\u7684 IIb\/III\u671f\u4e34\u5e8a\u7814\u7a76\uff08\u968f\u673a\u53cc\u76f2\u3001\u5b89\u6170\u5242\u5bf9\u7167\u300148\u5468\u5b89\u5168\u6027\u548c\u6709\u6548\u6027\u8bd5\u9a8c\uff09\u62db\u52df\u4e86\u9996\u4f4d\u53d7\u8bd5\u8005\u3002\u8be5\u7814\u7a76\u5c06\u7eb3\u5165\u5927\u7ea6450\u540d\u60a3\u8005\uff0c\u968f\u673a\u4ee51:1:1\u5206\u914d\u5230\u4e24\u79cd\u4e0d\u540c\u5242\u91cf\u7684Anavex 2-73\u6cbb\u7597\u7ec4\u6216\u5b89\u6170\u5242\u7ec4\u3002<\/p>\n


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                  \u56fe\u4e3aAN2\/AVex-73\u7684\u7ed3\u6784<\/span>
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                  \u8f89\u745e\u516c\u53f8\u7ec8\u6b62\u4e86\u4e24\u9879\u6b63\u5728\u8fdb\u884c\u7684domagrozumab\u5355\u6297\uff08PF-06252616\uff09\u6cbb\u7597\u675c\u6c0f\u808c\u8425\u517b\u4e0d\u826f\uff08DMD\uff09\u7684\u4e34\u5e8a\u7814\u7a76\uff0c\u5305\u62ec\u4e00\u9879II\u671f\u5b89\u5168\u6027\u548c\u6709\u6548\u6027\u7814\u7a76\uff08B5161002\uff09\u548c\u4e00\u9879\u5f00\u653e\u6807\u7b7e\u7684\u6269\u5c55\u7814\u7a76\uff08B5161004\uff09\uff08ClinicalTrials.gov\u7f16\u53f7NCT02310763\u548cNCT02907619\uff09\u3002<\/p>\n


                  <\/p>\n

                  B5161002\u662f\u4e00\u9879\u591a\u4e2d\u5fc3\u53cc\u76f2\u3001\u5b89\u6170\u5242\u5bf9\u7167\u7684\u4e34\u5e8a\u8bd5\u9a8c\uff0c\u5bf9121\u540d\u5e74\u9f84\u57286-15\u5c81\u7684DMD\u7537\u5b69\u8fdb\u884c\u7814\u7a76\u3002\u8fd9\u4e9b\u7537\u5b69\u65e0\u8bba\u662f\u5426\u6709\u6f5c\u5728\u7a81\u53d8\uff0c\u90fd\u63a5\u53d7\u6bcf\u6708\u7684domagrozumab\u9759\u8109\u6ce8\u5c04\u5e76\u8f85\u4ee5\u76ae\u8d28\u7c7b\u56fa\u9187\u6cbb\u7597\u3002\u8be5\u7814\u7a76\u4e3a\u671f2\u5e74\u4e14\u57281\u5e74\u540e\u8fdb\u884c\u521d\u6b65\u5206\u6790\u3002\u6269\u5c55\u7814\u7a76B5161004\u7684\u76ee\u7684\u662f\u6839\u636e\u6bcf\u4e2a\u60a3\u8005\u5bf9B5161002\u7684\u8010\u53d7\u6027\u6570\u636e\uff0c\u6bcf\u6708\u7ed9\u4e88\u4e2a\u4f53\u5316\u6700\u5927\u8010\u53d7\u6027\u5242\u91cf\u4ee5\u8bc4\u4f30\u957f\u671f\u5b89\u5168\u6027\u548c\u6709\u6548\u6027\u3002<\/p>\n


                  <\/p>\n

                  \u5176\u4e2d\uff0cB5161002\u7814\u7a76\u6ca1\u6709\u8fbe\u5230\u5176\u4e3b\u8981\u7597\u6548\u7ec8\u70b9\uff0c\u5373DMD\u60a3\u8005\u7528domagrozumab\u6cbb\u75971\u5e74\u540e\u5bf9\u6bd4\u5b89\u6170\u5242\u6cbb\u7597\u540e\u76844 Stair Climb\u6d4b\u8bd5\uff08\u65f6\u95f4\u4ee5\u79d2\u8ba1\u7b97\uff09\u4e0e\u57fa\u7ebf\u76f8\u6bd4\u7684\u5e73\u5747\u5dee\u5f02\u3002\u8fdb\u4e00\u6b65\u8bc4\u4f30\u7684\u5305\u62ec\u6b21\u8981\u7ec8\u70b9\u5728\u5185\u7684\u6240\u6709\u8bc1\u636e\uff0c\u4e5f\u5e76\u4e0d\u652f\u6301\u8be5\u836f\u5177\u5907\u663e\u8457\u7684\u6cbb\u7597\u6548\u679c\u3002\u7ec8\u6b62\u8be5\u7814\u7a76\u7684\u51b3\u5b9a\u662f\u5728\u5bf9\u521d\u6b21\u5206\u6790\u65f6\u7684\u53ef\u7528\u6570\u636e\u8fdb\u884c\u5168\u9762\u8bc4\u4f30\u540e\u505a\u51fa\u7684\uff0c\u5305\u62ec\u4e86\u6cbb\u7597\u4e00\u5e74\u548c\u8d85\u8fc7\u4e00\u5e74\u7684\u53c2\u4e0e\u8005\u3002\u7814\u7a76\u7684\u7ec8\u6b62\u4e0e\u5b89\u5168\u539f\u56e0\u65e0\u5173\u3002\u8f89\u745e\u4f1a\u7ee7\u7eed\u4fdd\u6301\u5bf9DMD\u548c\u7f55\u89c1\u7684\u795e\u7ecf\u808c\u8089\u75be\u75c5\u7684\u7814\u7a76\uff0c\u5176\u4e2d\u4e00\u6b3e\u6cbb\u7597DMD\u7684\u57fa\u56e0\u7597\u6cd5PF-06939926\u76ee\u524d\u6b63\u5728\u8fdb\u884c\u4e34\u5e8a\u7814\u7a76\u3002\uff08\u8f89\u745e\u516c\u53f8\u65b0\u95fb\u7a3f\uff1bClinicalTrials.gov\u7f51\u7ad9\uff09\u3002<\/p>\n


                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  <\/section>\n<\/section>\n
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                  \u80bf\u7624<\/p>\n<\/section>\n<\/section>\n

                  \n
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                  <\/section>\n<\/section>\n
                  \n
                  <\/section>\n<\/section>\n
                  <\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n
                  \n
                  \n
                  \n

                  2018\u5e748\u670830\u65e5\uff0cAstellasPharma\u53d1\u8868\u65b0\u7ed3\u6784\u7684KRAS Gly12Cys\u7a81\u53d8\u6291\u5236\u5242<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  <\/section>\n
                  \n


                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \n

                  AstellasPharma\u516c\u53f8\u62a5\u9053\u4e86\u4e00\u7c7b\u55b9\u5511\u5549\u5316\u5408\u7269\u4f5c\u4e3aKRAS\uff08Gly12Cys\u7a81\u53d8\u4f53\uff09\u6291\u5236\u5242\uff0c\u6709\u671b\u7528\u4e8e\u6cbb\u7597\u80ba\u764c\u3002\u4ee3\u8868\u5316\u5408\u7269\u80fd\u591f\u6291\u5236KRAS\/SOS\/c-Raf\u590d\u5408\u7269\u7684\u5f62\u6210\uff0c\u5728TR-FRET \u68c0\u6d4b\u4e2d\u7684IC50\u4e3a14nm\u3002\u5728ELISA\u5b9e\u9a8c\u4e2d\uff0c\u5b83\u80fd\u591f\u6291\u5236\u4ebaKRAS\uff08G12C\uff09\u975e\u5c0f\u7ec6\u80de\u80ba\u764cNCI-H1373\u7ec6\u80de\u7684ERK\u78f7\u9178\u5316\uff08IC50 = 3 nM\uff09\u3002<\/p>\n


                  <\/p>\n

                  \u5728Cell Titer-Glo\u7814\u7a76\u4e2d\u80fd\u591f\u6291\u5236\u4ebaKRAS\uff08G12C\uff09- NCI-H1373\u7ec6\u80de\u4e0d\u4f9d\u8d56\u652f\u6301\u7269\u7684\u751f\u957f\uff08IC50 = 4.3 nM\uff09\u3002\u8be5\u5316\u5408\u7269\u80fd\u6291\u5236\u96c4\u6027CAnN.Cg-Foxn1nu\/CrlCrlj (nu\/nu)\u88f8\u9f20\u7684\u7624\u5185ERK\u78f7\u9178\u5316\uff08\u6291\u5236\u738743%\uff09\uff0c\u8fd8\u80fd\u591f\u4ee510 mg\/kg\u7684\u53e3\u670d\u5242\u91cf\u572814\u5929\u5185\u6291\u5236NCI-H1373\u7ec6\u80de\u751f\u957f\uff08\u6291\u5236\u738796%\uff09\u3002\uff08\u8be6\u89c1\u4e13\u5229WO 2018143315\uff09\u3002<\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \"\u3010BioWorld<\/section>\n<\/section>\n<\/section>\n
                  \n
                  \n
                  \n

                  \u56fe\u4e3a\u4e13\u5229WO 2018143315\u4e2d\u4ee3\u8868\u5316\u5408\u7269\u7684\u7ed3\u6784<\/span><\/p>\n


                  <\/p>\n

                  2018\u5e748\u670829\u65e5\uff0cCelgene\u548cEpizym\u516c\u53f8\u53d1\u5e03pinometostat\u7528\u4e8e\u6cbb\u7597\u6025\u6027\u665a\u671f\u767d\u8840\u75c5\u7684\u5b89\u5168\u6027\u548c\u6709\u6548\u6027\u6570\u636e<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  <\/section>\n
                  \n


                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \n

                  Celgene\u548cEpizym\u8fd1\u65e5\u53d1\u8868\u4e86\u4e00\u9879\u591a\u56fdI\u671f\u4e34\u5e8a\u8bd5\u9a8c\u7684\u7ed3\u679c\uff0c\u8bc4\u4f30\u4e86pinometostat\uff08EPZ-5676\uff09\u7684\u5b89\u5168\u6027\u548c\u6709\u6548\u6027\u3002Pinometostat\u662f\u4e00\u79cd\u539f\u521b\u7684\u5c0f\u5206\u5b50\u7ec4\u86cb\u767d\u7532\u57fa\u8f6c\u79fb\u9176\u6291\u5236\u5242\uff0c\u53ef\u963b\u65ad\u7aef\u7c92\u6c89\u9ed81\u6837\uff08DOT1L\uff09\u6291\u5236\u5242\uff0c\u7528\u4e8e\u6210\u4eba\u665a\u671f\u6025\u6027\u767d\u8840\u75c5\u60a3\u8005\u3002<\/p>\n


                  <\/p>\n

                  \u5728\u5f00\u653e\u6807\u7b7e\u7684I\u671f\u5242\u91cf\u9012\u589e\u548c\u5242\u91cf\u6269\u5f20\u8bd5\u9a8c\u4e2d\uff0c51\u4f8b\u590d\u53d1\u6216\u96be\u6cbb\u6027\u6025\u6027\u767d\u8840\u75c5\u7684\u6210\u5e74\u60a3\u8005\uff08\u4e2d\u4f4d\u5e74\u9f8450\u5c81\uff09\u6301\u7eed\u9759\u8109\u8f93\u6ce8\u7ed9\u4e88pinometostat\u4e3a\u671f21\u5929\uff0c\u5468\u671f\u4e3a28\u5929\u3002\u6570\u636e\u663e\u793a\uff0c\u5728\u7b2c\u4e00\u6b21\u6ce8\u5c04\u8fbe\u5230\u7a33\u5b9a\u72b6\u6001\u540e4\u5c0f\u65f6\u5185\uff0cpinometostat\u7684\u8840\u6d46\u6d53\u5ea6\u8fbe\u5230\u5cf0\u503c\u5e76\u7ef4\u63018\u5c0f\u65f6\u3002\u8840\u6d46\u6d53\u5ea6\u5448\u53cc\u76f8\u4e0b\u964d\uff0calpha\u6d88\u9664\u671f\u534a\u8870\u671f\u4e3a0.8-2.0 h\uff0cbeta\u671f\u534a\u8870\u671f\u4e3a102-298 h\u3002\u5e73\u5747\u7a33\u6001\u6d53\u5ea6\u5448\u5242\u91cf\u4f9d\u8d56\u6027\u4e0a\u5347\uff0c\u4ee590 mg\/m2\/\u5929\u7684\u5242\u91cf\u8fde\u7eed\u7ed9\u836f28\u5929\u7684\u8840\u6d46\u6d53\u5ea6\u6700\u9ad8\u3002<\/p>\n


                  <\/p>\n

                  \u8be5\u836f\u80fd\u591f\u4f7f\u7ec4\u86cb\u767d-3\u8d56\u6c28\u9178-79\u7684\u4e8c\u7532\u57fa\u5316\u7a0b\u5ea6\uff08H3K79me2\uff09\u5728MLL-r\u9776\u57fa\u56e0\u4e0a\u6574\u4f53\u548c\u5c40\u90e8\u7684\u964d\u4f4e\uff0c\u5e76\u663e\u793a\u51fa\u4e0d\u540c\u7a0b\u5ea6\u7684\u7ec4\u86cb\u767d\u7532\u57fa\u8f6c\u79fb\u9176DOT1L\u6291\u5236\uff0c\u4f46\u6291\u5236\u6548\u679c\u4e0e\u836f\u7269\u8840\u6d46\u6d53\u5ea6\u76f8\u5173\u6027\u8f83\u5f31\u3002\u5b89\u5168\u6027\u65b9\u9762\uff0c\u5728\u5242\u91cf\u6269\u5927\u9636\u6bb590 mg\/m2\/\u5929\u548c54 mg\/m2\/\u5929\u6cbb\u759728\u5929\u7684\u5206\u7ec4\u4e2d\uff0c\u51fa\u73b0\u4e86\u5242\u91cf\u76f8\u5173\u76844\u7ea7\u5fc3\u8870\u4e8b\u4ef6\u3002\u6240\u6709\u60a3\u8005\u90fd\u81f3\u5c11\u7ecf\u5386\u8fc7\u4e00\u6b21\u7d27\u6025\u4e0d\u826f\u4e8b\u4ef6\uff08TEAE\uff09\uff0c\u4e3b\u8981\u4e3a2\u7ea7\uff0c\u901a\u5e38\u4e3a\u8840\u6db2\u5b66\uff0c\u4f46\u603b\u4f53\u8010\u53d7\u6027\u8f83\u597d\u3002<\/p>\n


                  <\/p>\n

                  \u6700\u5e38\u89c1\u7684\u4e0d\u826f\u53cd\u5e94\u5305\u62ec\u75b2\u52b3\uff0839%\uff09\u3001\u6076\u5fc3\uff0839%\uff09\u3001\u4fbf\u79d8\uff0835%\uff09\u548c\u53d1\u70ed\u6027\u4e2d\u6027\u7c92\u7ec6\u80de\u51cf\u5c11\uff0835%\uff09\u300210\u540d\u60a3\u8005\u56e0TEAE\u800c\u505c\u6b62\u6cbb\u7597\uff0c\u4f46\u6ca1\u6709\u4eba\u56e0TEAE\u6b7b\u4ea1\u300254 mg\/m2\/\u5929\u7684\u6cbb\u7597\u7ec4\u4e2d\u67092\u4f8b\u60a3\u8005\u5b8c\u5168\u7f13\u89e3\u3002\u7531\u4e0a\u8ff0\u6570\u636e\u5f97\u51fa\u7ed3\u8bba\u662f\uff0c\u5355\u836f\u6cbb\u7597\u53ef\u80fd\u4e0d\u8db3\u4ee5\u63a7\u5236\u590d\u53d1\/\u96be\u6cbb\u6027\u767d\u8840\u75c5\uff08Stein, E.M. et al. 2018, 131(24): 2661\uff09\u3002<\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \"\u3010BioWorld<\/section>\n<\/section>\n<\/section>\n
                  \n
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                  \n

                  \u56fe\u4e3aPinometostat\u7ed3\u6784<\/span><\/p>\n


                  <\/p>\n

                  2018\u5e748\u670823\u65e5\uff0cBYL-719\u7528\u4e8e\u6cbb\u7597\u4e73\u817a\u764c\u4e2d\u7684III\u671fSOLAR-1\u7814\u7a76\u8fbe\u5230\u4e3b\u8981\u7ec8\u70b9PFS<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
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                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
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                  \u8bfa\u534e\u516c\u53f8\u7684III\u671fSOLAR-1\u4e34\u5e8a\u8bd5\u9a8c\u8bc4\u4f30\u4e86alpha\u7279\u5f02\u6027PI3K\u6291\u5236\u5242BYL-719\uff08alpelisib\uff09\u7528\u4e8e\u6cbb\u7597\u4e73\u817a\u764c\u7684\u4f5c\u7528\uff0c\u8be5\u7814\u7a76\u8fbe\u5230\u4e86\u4e3b\u8981\u7ec8\u70b9\uff0c\u5373\u65e0\u8fdb\u5c55\u751f\u5b58\u671f\uff08PFS\uff09\u5f97\u5230\u4e86\u663e\u8457\u6539\u5584\u3002\uff08ClinicalTrials.gov\u7f16\u53f7NCT02437318\uff09\u3002<\/p>\n


                  <\/p>\n

                  \u8fd9\u9879\u968f\u673a\u53cc\u76f2\u3001\u6709\u5b89\u6170\u5242\u5bf9\u7167\u7684\u7814\u7a76\u8bc4\u4f30\u4e86BYL-719\u8054\u5408fulvestrant\u4e0e\u5355\u72ec\u4f7f\u7528fulvestrant\u7528\u4e8e\u6cbb\u7597572\u540d\u7edd\u7ecf\u540e\u5973\u6027\u548c\u7537\u6027\u60a3\u8005\u7684\u6548\u679c\u3002\u60a3\u8005\u5747\u4e3a\u6fc0\u7d20\u53d7\u4f53\u9633\u6027\u3001HER2\u9634\u6027\u4e14\u643a\u5e26PIK3CA\u7a81\u53d8\u7684\u665a\u671f\u6216\u8f6c\u79fb\u6027\u4e73\u817a\u764c\u60a3\u8005\uff0c\u63a5\u53d7\u8fc7\u82b3\u9999\u9176\u6291\u5236\u5242\u6cbb\u7597\uff0c\u4f46\u4e0d\u8003\u8651\u662f\u5426\u4f7f\u7528\u8fc7CDK4\/6\u6291\u5236\u5242\u6cbb\u7597\u3002BYL-719\u548cfulvestrant\u8054\u5408\u7528\u836f\u89c2\u5bdf\u5230\u7684\u4e0d\u826f\u4e8b\u4ef6\u4e0e\u4e4b\u524dBYL-719\u548cfulvestrant\u7814\u7a76\u4e2d\u57fa\u672c\u4e00\u81f4\u3002<\/p>\n


                  <\/p>\n

                  SOLAR-1\u8bd5\u9a8c\u5c06\u7ee7\u7eed\u8bc4\u4f30\u6b21\u8981\u7ec8\u70b9\uff0c\u5305\u62ec\u603b\u4f53\u751f\u5b58\u7387\u3001\u603b\u4f53\u5e94\u7b54\u7387\u3001\u4e34\u5e8a\u83b7\u76ca\u7387\u3001\u4e0e\u5065\u5eb7\u76f8\u5173\u7684\u751f\u6d3b\u8d28\u91cf\u3001PIK3CA\u975e\u7a81\u53d8\u4eba\u7fa4\u7684\u6709\u6548\u6027\u3001\u5b89\u5168\u6027\u548c\u8010\u53d7\u6027\u3002\u8bfa\u534e\u5c06\u6839\u636e\u8fd9\u4e9b\u7ed3\u679c\u4e0e\u5168\u7403\u536b\u751f\u5f53\u5c40\u5c55\u5f00\u8ba8\u8bba\u3002\uff08\u8bfa\u534e\u516c\u53f8\u65b0\u95fb\u7a3f\uff09\u3002<\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
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                  \"\u3010BioWorld<\/section>\n<\/section>\n<\/section>\n
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                  \u56fe\u4e3aAlpelisib\u7684\u7ed3\u6784<\/span><\/p>\n


                  <\/p>\n

                  2018\u5e748\u67087\u65e5\uff0cHPN-424\u7528\u4e8e\u8f6c\u79fb\u6027\u53bb\u52bf\u524d\u5217\u817a\u764c\u7684I\u671f\u4e34\u5e8a\u7814\u7a76\u7684\u9996\u4f4d\u60a3\u8005\u5f00\u59cb\u6cbb\u7597<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  Harpoon Therapeutics\u516c\u53f8\u5ba3\u5e03HPN-424\u7528\u4e8e\u8f6c\u79fb\u6027\u53bb\u52bf\u524d\u5217\u817a\u764c\uff08mCRPC\uff09\u7684I\u671f\u4e34\u5e8a\u7814\u7a76\u7684\u9996\u4f4d\u60a3\u8005\u5f00\u59cb\u6cbb\u7597\uff08ClinicalTrials.gov\u7f16\u53f7NCT03577028\uff09\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  HPN-424\u662f\u57fa\u4e8e\u8be5\u516c\u53f8\u7684TriTAC\uff08tri-specific T cell-activating construct\uff09\u5e73\u53f0\u5f00\u53d1\u7684\u7b2c\u4e00\u79cd\u5019\u9009\u836f\u7269\uff0c\u80fd\u591f\u7a7f\u900f\u5b9e\u4f53\u80bf\u7624\uff0c\u5ef6\u957f\u8840\u6e05\u534a\u8870\u671f\uff0c\u62db\u52df\u60a3\u8005\u81ea\u8eab\u7684T\u7ec6\u80de\u4ee5\u6467\u6bc1\u6076\u6027\u80bf\u7624\u3002HPN-424\u662f\u4e00\u79cd50 kd\u7684\u591a\u80bd\uff0c\u5305\u542b\u4e09\u4e2a\u7ed3\u5408\u57df\uff0c\u5206\u522b\u4e3a\u4eba\u524d\u5217\u817a\u7279\u5f02\u6027\u819c\u6297\u539f\uff08PSMA\uff09\u3001\u4eba\u8840\u6e05\u767d\u86cb\u767d\u548cCD3\u7684\u7ed3\u5408\u57df\u3002\u9884\u8ba1\u5c06\u670940\u4f8b\u60a3\u8005\u5c06\u53c2\u52a0\u8be5\u591a\u56fd\u591a\u4e2d\u5fc3\u7684\u5f00\u653e\u6807\u7b7e\u7684\u4e0a\u5347\u5242\u91cf\u8bd5\u9a8c\uff0c\u8bc4\u4f30\u5b89\u5168\u6027\u3001\u8010\u53d7\u6027\u548c\u836f\u4ee3\u52a8\u529b\u5b66\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u5728\u7814\u7a76\u7684\u7b2c\u4e00\u90e8\u5206\uff0cHPN-424\u5c06\u6bcf\u5468\u901a\u8fc7\u9759\u8109\u8f93\u6ce8\u7ed9\u836f\u4e00\u6b21\uff0c\u9010\u6e10\u589e\u52a0\u5242\u91cf\u76f4\u5230\u8fbe\u5230\u6cbb\u7597\u5242\u91cf\u6c34\u5e73\u3002\u5728\u5242\u91cf\u589e\u52a0\u7814\u7a76\u540e\uff0cHPN-424\u7684\u5b89\u5168\u6027\u548c\u6709\u6548\u6027\u8bc4\u4ef7\u5c06\u5728\u5df2\u5efa\u7acb\u7684\u63a8\u8350\u5242\u91cf\u4e0b\u8fdb\u884c\u8fdb\u4e00\u6b65II\u671f\u4e34\u5e8a\u8bc4\u4f30\uff08Harpoon Therapeutics\u516c\u53f8\u65b0\u95fb\u7a3f\uff09\u3002<\/span><\/p>\n


                  <\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  2018\u5e748\u670828\u65e5\uff0cBAY-1753011\u65e0\u9700\u6fc0\u6d3bRAAS\u7cfb\u7edf\u5373\u53ef\u63d0\u4f9b\u8840\u7ba1\u4fdd\u62a4\u548c\u8840\u7ba1\u6269\u5f20<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  \u62dc\u8033\u516c\u53f8\u5728\u6b27\u6d32\u5fc3\u810f\u75c5\u5b66\u5e74\u4f1a\u4e0a\u53d1\u8868\u4e86BAY-1753011\u7684\u4e34\u5e8a\u524d\u6570\u636e\u3002BAY-1753011\u662f\u4e00\u79cd\u65b0\u578b\u7684V1a\/V2\u53cc\u53d7\u4f53\u62ee\u6297\u5242\uff0c\u5b83\u80fd\u591f\u901a\u8fc7\u5bf9V2\u53d7\u4f53\u7684\u6291\u5236\u5f15\u8d77\u6392\u5c3f\uff0c\u4e0d\u7ecf\u7531\u80be\u7d20-\u8840\u7ba1\u7d27\u5f20\u7d20-\u919b\u56fa\u916e\u7cfb\u7edf\uff08RAAS\uff09\u7684\u6fc0\u6d3b\uff0c\u540c\u65f6\u963b\u65adV1a\u53d7\u4f53\u4ecb\u5bfc\u7684\u8840\u7ba1\u6536\u7f29\u3002<\/p>\n


                  <\/p>\n

                  \u53d7\u4f53\u7ed3\u5408\u5b9e\u9a8c\u663e\u793aBAY-1753011\u5728V1a\u548cV2\u53d7\u4f53\u7684K\u503c\u5206\u522b\u4e3a0.5\u548c0.6\uff0c\u800c\u9633\u6027\u836f\u6258\u4f10\u666e\u5766\u5728V1a\u548cV2\u53d7\u4f53\u7684K\u503c\u5206\u522b\u4e3a4.9\u548c0.8\u3002Wistar\u5927\u9f20\u5206\u522b\u4f7f\u7528BAY-1753011\u6216\u5229\u5c3f\u5242\u7ed9\u836f\u540e\u5206\u522b\u653e\u7f6e\u5728\u4ee3\u8c22\u7b3c\u4e2d\uff0c\u5e76\u540c\u65f6\u68c0\u6d4b\u5c3f\u7535\u89e3\u8d28\uff0c\u8840\u6d46\u80be\u7d20\u6d3b\u6027\uff08PRA\uff09\u548c\u8840\u6d46\u8840\u7ba1\u7d27\u5f20\u7d20I \uff08angI\uff09\u6c34\u5e73\u3002\u7ed3\u679c\u663e\u793a\uff0cBAY-1753011\u7ec4\u7684\u6392\u5c3f\u91cf\uff083 mg\/kg\uff0c214.39 mL\uff09\u6bd4\u5229\u5c3f\u5242\uff08300 mg\/kg\uff0c85.94 mL\uff09\u548c\u5b89\u6170\u5242\uff0817.05 mL\uff09\u66f4\u5927\u3002<\/p>\n


                  <\/p>\n

                  \u5229\u5c3f\u5242\u7ec4\u7684\u5c3f\u94a0\u3001\u5c3f\u94a0\u542b\u91cf\u660e\u663e\u964d\u4f4e\uff0c\u800cBAY-1753011\u7ec4\u4ec5\u7565\u6709\u589e\u52a0\u300210-300mg \/kg\u7684\u5229\u5c3f\u5242\u5904\u7406\u540e\u53ef\u68c0\u6d4b\u5230PRA\u548cangI\u6d53\u5ea6\u660e\u663e\u5242\u91cf\u4f9d\u8d56\u6027\u589e\u52a0\uff0c\u800cBAY-1753011\u57280.1 mg\/kg\u65f6\u65e0RAAS\u6fc0\u6d3b\u3002\u6b64\u5916\uff0c\u9759\u8109\u6ce8\u5c040.1 mg\/kg\u53ca\u4ee5\u4e0a\u5242\u91cf\u65f6\uff0cBAY-1753011\u5242\u91cf\u4f9d\u8d56\u7684\u963b\u65ad\u4e86\u9ebb\u9189\u96c4\u6027SD\u5927\u9f20\u7531\u6297\u5229\u5c3f\u4f5c\u7528\u8bf1\u5bfc\u7684\u6536\u7f29\u538b\u5347\u9ad8\u3002(Kolkhof, P. et al. ESC Congr (Aug 25-29, Munich) 2018, Abst P1263)\u3002<\/p>\n


                  <\/p>\n

                  2018\u5e74<\/span>8\u670821\u65e5\uff0c\u65b0\u578b\u53e3\u670d\u9009\u62e9\u6027apelin\u6fc0\u52a8\u5242AM-2995\u6709\u671b\u7528\u4e8e\u6cbb\u7597\u5fc3\u810f\u75c5<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  Apelin\u591a\u80bd\uff08APLN\uff09\u662fApelin\u53d7\u4f53\uff08APLNR\uff09\u7684\u5185\u6e90\u6027\u914d\u4f53\uff0c\u5728\u4eba\u7c7b\u5fc3\u8840\u7ba1\u529f\u80fd\u4e2d\u8d77\u5173\u952e\u4f5c\u7528\u3002\u7531\u4e8eapelin\u591a\u80bd\u7c7b\u4f3c\u7269\u7684\u836f\u4ee3\u52a8\u529b\u5b66\u6027\u8d28\u8f83\u5dee\uff0c\u4e0d\u9002\u5408\u53e3\u670d\u6cbb\u7597\uff0c\u56e0\u6b64\u53d1\u73b0\u65b0\u7684\u975e\u80bd\u7c7b\u5c0f\u5206\u5b50apelin\u6fc0\u52a8\u5242\u662f\u76ee\u524d\u7814\u7a76\u7684\u91cd\u8981\u9886\u57df\u3002\u5b89\u8fdb\u516c\u53f8\u8fd1\u65e5\u53d1\u8868\u4e86\u4e00\u79cd\u65b0\u7684\u544b\u5583\u4e09\u5511\u884d\u751f\u7269AM-2995\uff0c\u8fd9\u662f\u4e00\u79cd\u6709\u6548\u4e14\u6709\u9009\u62e9\u6027\u7684apelin\u6fc0\u52a8\u5242\uff0c\u4ee5\u8bc1\u5b9e\u5177\u6709\u6cbb\u7597\u5fc3\u8870\u548c\u76f8\u5173\u5e76\u53d1\u75c7\u7684\u6f5c\u5728\u4f5c\u7528\u3002<\/p>\n


                  <\/p>\n

                  \u5728\u4f53\u5916\u5b9e\u9a8c\u4e2d\uff0c\u5316\u5408\u7269\u7684Ki\u503c\u4e3a0.2 nM\u3002\u5728GTP\u7ed3\u5408\u8bd5\u9a8c\u4e2d\uff0c\u5176\u6fc0\u52a8\u5242EC50\u503c\u4e3a3 nM\u3002\u7ed9\u4e88\u6025\u6027\u5fc3\u808c\u6897\u6b7b\u5c0f\u9f20\u6a21\u578b\u8fde\u7eed\u6ce8\u5c04AM-2995 30 mg\/kg\uff0c\u5728\u8d85\u8fc72\u4e2a\u6708\u7684\u65f6\u95f4\u5185\u5747\u6709\u826f\u597d\u7684\u7597\u6548\u3002(Ma, Z.M. et al. 256th Am ChemSoc (ACS) Natl Meet (August 19-23, Boston) 2018, Abst MEDI 108)\u3002\uff08\u8be6\u89c1\u4e13\u5229WO 2018097944\uff09\u3002<\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \"\u3010BioWorld<\/section>\n<\/section>\n<\/section>\n
                  \n
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                  \u56fe\u4e3a\u5316\u5408\u7269AM-2995\u7684\u7ed3\u6784<\/p>\n


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                  2018\u5e748\u670824\u65e5\uff0c\u4e0b\u4e00\u4ee3TYK2\u6291\u5236\u5242PF-06826647\u7684\u7ed3\u6784\u548c\u4e34\u5e8a\u524d\u7814\u7a76\u6570\u636e<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  Janus\u6fc0\u9176\uff08JAKs\uff09\u662f\u4e00\u7c7b\u975e\u53d7\u4f53\u916a\u6c28\u9178\u6fc0\u9176\uff0c\u7531JAK-1\u3001JAK-2\u3001JAK-3\u548cTYK2\u56db\u4e2a\u6210\u5458\u7ec4\u6210\uff0c\u4f5c\u7528\u4e8e\u7ec6\u80de\u56e0\u5b50\u4fe1\u53f7\u901a\u8def\uff0c\u4e0e\u708e\u75c7\u548c\u81ea\u8eab\u514d\u75ab\u6027\u75be\u75c5\u76f8\u5173\u3002TYK2\u4e0eJAK-2\u5171\u540c\u5728IL-23\u548cIL-12\u4fe1\u53f7\u4f20\u5bfc\u4e2d\u53d1\u6325\u91cd\u8981\u4f5c\u7528\uff0c\u4e5f\u4e0eI\u578b\u5e72\u6270\u7d20\u4fe1\u53f7\u4f20\u5bfc\u76f8\u5173\uff0c\u7c7b\u4f3c\u4e8eJAK-1\u3002TYK2\u88ab\u62a5\u9053\u4e0e\u514b\u7f57\u6069\u75c5\u3001\u6e83\u75a1\u6027\u7ed3\u80a0\u708e\u3001\u725b\u76ae\u7663\u3001\u7cfb\u7edf\u6027\u7ea2\u6591\u72fc\u75ae\u548c\u98ce\u6e7f\u6027\u5173\u8282\u708e\u76f8\u5173\u3002<\/p>\n


                  <\/p>\n

                  \u8f89\u745e\u516c\u53f8\u6700\u8fd1\u83b7\u5f97\u4e86\u4e00\u79cd\u9009\u62e9\u6027\u7684\u5f3a\u6548TYK2\u6291\u5236\u5242\uff0c\u7528\u4ee5\u5f00\u53d1\u4e0b\u4e00\u4ee3\u7684JAK\u6291\u5236\u5242\u3002\u5316\u5408\u7269\u5bf9JAK-1\u548cJAK-3\u5177\u6709\u9009\u62e9\u6027\uff0c\u4e14\u5177\u5907\u826f\u597d\u7684IL-12\u548cIL-23\u6291\u5236\u4f5c\u7528\u3002\u7814\u7a76\u4eba\u5458\u57fa\u4e8e\u5421\u5511\u5e76\u5421\u5576\u7c7b\u9aa8\u67b6\u5408\u6210\u4e86\u4e00\u7cfb\u5217\u7c7b\u4f3c\u7269\uff0c\u6700\u7ec8\u53d1\u73b0\u4e86\u5316\u5408\u7269PF-06826647\u3002\u8be5\u5316\u5408\u7269\u5bf9TYK2\uff0cJAK-1\u548cJAK-2\u7684\u6291\u5236\u6d3b\u6027\u5206\u522b\u4e3apIC50 = 7.8\uff0c6.4\u548c7.1\uff0c\u5728\u7ec6\u80de\u5b9e\u9a8c\u4e2d\u5bf9IL-12\u663e\u793a\u51fa\u4fe1\u53f7\u6291\u5236\uff0c\u5728\u4eba\u7c7b\u5168\u8840IL-12\u8bf1\u5bfc\u7684STAT4\u78f7\u9178\u5316\u5b9e\u9a8c\u4e2d\uff0cIC80\u4e3a22nM\u3002\uff08Gerstenberger, B.S. et al. 256th Am ChemSoc (ACS) Natl Meet (August 19-23, Boston) 2018, Abst MEDI 319\uff09\u3002<\/p>\n


                  <\/p>\n

                  \u76ee\u524d\uff0c\u4e00\u9879PF-06826647\u9488\u5bf9\u5065\u5eb7\u53d7\u8bd5\u8005\u548c\u6591\u5757\u578b\u94f6\u5c51\u75c5\u53d7\u8bd5\u8005\u7684I\u671f\u4e34\u5e8a\u7814\u7a76\u6b63\u5728\u62db\u52df\u60a3\u8005\uff08ClinicalTrials.gov \u7f16\u53f7NCT03210961)\u3002<\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
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                  \"\u3010BioWorld<\/section>\n<\/section>\n<\/section>\n
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                  \u56fe\u4e3aPF-6826647\u7684\u7ed3\u6784<\/span><\/p>\n


                  <\/p>\n

                  2018\u5e748\u670823\u65e5\uff0cNuevolution\u516c\u53f8\u62a5\u9053IL-17A\u5c0f\u5206\u5b50\u6291\u5236\u5242\u7684\u7814\u7a76\u8fdb\u5c55<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  Nuevolution\u516c\u53f8\u62a5\u9053\u4e86\u5176\u7ec6\u80de\u56e0\u5b50X\u9879\u76ee\u7684\u7814\u7a76\u8fdb\u5c55\uff0c\u5373IL-17A\u5c0f\u5206\u5b50\u6291\u5236\u5242\u7684\u5148\u5bfc\u5316\u5408\u7269\u5f00\u53d1\uff0c\u8fd9\u4e9b\u5c0f\u5206\u5b50\u53ef\u7528\u4e8e\u57fa\u4e8e\u5c40\u90e8\u548c\u5168\u8eab\u6cbb\u7597\u3002\u8be5\u516c\u53f8\u5229\u7528\u5176\u5316\u5b66\u5e73\u53f0\u548c\u836f\u7269\u53d1\u73b0\u4f18\u5316\u5e73\u53f0\u5bf9IL-17A\u5c0f\u5206\u5b50\u6291\u5236\u5242\u8fdb\u884c\u7b5b\u9009\u548c\u8bc6\u522b\uff0c\u5f97\u5230\u4e86\u4e00\u4e9b\u5f3a\u6548\u7684\u5148\u5bfc\u5316\u5408\u7269\u3002<\/p>\n


                  <\/p>\n

                  \u8fd9\u4e9b\u5316\u5408\u7269\u53ef\u4ee5\u9009\u62e9\u6027\u5730\u7ed3\u5408\u4eba\u7c7bIL-17A\u86cb\u767d\uff0c\u6709\u6548\u963b\u65adIL-17A\u5411\u89d2\u8d28\u7ec6\u80de\u7684\u4fe1\u53f7\u4f20\u5bfc\u3002Nuevolution\u516c\u53f8\u6700\u8fd1\u7684\u7814\u7a76\u6570\u636e\u8bc1\u5b9e\uff0c\u5176\u4e2d\u4e00\u4e2a\u5148\u5bfc\u5316\u5408\u7269\u5728\u5c0f\u9f20\u4f53\u5185\u5173\u8282\u708e\u6a21\u578b\u4e2d\u4e0e\u73b0\u6709\u7684IL-17A\u4e2d\u548c\u6297\u4f53\u6548\u679c\u76f8\u5f53\u3002X\u5c04\u7ebf\u7ed3\u6676\u884d\u5c04\u5b9e\u9a8c\u786e\u5b9a\u4e86\u5316\u5408\u7269\u4e0eIL-17A\u9776\u70b9\u7684\u7ed3\u5408\uff0c\u5e76\u660e\u786e\u4e86\u4e0d\u540c\u5316\u5b66\u7ed3\u6784\u6709\u7740\u4e0d\u540c\u7684\u7ed3\u5408\u673a\u5236\u3002\u516c\u53f8\u5c06\u7ee7\u7eed\u8fdb\u884c\u4f18\u5316\u5de5\u4f5c\u4ee5\u786e\u5b9a\u5019\u9009\u5316\u5408\u7269\u3002<\/p>\n


                  <\/p>\n

                  \u6b64\u5916\uff0c\u6709\u6570\u636e\u652f\u6301\u8fd9\u4e9b\u76f4\u63a5\u9776\u5411IL-17A\u7684\u5c0f\u5206\u5b50\u6709\u671b\u5728\u4e34\u5e8a\u6548\u679c\u4e0a\u4e0eIL-17A\u6297\u4f53\u76f8\u5f53\u3002\u8be5\u516c\u53f8\u76ee\u524d\u7684\u91cd\u70b9\u662f\u786e\u5b9a\u6570\u636e\u4ee5\u5f00\u5c55IL-17A\u6291\u5236\u5242\u5728\u5c40\u90e8\u6cbb\u7597\u4e2d\u7684\u7814\u7a76\uff0c\u540c\u65f6\u5f00\u5c55\u7528\u4e8e\u5168\u8eab\u6cbb\u7597\u7684\u5236\u5242\u7814\u7a76\uff0c\u671f\u671b\u5f00\u53d1\u51fa\u5728\u5c40\u90e8\u548c\u5168\u8eab\u6cbb\u7597\u5747\u53ef\u7528\u7684\u539f\u521b\u5019\u9009\u836f\u7269\u3002\u4ee5IL-17\u901a\u8def\u4e3a\u9776\u6807\u7684\u6cbb\u7597\u53ef\u80fd\u5728\u94f6\u5c51\u75c5\u3001\u94f6\u5c51\u75c5\u5173\u8282\u708e\u548c\u5176\u4ed6\u708e\u75c7\u6027\u75be\u75c5\u4e2d\u5177\u6709\u6f5c\u5728\u7684\u5e94\u7528\u4ef7\u503c\u3002\u516c\u53f8\u5c06\u5f00\u59cb\u4e3a\u8fd9\u4e2a\u9879\u76ee\u5bfb\u627e\u5408\u4f5c\u673a\u4f1a\u3002\uff08Nuevolution\u516c\u53f8\u65b0\u95fb\u7a3f\uff09\u3002<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  2018\u5e748\u670824\u65e5\uff0c\u809d\u9776\u5411\u524d\u836f\u6709\u671b\u7528\u4e8e\u6cbb\u7597\u809d\u7ea4\u7ef4\u5316<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  \u9ebb\u7701\u7406\u5de5\u5b66\u9662\u548cXTuit Pharmaceuticals\u516c\u53f8\u7684\u7814\u7a76\u4eba\u5458\u62a5\u9053\uff0c\u4ed6\u4eec\u5408\u7406\u5730\u8bbe\u8ba1\u4e86\u4e00\u79cd\u8840\u7ba1\u7d27\u5f20\u7d20II\u578b\u53d7\u4f53\u963b\u6ede\u5242\uff08ARB\uff09\u2014\u6297\u9ad8\u8840\u538b\u836f\u7269\u66ff\u7c73\u6c99\u5766\uff08telmisartan\uff09\u7684\u5927\u5206\u5b50\u524d\u836f\uff0c\u6570\u636e\u663e\u793a\u5b83\u80fd\u591f\u6210\u529f\u5730\u51cf\u5c11\u52a8\u7269\u6a21\u578b\u7684\u809d\u7ea4\u7ef4\u5316\u3002\u7531\u9ebb\u7701\u7406\u5de5\u5b66\u9662\u5316\u5b66\u7cfb\u526f\u6559\u6388Jeremiah Johnson\u548cXTuit Pharmaceuticals\u516c\u53f8\u524d\u9996\u5e2d\u79d1\u5b66\u5b98\u3001Acrivon Therapeutics \u516c\u53f8\u521b\u59cb\u4ebaPeter Blume-Jensen\u9886\u5bfc\u7684\u7814\u7a76\u56e2\u961f\uff0c\u8bc1\u660e\u4e86\u8be5\u524d\u836f\u5e76\u6ca1\u6709\u5bfc\u81f4\u5168\u8eab\u6027\u4f4e\u8840\u538b\uff0c\u663e\u793a\u5176\u4e0d\u4f1a\u5728\u975e\u5fc3\u8840\u7ba1\u6cbb\u7597\u9886\u57df\u4ea7\u751f\u526f\u4f5c\u7528\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u9152\u7cbe\u548c\u975e\u9152\u7cbe\u6027\u8102\u80aa\u6027\u809d\u708e\u3001\u75c5\u6bd2\u6027\u809d\u708e\u662f\u7ea4\u7ef4\u5316\u6700\u5e38\u89c1\u7684\u81f4\u75c5\u56e0\u7d20\uff0c\u665a\u671f\u53d1\u5c55\u4e3a\u809d\u786c\u5316\u53ef\u5bfc\u81f4\u5168\u7403\u8d85\u8fc7100\u4e07\u4eba\u6b7b\u4ea1\uff0c\u7ea6\u53602010\u5e74\u6240\u6709\u6b7b\u4ea1\u4eba\u6570\u76842%\u3002\u8fd9\u79cd\u76ee\u524d\u5c1a\u65e0\u6709\u6548\u6cbb\u7597\u65b9\u6cd5\u7684\u75be\u75c5\u786e\u8bca\u540e\u7684\u9884\u540e\u5f88\u5dee\uff0c\u809d\u786c\u5316\u5931\u4ee3\u507f\u671f\u76845\u5e74\u751f\u5b58\u7387\u4ec5\u4e3a45%\u3002<\/span><\/p>\n


                  <\/p>\n

                  \u5728\u4e34\u5e8a\u524d\u7814\u7a76\u4e2d\uff0c\u5c0f\u5206\u5b50ARBs\u53ef\u6291\u5236\u80be\u7d20-\u8840\u7ba1\u7d27\u5f20\u7d20\u7cfb\u7edf\uff08RAS\uff09\uff0c\u5df2\u88ab\u8bc1\u660e\u53ef\u4ee5\u9650\u5236\u809d\u57fa\u8d28\u7ec6\u80de\u7684\u6d3b\u5316\u3001\u589e\u6b96\u3001\u708e\u75c7\u548c\u6c27\u5316\u5e94\u6fc0\uff0c\u800c\u8fd9\u4e9b\u90fd\u4e0e\u7ea4\u7ef4\u5316\u76f8\u5173\u3002Blume-Jensen\u544a\u8bc9BioWorld\uff1a\u201c\u8fd9\u662fARBs\u56fa\u6709\u7684\u4e00\u79cd\u6548\u5e94\uff0c\u5b83\u4eec\u5747\u9488\u5bf9\u8840\u7ba1\u7d27\u5f20\u7d20II\u578b\u53d7\u4f53\u4ea7\u751f\u7c7b\u4f3c\u7684\u6548\u5e94\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u6211\u4eec\u9009\u62e9\u66ff\u7c73\u6c99\u5766\u662f\u56e0\u4e3a\u5b83\u662f\u6700\u5f3a\u6548\u7684ARBs\u4e4b\u4e00\u3002\u201dBlume-Jensen\u8bf4\uff1a\u201c\u5927\u91cf\u7814\u7a76\u8868\u660eARBs\u53ef\u4ee5\u51cf\u5c11\u8f7b\u5ea6\u60a3\u8005\u7684\u7ea4\u7ef4\u5316\uff0c\u4f46\u76ee\u524d\u9762\u4e34\u7684\u6311\u6218\u662f\u5728\u66f4\u665a\u671f\u7684\u809d\u75c5\u60a3\u8005\u4e2dARBs\u7684\u8840\u538b\u4e0b\u964d\u4f5c\u7528\u3002\u201d\u4ed6\u6307\u51fa\uff0c\u201c\u4f4e\u8840\u538b\u5728\u8fd9\u7c7b\u60a3\u8005\u4e2d\u5f88\u5e38\u89c1\uff0c\u800c\u4e14\u7531\u4e8e\u809d\u810f\u4ee3\u8c22\u53d7\u635f\u4f1a\u5bfc\u81f4\u836f\u7269\u7d2f\u79ef\u52a0\u91cd\u3002\u201d<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u4e3a\u4e86\u5e94\u5bf9\u8fd9\u4e9b\u6311\u6218\uff0cXTuit\u4e0e\u9ebb\u7701\u7406\u5de5\u5b66\u9662\u7684Johnson\u56e2\u961f\u5408\u4f5c\uff0c\u8bbe\u8ba1\u4e86\u4e00\u4e2a\u6a21\u5757\u5316\u7684\u3001\u53ef\u6269\u5c55\u7684\u524d\u836f\u5408\u6210\u5e73\u53f0\u3002\u7814\u7a76\u4eba\u5458\u8bbe\u8ba1\u4f18\u5316\u4e86\u66ff\u7c73\u6c99\u5766\u524d\u836f\uff0c\u4f7f\u5176\u80fd\u591f\u5728\u7ea4\u7ef4\u5316\u809d\u7ec4\u7ec7\u4e2d\u4f18\u5148\u91ca\u653e\u6d3b\u6027\u836f\u7269\u5e76\u7ef4\u6301\u7a33\u5b9a\u7684\u6cbb\u7597\u5242\u91cf\u3002\u540c\u65f6\uff0cBlume-Jensen\u9886\u5bfc\u7740XTuit\u7684\u79d1\u5b66\u5bb6\u56e2\u961f\u8fdb\u884c\u751f\u7269\u5b66\u7814\u7a76\u3001\u5de5\u827a\u653e\u5927\u548c\u5206\u6790\u5de5\u4f5c\uff0c\u6700\u7ec8\u79fb\u4ea4\u7ed9CMO\u8fdb\u884c\u751f\u4ea7\u5236\u9020\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u7814\u7a76\u4eba\u5458\u8bbe\u8ba1\u7684\u4e00\u79cd\u66ff\u7c73\u6c99\u5766\u661f\u5f62\u805a\u5408\u7269\uff08Tel-BASPs\uff09\u83b7\u5f97\u4e86\u6700\u4f73\u7684\u836f\u7269\u91ca\u653e\u3002BASPs\u7531\u591a\u4e2a\u5355\u4f53\u7ec4\u5408\u6210\u5927\u5206\u5b50\uff0c\u6bcf\u4e2a\u5355\u4f53\u90fd\u6709\u4e0e\u4e4b\u7ed3\u5408\u7684\u6d3b\u6027\u836f\u7269\uff0c\u518d\u901a\u8fc7\u4ea4\u8054\u5f62\u6210\u66f4\u9ad8\u9636\u7684\u7ed3\u6784\u3002Johnson\u4ecb\u7ecd\u8bf4\uff1a\u201c\u6211\u4eec\u53ef\u4ee5\u63a7\u5236\u4ea4\u8054\u6570\u91cf\u548c\u524d\u4f53\u836f\u7269\u7684\u5927\u5c0f\uff0c\u66f4\u91cd\u8981\u7684\u662f\uff0c\u80fd\u591f\u6839\u636e\u53ef\u53d8\u7684\u5316\u5b66\u8fde\u63a5\u65b9\u6cd5\u63a7\u5236\u4e0d\u540c\u7ec4\u7ec7\u4e2d\u7684\u6d3b\u6027\u836f\u7269\u7684\u91ca\u653e\u901f\u7387\u3002\u6839\u636e\u4ee5\u4e0a\u65b9\u6cd5\uff0c\u6700\u7ec8\u7684Tel-BASPs\u662f\u7528\u4f18\u5316\u8fc7\u7684\u916f\u94fe\u8fdb\u884c\u8fde\u63a5\u7684\uff0c\u4f7f\u5f97\u6d3b\u6027\u836f\u7269\u5728\u60a3\u8005\u809d\u810f\u4e2d\u663e\u793a\u4e86\u826f\u597d\u7684\u91ca\u653e\u7387\uff0c\u800c\u5168\u8eab\u6027\u91ca\u653e\u7387\u5219\u8981\u4f4e\u5f97\u591a\u3002\u201d<\/span><\/p>\n


                  <\/span><\/p>\n

                  XTuit\u56e2\u961f\u968f\u540e\u5728\u300aNature Biomedical Engineering\u300b\u6742\u5fd7\u4e0a\u5bf9\u5de5\u4f5c\u8fdb\u884c\u4e86\u62a5\u9053\uff0c\u6570\u636e\u663e\u793a\uff0c\u8fd9\u4e9b\u524d\u4f53\u836f\u7269\u5728\u4ee3\u8c22\u548c\u5316\u5b66\u8bf1\u5bfc\u7684\u5c0f\u9f20\u809d\u7ea4\u7ef4\u5316\u6a21\u578b\u4e2d\u5747\u6709\u7597\u6548\uff0c\u5e76\u4e14\u907f\u514d\u4e86\u5242\u91cf\u9650\u5236\u6027\u4f4e\u8840\u538b\u7684\u53d1\u751f\u3002Blume-Jensen\u8bf4\uff1a\u201c\u6211\u4eec\u5728\u4f53\u5185\u8fdb\u884c\u4e86\u8d85\u8fc76\u5468\u7684\u7814\u7a76\uff0c\u5728\u6301\u7eed\u7ed9\u52a8\u7269\u6ce8\u5c04\u8bf1\u5bfc\u7ea4\u7ef4\u5316\u7684\u56db\u6c2f\u5316\u78b3\u540e\uff0c\u836f\u7269\u4ecd\u53ef\u663e\u8457\u5730\u51cf\u5c11\u7ea4\u7ef4\u5316\u7684\u53d1\u751f\u3002\u5728\u6b64\u671f\u95f4\uff0c\u836f\u7269\u5728\u8840\u6db2\u4e2d\u7684\u6d53\u5ea6\u660e\u663e\u4f4e\u4e8e\u5f15\u8d77\u964d\u4f4e\u8840\u538b\u7684\u6d53\u5ea6\u3002\u201d\u8be5\u7597\u6cd5\u7684\u5b89\u5168\u6027\u548c\u6709\u6548\u6027\u4e5f\u901a\u8fc7\u7ec4\u7ec7\u75c5\u7406\u5b66\u3001ALT\u3001AST\u6c34\u5e73\u3001\u7ec4\u7ec7\u86cb\u767d\u6807\u5fd7\u7269\u6d4b\u8bd5\u3001\u809d\u7ec6\u80de\u574f\u6b7b\u4fdd\u62a4\u3001\u57fa\u56e0\u8868\u8fbe\u5206\u6790\u7b49\u591a\u79cd\u65b9\u6cd5\u8bc1\u5b9e\u3002Blume-Jensen\u8bf4\uff1a\u201c\u6240\u6709\u6570\u636e\u90fd\u5f88\u597d\u5730\u8bc1\u660e\u4e86\u809d\u810f\u7684\u6b63\u5e38\u5de5\u4f5c\uff0c\u5c3d\u7ba1\u5728Tel-BASPs\u6cbb\u7597\u8fc7\u7a0b\u4e2d\u56db\u6c2f\u5316\u78b3\u4e00\u76f4\u5728\u5bf9\u809d\u810f\u8fdb\u884c\u6bd2\u6027\u653b\u51fb\u3002\u201d<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u5728\u5927\u9f20\u548c\u72d7\u7684\u809d\u810f\u7ec4\u7ec7\u4e2d\uff0c\u524d\u836f\u80fd\u591f\u88ab\u957f\u671f\u4fdd\u7559\u7684\u4e14\u5177\u6709\u826f\u597d\u7684\u8010\u53d7\u6027\u3002\u6570\u636e\u663e\u793a\u836f\u7269\u53ef\u4ee5\u88ab\u4fdd\u7559\u6570\u6708\uff0c\u5e76\u4ece\u524d\u836f\u4e2d\u6301\u7eed\u91ca\u653e\u5e76\u53d1\u6325\u4f5c\u7528\u3002\u201dBlume-Jensen\u8bf4\u3002\u201c\u6211\u4eec\u76f8\u4fe1\u8fd9\u6709\u5e0c\u671b\u8f6c\u5316\u4e3a\u5bf9\u809d\u7ea4\u7ef4\u5316\u60a3\u8005\u975e\u5e38\u6709\u5229\u7684\u6cbb\u7597\u65b9\u6cd5\uff0c\u5c31\u4f9d\u4ece\u6027\u800c\u8a00\u4e5f\u5177\u6709\u7f8e\u597d\u7684\u524d\u666f\u3002\u201d\u9664\u4e86\u76ee\u524d\u7684\u805a\u5408\u7269\uff0c\u6211\u4eec\u8fd8\u6709\u4e00\u79cd\u540d\u4e3aTel-Brush\u7684\u66f4\u4f4e\u5206\u5b50\u91cf\u7684\u524d\u836f\uff0c\u5b83\u5728\u4f53\u5185\u7684\u6548\u679c\u53ef\u80fd\u66f4\u597d\u3002\u201d\u8fd9\u4e9b\u53d1\u73b0\u652f\u6301\u4e86\u66ff\u7c73\u6c99\u5766\u524d\u836f\u7684\u8fdb\u4e00\u6b65\u53d1\u5c55\uff0c\u8fd9\u79cd\u836f\u7269\u5728\u809d\u7ea4\u7ef4\u5316\u9886\u57df\u5f88\u5c11\u4f7f\u7528\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u201c\u5728Acrivon Therapeutics\uff0c\u6211\u4eec\u540c\u65f6\u6b63\u5728\u57fa\u4e8e\u540c\u6837\u7684\u5e73\u53f0\u63a8\u8fdb\u524d\u836f\u7814\u7a76\uff0c\u76ee\u6807\u662f\u6cbb\u7597\u764c\u75c7\u3002\u201dBlume-Jensen\u4e0eJohnson\u5171\u540c\u521b\u5efa\u4e86\u8fd9\u5bb6\u516c\u53f8\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  Blume-Jensen\u8bf4\uff1a\u201c\u968f\u7740Tel-BASP\u6216Tel-Brush\u7684\u7814\u7a76\uff0c\u4e00\u65e6\u6211\u4eec\u7684\u524d\u836f\u901a\u8fc7\u4e86\u764c\u75c7\u6216\u5176\u4ed6\u9002\u5e94\u75c7IND\u7533\u62a5\uff0c\u5c06\u4e3a\u8fd9\u7c7b\u524d\u836f\u5728\u5176\u4ed6\u9886\u57df\u7684\u5e94\u7528\u63a8\u5f00\u5927\u95e8\u3002\u201d Johnson\u8bf4\uff1a\u201c\u8fd9\u4e2a\u6982\u5ff5\u4e0d\u4ec5\u5728\u809d\u75c5\u5177\u6709\u5438\u5f15\u529b\uff0c\u5728\u5176\u4ed6\u6cbb\u7597\u9886\u57df\u4e5f\u4e00\u6837\u3002\u6211\u4eec\u6253\u7b97\u7ee7\u7eed\u5229\u7528Acrivon\u5e73\u53f0\u7684\u4f18\u52bf\uff0c\u5c06\u4e34\u5e8a\u4e0a\u5df2\u8bc1\u5b9e\u6709\u6548\u7684\u836f\u7269\u901a\u8fc7\u4ea4\u8054\u7684\u65b9\u5f0f\u5e94\u7528\u5230\u66f4\u5e7f\u6cdb\u7684\u9886\u57df\u201d\u3002\uff08Golder, M.R. et al. Nat Biomed Engineer 2018 Adv. Publication\uff09\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \"\u3010BioWorld<\/section>\n<\/section>\n<\/section>\n
                  \n
                  \n
                  \n

                  \u56fe\u4e3a\u66ff\u7c73\u6c99\u5766\u7684\u7ed3\u6784<\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \n


                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \n

                  2018\u5e748\u670831\u65e5\uff0cBMS\u62a5\u9053\u65b0\u7684\u53d7\u4f53\u76f8\u4e92\u4f5c\u7528\u4e1d\/\u82cf\u6c28\u9178\u86cb\u767d\u6fc0\u91761\u6291\u5236\u5242<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  <\/section>\n
                  \n


                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \n

                  \u767e\u65f6\u7f8e\u65bd\u8d35\u5b9d\u516c\u53f8\u53d1\u73b0\u4e86\u4e00\u7c7b\u6c28\u57fa\u4e09\u6c2e\u5511\u5e76\u5421\u5576\u7c7b\u5316\u5408\u7269\u4f5c\u4e3a\u53d7\u4f53\u76f8\u4e92\u4f5c\u7528\u7684\u4e1d\/\u82cf\u6c28\u9178\u86cb\u767d\uff08RIP-1\uff09\u6fc0\u9176\u6291\u5236\u5242\uff0c\u6709\u671b\u7528\u4e8e\u6cbb\u7597\u708e\u75c7\u6027\u80a0\u75c5\uff08\u5305\u62ec\u6e83\u75a1\u6027\u7ed3\u80a0\u708e\u548c\u514b\u7f57\u6069\u75c5\uff09\u3001\u725b\u76ae\u7663\u3001\u5fc3\u529b\u8870\u7aed\u3001\u975e\u9152\u7cbe\u6027\u8102\u80aa\u6027\u809d\u708e\u548c\u7c7b\u98ce\u6e7f\u5173\u8282\u708e\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u4ee3\u8868\u5316\u5408\u7269\u5728HTRF\u7ed3\u5408\u8bd5\u9a8c\u4e2d\u5bf9RIP-1\u6fc0\u9176\u7684\u6291\u5236\u6d3b\u6027\u4e3aIC50 < 20 nM\u3002\u5b83\u80fd\u5728TNF-alpha\u8bf1\u5bfc\u7a0b\u5e8f\u6027\u574f\u6b7b\u7684\u4eba\u7ed3\u76f4\u80a0\u764c\u7ec6\u80deHT-29-L23\u4e2d\u6291\u5236MLKL\u7684\u78f7\u9178\u5316\uff08IC50 < 20 nM\uff09\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u8be5\u5316\u5408\u7269\u57280.1 mg\/kg\u53e3\u670d\u5242\u91cf\u4e0b\u4fdd\u62a4\u4e86TNF-alpha\u8bf1\u5bfc\u7684RIP-1\u6fc0\u9176\u4f9d\u8d56\u7684\u5168\u8eab\u708e\u75c7\u53cd\u5e94\u7efc\u5408\u5f81\u96cc\u6027\u5c0f\u9f20C57BL\/6\u6a21\u578b\u7684\u4f53\u6e29\u4e0b\u964d\uff08\u76f8\u5bf9\u4e8e\u9633\u6027\u5bf9\u7167\u63d0\u534780%\uff09\uff0c\u5e76\u51cf\u5c11\u4e86IL-6\u7ec6\u80de\u56e0\u5b50\u6c34\u5e73\uff08\u76f8\u5bf9\u4e8e\u9633\u6027\u5bf9\u7167\u51cf\u5c11\u4e8693%\uff09\u3002\uff08\u8be6\u89c1\u4e13\u5229WO 2018148626\uff09\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \"\u3010BioWorld<\/section>\n<\/section>\n<\/section>\n
                  \n
                  \n
                  \n

                  \u56fe\u4e3aWO 2018148626\u4e2d\u4ee3\u8868\u5316\u5408\u7269\u7684\u7ed3\u6784<\/p>\n


                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

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                  \n
                  <\/section>\n<\/section>\n
                  \n
                  <\/section>\n<\/section>\n
                  <\/section>\n<\/section>\n
                  \n
                  \n

                  \u5185\u5206\u6ccc\u7cfb\u7edf\u75be\u75c5<\/p>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \n

                  2018\u5e748\u670828\u65e5, \u9ed8\u514b\u516c\u53f8\u62a5\u9053\u4e86GPR40\u53d8\u6784\u5b8c\u5168\u6fc0\u52a8\u5242\u7684\u7814\u53d1\u8fdb\u7a0b<\/span><\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  <\/section>\n
                  \n


                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \n

                  \u9ed8\u514b\u516c\u53f8\u7684\u7814\u7a76\u4eba\u5458\u5f00\u53d1\u4e86\u4e00\u79cdGPR40\uff08\u6e38\u79bb\u8102\u80aa\u9178\u53d7\u4f531\uff09\u7684\u53d8\u6784\u5b8c\u5168\u6fc0\u52a8\u5242AgoPAMs\u3002GPR40\u7684\u90e8\u5206\u6fc0\u52a8\u5242\u53ef\u4ee5\u964d\u4f4e\u8840\u7cd6\u6c34\u5e73\uff0c\u800c\u5b8c\u5168\u6fc0\u52a8\u5242\u5df2\u88ab\u8bc1\u660e\u80fd\u591f\u63d0\u4f9b\u66f4\u52a0\u7684\u964d\u7cd6\u6548\u679c\u3002\u8fd9\u79cdGPR40\u7684\u5b8c\u5168\u6fc0\u52a8\u5242\u662f\u57fa\u4e8e\u5316\u5408\u7269TAK-875\u53d1\u73b0\u7684\uff0cTAK-875\u662f\u4e00\u79cd\u4e8e2013\u5e74\u505c\u6b62\u4f7f\u7528\u7684GPR40\u90e8\u5206\u6fc0\u52a8\u5242\u3002\u6570\u636e\u663e\u793a\uff0c\u5019\u9009\u5316\u5408\u7269I\u5728\u4eba\u3001\u5927\u9f20\u548c\u5c0f\u9f20\u4e2d\u5bf9GPR40\u7684EC50\u503c\u5206\u522b\u4e3a0.6\u30012.9\u548c1.7 nM\uff0c\u5728pH\u4e3a2\u30016.5\u548c7.0\u65f6\u7684\u6eb6\u89e3\u5ea6\u5206\u522b\u4e3a27\u3001147\u548c121 mcM\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u5bf9Goto-Kakizaki\u5927\u9f20\u8fdb\u884c\u7684\u4f53\u5185\u7814\u7a76\u663e\u793a\uff0c3\u300110\u548c30 mg\/kg\u5242\u91cf\u7684\u9776\u6807\u7ed3\u5408\u7387\u5206\u522b\u4e3a49%\u300168%\u548c82%\u3002\u5927\u9f20\u7684\u836f\u4ee3\u52a8\u529b\u5b66\u9776\u6807\u7ed3\u5408\u7387\u5448\u5242\u91cf\u4f9d\u8d56\u5173\u7cfb\uff0c30mg \/kg\u7684\u5242\u91cf\u57281\u30013\u30015\u548c24\u5c0f\u65f6\u7684\u9776\u6807\u7ed3\u5408\u5206\u522b\u4e3a83%\u300186%\u300187%\u548c75%\uff0c\u800cTAK-875\u5206\u522b\u4e3a90%\u300194%\u300193%\u548c41%\u3002\u901a\u8fc7\u4f53\u5185\u6570\u636e\u5916\u63a8\uff0c\u9884\u8ba14mg\/70kg\u5242\u91cf\u7684 Cmax\u4e3a 479 nM\uff0cCmin\u4e3a233nM\uff1b\u5728\u8fdb\u884c\u5242\u91cf\u4e3a10mg\/70kg\u7684\u5f02\u901f\u6bd4\u4f8b\u653e\u5927\u65f6\uff0c Cmax\u4e3a815nM\uff0c\u800cCmin\u7ef4\u6301\u4e0d\u53d8\uff0c\u8868\u660e\u5316\u5408\u7269\u6709\u671b\u5728\u8f83\u4f4e\u5242\u91cf\u4e0b\u8d77\u6548\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u66b4\u9732\u91cf\u6570\u636e\u663e\u793a\uff0c750 mg\/kg\/day\u7684AUC\u4e3a1520 mcM*h\uff0c\u4e0e200 mg\/kg\/day\u7684AUC = 1300 mcM*h\u76f8\u6bd4\u4ec5\u7565\u6709\u589e\u52a0\u3002\u6b64\u5916\uff0cAgoPAM\u5f15\u8d77\u7684\u80a0\u4fc3\u80f0\u5c9b\u7d20\u91ca\u653e\u4e0d\u540c\u4e8e\u5148\u524d\u62a5\u9053\u7684TAK-875\u3002\u4e0a\u8ff0\u7ed3\u679c\uff0c\u518d\u52a0\u4e0a\u6ca1\u6709\u89c2\u5bdf\u5230\u836f\u7269\u5bf9\u809d\u810f\u7684\u5f71\u54cd\uff0c\u652f\u6301\u5bf9\u8be5\u5316\u5408\u7269\u8fdb\u884c\u8fdb\u4e00\u6b65\u7814\u7a76\u3002\uff08DeMong, D. et al. 256 Am ChemSoc (ACS) Natl Meet (august 19-23, Boston) 2018, Abst medi311\uff09\u3002\u5316\u5408\u7269I\u5728\u4e13\u5229WO 2014130608\u4e2d\u88ab\u62a5\u9053\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \"\u3010BioWorld<\/section>\n<\/section>\n<\/section>\n
                  \n
                  \n
                  \n

                  \u56fe\u4e3a\u5316\u5408\u7269I\u7684\u7ed3\u6784<\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \n
                  \n
                  \n
                  <\/section>\n<\/section>\n
                  \n
                  <\/section>\n<\/section>\n
                  <\/section>\n<\/section>\n
                  \n
                  \n

                  \u6297\u611f\u67d3\u836f\u7269<\/p>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  <\/section>\n<\/section>\n
                  \n
                  <\/section>\n<\/section>\n
                  <\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n
                  \n
                  \n
                  \n

                  2018\u5e748\u670830\u65e5\uff0c\u6297\u759f\u5019\u9009\u65b0\u836fGSK-701\u5177\u6709\u826f\u597d\u7684\u53e3\u670d\u751f\u7269\u6709\u6548\u6027<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  <\/section>\n
                  \n


                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \n

                  GSK-701\u662f\u845b\u5170\u7d20\u53f2\u514b\u516c\u53f8\u901a\u8fc7\u8868\u578b\u7b5b\u9009\u53d1\u73b0\u7684\u4e00\u79cd\u65b0\u578b\u5421\u54af\u70f7\u80fa\u7c7b\u6297\u759f\u5316\u5408\u7269\uff0c\u8fd1\u65e5GSK\u62a5\u9053\u4e86\u8be5\u5316\u5408\u7269\u7684\u7ed3\u6784\u548c\u4e34\u5e8a\u524d\u6570\u636e\u3002GSK-701\u5728\u5bcc\u542b\u8102\u8d28\u7684\u5c0f\u725b\u8840\u6e05\u4e2d\u5bf9\u6076\u6027\u759f\u539f\u866b\u7684IC50\u4e3a0.006 mcM\uff0c\u5728\u4eba\u8840\u6e05\u4e2d\u7684IC50 = 0.009 mcM\uff0c\u5e76\u663e\u793a\u4e86\u76f8\u6bd4\u9752\u84bf\u7d20\u66f4\u5feb\u901f\u7684\u759f\u539f\u866b\u6740\u4f24\u7387\u3002\u5b83\u5bf9\u4efb\u4f55\u5e38\u89c1\u7684CYP\u4e9a\u578b\u5747\u6ca1\u6709\u660e\u663e\u6291\u5236\uff08IC50 > 90 mcM\uff09\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u5728\u6076\u6027\u759f\u539f\u866b\u611f\u67d3\u6a21\u578b\u4e2d\u53e3\u670d\u6709\u6548\uff08ED90 = 0.2 mg\/kg\uff09\uff0c\u4e14\u5177\u6709\u826f\u597d\u7684\u66b4\u9732\u91cf\uff08\u5728ED90\u6d53\u5ea6\u4e0b\u7684AUC\u4e3a0.08 mcg*h\/mL\/day\uff09\u3002\u5c0f\u9f20\u3001\u5927\u9f20\u548c\u72d7\u7684\u7814\u7a76\u8bc1\u5b9e\uff0cGSK-701\u5177\u6709\u9002\u5b9c\u7684\u53e3\u670d\u836f\u4ee3\u52a8\u529b\u5b66\u7279\u5f81\u548c\u8f83\u4f4e\u7684\u809d\u810f\u6e05\u9664\u7387\u3002\u6839\u636e\u76ee\u524d\u7684\u6570\u636e\u9884\u6d4b\uff0c\u5bf9\u4eba\u4f53\u8fdb\u884c\u53e3\u670d\u7ed9\u836f\uff0c\u8be5\u5316\u5408\u7269\u5e94\u5177\u5907\u751f\u7269\u5229\u7528\u5ea6\u9ad8\uff0890%\uff09\uff0c\u6e05\u9664\u7387\u4f4e\uff081.8 mL\/min\/kg\uff09\u548c\u5206\u5e03\u9002\u4e2d\uff082.00 L\/kg\uff09\u7b49\u7279\u70b9\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u8fdb\u4e00\u6b65\u7684\u836f\u4ee3\u52a8\u529b\u5b66\u7814\u7a76\u8868\u660e\uff0c\u8001\u9f20\u6bcf\u65e5\u4e00\u6b2130mg\u5242\u91cf\u53e3\u670d3\u5929\u540e\u8868\u73b0\u51fa\u7684\u836f\u52a8\u5b66\u7279\u5f81\uff08Cmax = 208 ng \/ mL\uff0cAUC0 – 120 h * h = 10691 ng \/ mL\uff09\uff0c\u76f8\u6bd4\u5355\u6b21\u53e3\u670d250\u6beb\u514b\uff08Cmax = 856 ng \/ mL\uff0cAUC0 – 120 h 28070 ng * h \/ mL\uff09\u66f4\u5177\u4f18\u52bf\uff0c\u4e14\u8fd9\u4e24\u4e2a\u5242\u91cf\u65b9\u6848\u5747\u6709\u5f88\u597d\u7684\u5b89\u5168\u6027\u3002\u76ee\u524d\uff0c\u8be5\u836f\u6b63\u5728\u8ba1\u5212\u5bf9\u5065\u5eb7\u5fd7\u613f\u8005\u548c\u60a3\u6709\u6076\u6027\u759f\u539f\u866b\u5fd7\u613f\u8005\u8fdb\u884c\u4e34\u5e8a\u7814\u7a76\u4ee5\u786e\u5b9a\u6700\u4f73\u5242\u91cf\u3002(Rami, H. et al. 256th Am ChemSoc (ACS) Natl Meet (August 19-23, Boston) 2018, Abst MEDI 332)\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \"\u3010BioWorld<\/section>\n<\/section>\n<\/section>\n
                  \n
                  \n
                  \n

                  \u56fe\u4e3aGSK-701\u7684\u7ed3\u6784<\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
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                  \n
                  <\/section>\n<\/section>\n
                  \n
                  <\/section>\n<\/section>\n
                  <\/section>\n<\/section>\n
                  \n
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                  \u547c\u5438\u7cfb\u7edf\u75be\u75c5<\/p>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  <\/section>\n<\/section>\n
                  \n
                  <\/section>\n<\/section>\n
                  <\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n
                  \n
                  \n
                  \n

                  2018\u5e748\u670810\u65e5\uff0c\u963f\u65af\u5229\u5eb7\u53d1\u73b0\u65b0\u578bJAK1\u6291\u5236\u5242<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  <\/section>\n
                  \n


                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
                  \n
                  \n

                  \u963f\u65af\u5229\u5eb7\u516c\u53f8\u62a5\u9053\u4e86\u4e00\u7c7bJanus\u6fc0\u91761\uff08JAK1\uff09\u6291\u5236\u5242\uff0c\u6709\u671b\u7528\u4e8e\u6cbb\u7597\u54ee\u5598\uff0c\u72fc\u75ae\uff0cI\u578b\u7cd6\u5c3f\u75c5\uff0c\u591a\u53d1\u6027\u786c\u5316\u75c7\uff0c\u98ce\u6e7f\u6027\u5173\u8282\u708e\uff0c\u708e\u75c7\u6027\u80a0\u75c5\uff0c\u6591\u79c3\u548c\u81ea\u8eab\u514d\u75ab\u6027\u7532\u72b6\u817a\u75be\u75c5\u7b49\u3002\u4ee3\u8868\u5316\u5408\u7269\u80fd\u591f\u663e\u8457\u7684\u6291\u5236\u91cd\u7ec4JAK1\uff08IC50 < 0.003 mcM\uff09\uff0c\u4e14\u5bf9JAK2\u548cJAK3\u5177\u6709\u9009\u62e9\u6027\uff08IC50 = 1.22\uff0cIC50 > 30 mcM\uff09\u3002\u5176JAK1\u6291\u5236\u6d3b\u6027\u548c\u9009\u62e9\u6027\u6bd4\u9633\u6027\u836ftofacitinib\u548cfilgotinib\u66f4\u5177\u4f18\u52bf\u3002<\/span><\/p>\n


                  <\/span><\/p>\n

                  \u5728\u8367\u5149\u7d20\u9176\u68c0\u6d4b\u4e2d\uff0c\u5b83\u53ef\u663e\u8457\u6291\u5236IL-13\u523a\u6fc0\u7684\u4eba\u7ec4\u7ec7\u7ec6\u80de\u6dcb\u5df4\u7624U-937\u7ec6\u80de\u4e2d\u7531JAK-1\u4ecb\u5bfc\u7684STAT6\u78f7\u9178\u5316\uff08IC50 = 0.034 mcM\uff09\u3002\u5728\u53e3\u670d0.5\u30012.5\u548c12.5 mg\/kg\u5242\u91cf\u4e0b\uff0c\u5b83\u589e\u52a0\u4e86\u6591\u79c3\u5c0f\u9f20\u6a21\u578bC3H\/HeJ\u7684\u6bdb\u53d1\u751f\u957f\uff1b\u57280.08\u30010.11\u30010.6\u548c4.76 mcg\/kg\u5438\u5165\u5242\u91cf\u65f6\uff0c\u80fd\u591f\u964d\u4f4e\u5c0f\u9f20\u652f\u6c14\u7ba1\u80ba\u6ce1\u704c\u6d17\u4e2d\u55dc\u9178\u6027\u7c92\u7ec6\u80de\u7684\u6c34\u5e73\uff08\u5206\u522b\u964d\u4f4e\u4e867%\u300128%\u300168%\u548c61%\uff09\u3002\uff08\u8be6\u89c1\u4e13\u5229WO 2018134213\uff09\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

                  \n
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                  \"\u3010BioWorld<\/section>\n<\/section>\n<\/section>\n
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                  \u56fe\u4e3aWO 2018134213\u4e2d\u4ee3\u8868\u5316\u5408\u7269\u7684\u7ed3\u6784<\/p>\n


                  <\/p>\n


                  <\/p>\n

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                  <\/span><\/p>\n

                  \u79d1\u777f\u552f\u5b89\u5bf9\u672c\u6587\u7684\u5168\u90e8\u5185\u5bb9\u4ee5\u53ca\u53ef\u80fd\u9644\u5e26\u7684\u5168\u90e8\u8d44\u6599\u62e5\u6709\u5168\u90e8\u77e5\u8bc6\u4ea7\u6743\uff0c\u5e76\u53d7\u6cd5\u5f8b\u4fdd\u62a4\u3002\u7f51\u7edc\u8f6c\u8f7d\u3001\u7f16\u8bd1\u53ca\u5176\u4ed6\u5546\u4e1a\u4f7f\u7528\u8bf7\u8054\u7cfb\u5e02\u573a\u90e8\uff1ayili1@Clarivate.com<\/span>
                  <\/p>\n


                  <\/span><\/p>\n

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                  Clarivate Analytics \u836f\u7269\u65b0\u95fb<\/span><\/strong><\/span><\/p>\n


                  <\/p>\n

                  \u5468\u4e00\u81f3\u5468\u4e94\u52a8\u6001\u66f4\u65b0\u7684\u836f\u7269\u65b0\u95fb\u548cEMAIL\u8ddf\u8e2a\u63d0\u9192<\/span>
                  <\/p>\n


                  <\/span><\/p>\n

                  \u25a0 <\/span> \u6bcf\u5468\u4e00\u81f3\u4e94, Clarivate Analytics\u836f\u7269\u65b0\u95fb\uff08Clarivate Analytics BioWorld Science\uff09\u7cbe\u9009\u6700\u65b0\u3001\u6700\u91cd\u8981\u7684\u836f\u7269\u7814\u53d1\u65b0\u95fb\u5728\u7ebf\u53d1\u5e03\uff0c\u5e76\u4ee5\u7b80\u660e\u627c\u8981\u7684\u683c\u5f0f\u53d1\u9001\u63d0\u9192\u90ae\u4ef6\u81f3\u60a8\u7684\u90ae\u7bb1\uff0c\u5e2e\u52a9\u60a8\u5feb\u901f\u9501\u5b9a\u91cd\u8981\u7684\u65b0\u95fb\u4e8b\u4ef6\u3002<\/span><\/p>\n

                  \u25a0<\/span>  \u60a8\u53ef\u4ee5\u5728\u7ebf\u68c0\u7d22\u6211\u4eec\u6240\u6709\u7684\u65b0\u95fb\u8d44\u6e90\uff0c\u5e76\u8bbe\u5b9a\u68c0\u7d22\u6761\u4ef6\uff08\u9650\u5b9a\u65b0\u95fb\u53d1\u751f\u7684\u65f6\u95f4\u3001\u836f\u540d\u3001\u4e13\u5229\u53f7\u3001\u516c\u53f8\u3001\u5927\u5b66\u3001\u673a\u6784\u3001\u6cbb\u7597\u7c7b\u522b\/\u5206\u7ec4\u3001\u5316\u5408\u7269\u7c7b\u578b\u3001\u4fe1\u606f\u6e90\uff09\u627e\u5230\u4e0e\u60a8\u7814\u7a76\u76f8\u5173\u7684\u5185\u5bb9\u3002\u836f\u7269\u65b0\u95fb\uff08BioWorld Science\uff09\u5185\u5bb9\u53ef\u56de\u6eaf\u81f31996\u5e74\uff0c\u5e76\u53ef\u67e5\u770b\u5316\u5b66\u7ed3\u6784\u5f0f\u3002<\/span><\/p>\n


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                  \u836f\u7269\u65b0\u95fb\uff08BioWorld Science\uff09\u63d0\u4f9b\u5982\u4e0b\u5185\u5bb9\uff1a<\/span><\/p>\n

                  \u25a0<\/span>  \u4ece\u6d77\u91cf\u4fe1\u606f\u6e90\u4e2d\u603b\u7ed3\u51fa\u7684\u6458\u8981\u62a5\u544a\u3002<\/span><\/p>\n

                  \u25a0<\/span>  \u5728\u5168\u7403\u91cd\u8981\u4f1a\u8bae\u4e2d\u62ab\u9732\u7684\u65b0\u95fb\u4fe1\u606f\u3002<\/span><\/p>\n

                  \u25a0 <\/span> \u6bcf\u5468\u66f4\u65b0\u7684\u90ae\u4ef6\u63d0\u9192\u670d\u52a1\uff0c\u4ee5\u8868\u683c\u7684\u5f62\u5f0f\u544a\u77e5\u60a8\u8fdb\u5165\u4e34\u5e8a\u524d\u5f00\u53d1\u6700\u6709\u524d\u666f\u7684\u5316\u5408\u7269\u3001lead compounds\u548c\u6700\u65b0\u7684\u4f5c\u7528\u673a\u5236\u3002<\/span><\/p>\n

                  \u25a0<\/span>  \u6bcf\u5468\u66f4\u65b0\u7684\u90ae\u4ef6\u63d0\u9192\u670d\u52a1\uff0c\u544a\u77e5\u60a8\u5728\u7814\u836f\u7269\u7814\u53d1\u72b6\u6001\u7684\u53d8\u66f4\u3002<\/span><\/p>\n


                  <\/p>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n

                  <\/span><\/p>\n


                  <\/p>\n

                  \n<\/section>\n<\/section>\n<\/section>\n<\/section>\n


                  <\/p>\n<\/p><\/div>\n","protected":false},"excerpt":{"rendered":"

                  \u4e2d\u6587\u7ffb\u8bd1\uff1a\u963f\u6817\u535a\u58eb Dailly Drug News \u5df2\u6b63\u5f0f\u66f4\u540d\u4e3aBioWorld Science \u5feb\u901f\u5bfc\u89c8 […]<\/p>\n","protected":false},"author":1,"featured_media":42633,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":[],"categories":[2],"tags":[],"_links":{"self":[{"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts\/42632"}],"collection":[{"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/comments?post=42632"}],"version-history":[{"count":1,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts\/42632\/revisions"}],"predecessor-version":[{"id":42654,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts\/42632\/revisions\/42654"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/media\/42633"}],"wp:attachment":[{"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/media?parent=42632"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/categories?post=42632"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/tags?post=42632"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}