{"id":67636,"date":"2022-04-14T07:29:00","date_gmt":"2022-04-14T00:29:00","guid":{"rendered":"https:\/\/www.xinwengao.com\/cn\/pr\/2022041407290067636"},"modified":"2022-04-14T18:35:13","modified_gmt":"2022-04-14T10:35:13","slug":"%e3%80%90aacr-2022%e3%80%91%e4%ba%9a%e7%9b%9b%e5%8c%bb%e8%8d%af%e5%85%b1%e5%85%ad%e9%a1%b9%e4%b8%b4%e5%ba%8a%e5%89%8d%e8%bf%9b%e5%b1%95%e4%ba%ae%e7%9b%b82022%e5%b9%b4%e7%be%8e%e5%9b%bd%e7%99%8c","status":"publish","type":"post","link":"https:\/\/www.xinwengao.com\/cn\/pr\/2022041407290067636","title":{"rendered":"\u3010AACR 2022\u3011\u4e9a\u76db\u533b\u836f\u5171\u516d\u9879\u4e34\u5e8a\u524d\u8fdb\u5c55\u4eae\u76f82022\u5e74\u7f8e\u56fd\u764c\u75c7\u7814\u7a76\u534f\u4f1a\u5e74\u4f1a"},"content":{"rendered":"\n\n\n
\"\"<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

\u4e2d\u56fd\u82cf\u5dde\u548c\u7f8e\u56fd\u9a6c\u91cc\u5170\u5dde\u7f57\u514b\u7ef4\u5c14\u5e02<\/span>2022\u5e744\u670814\u65e5<\/span> \/\u7f8e\u901a\u793e\/ — \u81f4\u529b\u4e8e\u5728\u80bf\u7624\u3001\u4e59\u809d\u53ca\u4e0e\u8870\u8001\u76f8\u5173\u75be\u75c5\u7b49\u6cbb\u7597\u9886\u57df\u5f00\u53d1\u521b\u65b0\u836f\u7269\u7684\u9886\u5148\u7684\u751f\u7269\u533b\u836f\u4f01\u4e1a\u2014\u2014\u4e9a\u76db\u533b\u836f\uff086855.HK\uff09\u5ba3\u5e03\uff0c\u516c\u53f8\u5728\u521a\u521a\u4e3e\u884c\u76842022\u5e74\u7f8e\u56fd\u764c\u75c7\u7814\u7a76\u534f\u4f1a\uff08AACR\uff09\u5e74\u4f1a\u4e0a\u516c\u5e03\u4e86\u516d\u9879\u6700\u65b0\u4e34\u5e8a\u524d\u7814\u7a76\u7ed3\u679c\uff0c\u5305\u62ec\u7ec6\u80de\u51cb\u4ea1\u7ba1\u7ebf\u91cd\u8981\u54c1\u79cdBcl-2\u6291\u5236\u5242lisaftoclax\uff08APG-2575\uff09\u3001MDM2-p53 \u6291\u5236\u5242alrizomadlin\uff08APG-115\uff09\uff0cFAK\u6291\u5236\u5242APG-2449\uff0cEED\u6291\u5236\u5242APG-5918\uff0cKRAS\u6291\u5236\u5242APG-1842\u4e94\u4e2a\u5728\u7814\u54c1\u79cd\u3002<\/p>\n

\n<\/p><\/div>\n

AACR\u5e74\u4f1a\u662f\u5168\u7403\u5386\u53f2\u6700\u60a0\u4e45\u3001\u89c4\u6a21\u6700\u5927\u7684\u80bf\u7624\u7814\u7a76\u5b66\u672f\u4f1a\u8bae\u4e4b\u4e00\u3002\u4f1a\u8bae\u5173\u6ce8\u9ad8\u8d28\u91cf\u80bf\u7624\u7814\u7a76\u53ca\u521b\u65b0\u7684\u5404\u4e2a\u65b9\u9762\uff0c\u662f\u5168\u7403\u80bf\u7624\u7814\u7a76\u7684\u7126\u70b9\uff0c\u5c06\u6c47\u96c6\u80bf\u7624\u9886\u57df\u7684\u6700\u524d\u6cbf\u7684\u7814\u7a76\u6210\u679c\u3002<\/p>\n

\u4e9a\u76db\u533b\u836f\u9996\u5e2d\u533b\u5b66\u5b98\u7fdf\u4e00\u5e06\u8868\u793a\uff1a"\u5728\u4eca\u5e74\u7684AACR\u5e74\u4f1a\u4e0a\uff0c\u6211\u4eec\u5c55\u793a\u4e86\u4ee5\u89e3\u51b3\u60a3\u8005\u672a\u6ee1\u8db3\u7684\u4e34\u5e8a\u9700\u6c42\u5bfc\u5411\u4e0b\u7684\u8fdb\u4e00\u6b65\u63a2\u7d22\uff0c\u4e3a\u516c\u53f8\u591a\u4e2a\u91cd\u8981\u54c1\u79cd\u4e0e\u5176\u4ed6\u9776\u70b9\u3001\u5176\u4ed6\u673a\u7406\u836f\u7269\u7684\u8054\u5408\u6cbb\u7597\u63d0\u4f9b\u4e86\u5145\u5206\u7684\u79d1\u5b66\u652f\u6301\u3002\u7279\u522b\u53ef\u5708\u53ef\u70b9\u7684\u662f\uff0c\u6211\u4eec\u7684MDM2-p53 \u6291\u5236\u5242APG-115 \u5171\u6709\u4e09\u9879\u7814\u7a76\u83b7\u5f97\u5c55\u793a\uff0c\u5728\u5448\u73b0\u591a\u79cd\u6cbb\u7597\u6f5c\u529b\u7684\u540c\u65f6\uff0c\u8fd8\u6709\u671b\u8fdb\u4e00\u6b65\u63ed\u793a\u65b0\u7684\u4f5c\u7528\u673a\u5236\uff1bEED\u6291\u5236\u5242APG-5918\u540c\u6837\u5448\u73b0\u8f83\u5927\u7684\u5f00\u53d1\u6f5c\u529b\u7b49\u3002\u6211\u4eec\u5c06\u7ee7\u7eed\u63a8\u8fdb\u76f8\u5173\u66f4\u6df1\u5165\u7684\u4e34\u5e8a\u7814\u7a76\uff0c\u65e9\u65e5\u9020\u798f\u60a3\u8005\u3002"<\/p>\n

\u4e9a\u76db\u533b\u836f\u5728\u672c\u5c4aAACR\u5e74\u4f1a\u4e0a\u5c55\u793a\u4e86\u4ee5\u4e0b\u58c1\u62a5\u4fe1\u606f\uff1a<\/p>\n

\n\n\n\n\n\n\n\n\n\n
\n

\u4ea7\u54c1<\/span><\/p>\n<\/td>\n

\n

\u58c1\u62a5\u6807\u9898<\/span><\/p>\n<\/td>\n

\n

\u7f16\u53f7<\/span><\/p>\n<\/td>\n<\/tr>\n

\n

Lisaftoclax & Alrizomadlin<\/span><\/p>\n<\/td>\n

\n

Co-targeting MDM2-p53 and BCL-2 apoptosis pathways overcomes resistance conferred by acquired BCL-2 gene mutations in preclinical models<\/span><\/p>\n<\/td>\n

\n

3964<\/span><\/p>\n<\/td>\n<\/tr>\n

\n

Alrizomadlin<\/span><\/p>\n<\/td>\n

\n

Inhibition of MDM2-p53 interaction by alrizomadlin (APG-115) induces pyroptotic cell death in gasdermin E (GSDME)-expressing cancer cells<\/span><\/p>\n<\/td>\n

\n

2998<\/span><\/p>\n<\/td>\n<\/tr>\n

\n

MDM2 inhibitor alrizomadlin (APG-115) stabilizes p53 and synergizes with proteasome inhibitors in multiple myeloma<\/span><\/p>\n<\/td>\n

\n

5439<\/span><\/p>\n<\/td>\n<\/tr>\n

\n

APG-2449<\/span><\/p>\n<\/td>\n

\n

FAK inhibitor APG-2449 and CDK4\/6 inhibitor palbociclib synergistically suppress mesothelioma tumor growth via autophagy induction<\/span><\/p>\n<\/td>\n

\n

2563<\/span><\/p>\n<\/td>\n<\/tr>\n

\n

APG-5918<\/span><\/p>\n<\/td>\n

\n

Preclinical development of embryonic ectoderm development (EED) inhibitor APG-5918\/EEDi-5273 for cancer therapy<\/span><\/p>\n<\/td>\n

\n

3939<\/span><\/p>\n<\/td>\n<\/tr>\n

\n

APG-1842<\/span><\/p>\n<\/td>\n

\n

Development of covalent KRASG12C<\/sup> inhibitor APG-1842 for the treatment of solid tumors<\/span><\/p>\n<\/td>\n

\n

2664<\/span><\/p>\n<\/td>\n<\/tr>\n<\/tbody>\n<\/table><\/div>\n

Co-targeting MDM2-p53 and BCL-2 apoptosis pathways overcomes resistance conferred by acquired BCL-2 gene mutations in preclinical models<\/b><\/p>\n

\u53cc\u91cd\u9776\u5411<\/b>MDM2-p53<\/b>\u548c<\/b>BCL-2<\/b>\u7ec6\u80de\u51cb\u4ea1\u901a\u8def\u53ef\u514b\u670d\u4e34\u5e8a\u524d\u6a21\u578b\u4e2d\u83b7\u5f97\u6027<\/b>BCL-2<\/b>\u57fa\u56e0\u7a81\u53d8\u5bfc\u81f4\u7684\u8010\u836f<\/b><\/p>\n

    \n
  • \u6458\u8981\u7f16\u53f7\uff1a3964<\/li>\n
  • \u7814\u7a76\u80cc\u666f\uff1a<\/li>\n<\/ul>\n

    BCL-2\u6291\u5236\u5242venetoclax\u5728\u6162\u6027\u6dcb\u5df4\u7ec6\u80de\u767d\u8840\u75c5\u60a3\u8005\u4e2d\u5177\u6709\u663e\u8457\u7597\u6548\uff0c\u4f46\u5b83\u7684\u4e34\u5e8a\u6548\u76ca\u53d7\u5230\u83b7\u5f97\u6027BCL-2\u57fa\u56e0\u7a81\u53d8\u5e26\u6765\u7684\u8010\u836f\u6027\u9650\u5236\u3002\u5728\u83b7\u5f97\u6027\u7a81\u53d8\u4e2d\uff0cBH3\u7ed3\u5408\u57fa\u5e8f\u90bb\u8fd1\u7684\u7a81\u53d8(\u5982G101V\u3001D103E\u548cV156D)\u5bf9BCL-2\u4e0eBH3-only\u4fc3\u6b7b\u4ea1\u86cb\u767d\u548cBH3\u6a21\u62df\u7269(\u5982venetoclax)\u7684\u7ed3\u5408\u5f71\u54cd\u6700\u5927\u3002\u56e0\u6b64\uff0c\u4e3a\u8fd9\u4e00\u5c1a\u672a\u6ee1\u8db3\u7684\u4e34\u5e8a\u9700\u6c42\u5bfb\u6c42\u65b0\u7684\u6cbb\u7597\u624b\u6bb5\u662f\u975e\u5e38\u91cd\u8981\u7684\u3002<\/p>\n

      \n
    • \u7ed3\u8bba\uff1a<\/li>\n<\/ul>\n

      \u8be5\u7814\u7a76\u8868\u660e\uff0c APG-2575\uff08lisaftoclax\uff09\u8054\u5408APG-115\uff08alrizomadlin\uff09\u53ef\u534f\u540c\u6291\u5236\u643a\u5e26BCL-2\u7a81\u53d8\u7684RS4:11\u7ec6\u80de\u7684\u589e\u6b96\u53ca\u5176\u5728\u6d3b\u4f53\u5f02\u79cd\u79fb\u690d\u7624\u6a21\u578b\u4e2d\u7684\u751f\u957f\u3002\u8054\u5408\u9776\u5411BCL-2\u548cMDM2-p53\u7ec6\u80de\u51cb\u4ea1\u901a\u8def\u4e3a\u514b\u670d\u7531BCL-2\u7a81\u53d8\u6240\u5bfc\u81f4\u7684\u83b7\u5f97\u6027\u8010\u836f\u6027\u63d0\u4f9b\u4e86\u4e00\u79cd\u6709\u6548\u7684\u5168\u65b0\u7b56\u7565\u3002 <\/p>\n

      Inhibition of MDM2-p53 interaction by alrizomadlin (APG-115) induces pyroptotic cell death in gasdermin E (GSDME)-expressing cancer cells<\/b><\/p>\n

      Alrizomadlin (APG-115) <\/b>\u5bf9\u4e8e<\/b>MDM2-p53<\/b>\u76f8\u4e92\u4f5c\u7528\u7684\u6291\u5236\u53ef\u8bf1\u5bfc<\/b>gasdermin E (GSDME) <\/b>\u9633\u6027\u764c\u7ec6\u80de\u7684\u7126\u4ea1\u6027\u7ec6\u80de\u6b7b\u4ea1<\/b><\/p>\n

        \n
      • \u6458\u8981\u7f16\u53f7\uff1a2998<\/li>\n
      • \u7814\u7a76\u80cc\u666f\uff1a<\/li>\n<\/ul>\n

        MDM2-p53\u6291\u5236\u5242APG-115\uff08alrizomadlin\uff09\u662f\u4e00\u79cd\u53ef\u8bf1\u5bfctp53<\/i>\u91ce\u751f\u578b\u764c\u7ec6\u80de\u51cb\u4ea1\u7684\u5728\u7814\u836f\u7269(Aguilar et al, J Med Chem 2017)\u3002\u66f4\u591a\u8bc1\u636e\u8868\u660e\uff0cAPG-115\u6fc0\u6d3bp53\u4e5f\u80fd\u4fc3\u8fdb\u80bf\u7624\u5fae\u73af\u5883\u4e2d\u7684\u6297\u80bf\u7624\u514d\u75ab(Fang et al, JITC 2019; Zhou et al, Nat Immunol 2021)\uff0c\u4f46\u8fd9\u4e9b\u8fc7\u7a0b\u4e4b\u95f4\u7684\u5173\u7cfb\u5c1a\u672a\u88ab\u5b8c\u5168\u4e86\u89e3\u3002\u7126\u4ea1\u6307\u7684\u662f\u708e\u6027\u7a0b\u5e8f\u6027\u7ec6\u80de\u6b7b\u4ea1\u3002\u8fd9\u4e00\u8fc7\u7a0b\u7684\u6838\u5fc3\u662fgasdermin\u5bb6\u65cf\u86cb\u767d\uff0c\u5b83\u53ef\u4ee5\u5728\u7ec6\u80de\u819c\u4e0a\u5f62\u6210\u5b54\u9699\uff0c\u5bfc\u81f4\u514d\u75ab\u523a\u6fc0\u7269\u7684\u88c2\u89e3\u548c\u91ca\u653e\u3002\u5728\u8868\u8fbe\u8fd9\u4e9b\u86cb\u767d\u7684\u7ec6\u80de\u4e2d\uff0cGSDME\u53ef\u4ee5\u88abcaspase-3\u5207\u5272\uff0c\u5c06\u975e\u708e\u6027\u7ec6\u80de\u51cb\u4ea1\u8f6c\u5316\u4e3a\u7126\u4ea1(Zhang et al .\uff0cNature 2020)\u3002\u5728\u8fd9\u79cd\u60c5\u51b5\u4e0b\uff0ccaspase-3\/GSDME\u4ee3\u8868\u4e86\u51cb\u4ea1\u548c\u7126\u4ea1\u4e4b\u95f4\u7684\u5207\u6362\u3002\u9274\u4e8e\u5927\u849c\u7d20\u4e3b\u8981\u901a\u8fc7\u6fc0\u6d3bcaspase-3\u6765\u6fc0\u53d1\u5176\u51cb\u4ea1\u6d3b\u6027\uff0c\u6211\u4eec\u5047\u8bbeMDM2-p53\u6291\u5236\u5242\u4e5f\u53ef\u80fd\u901a\u8fc7\u88c2\u89e3caspase\u6765\u8bf1\u5bfcGSDME\u9633\u6027\u764c\u7ec6\u80de\u7684\u51cb\u4ea1\u3002<\/p>\n

          \n
        • \u7ed3\u8bba\uff1a<\/li>\n<\/ul>\n

          \u8be5\u7814\u7a76\u8868\u660e\uff0c\u9664\u7ec6\u80de\u51cb\u4ea1\u5916\uff0cMDM2-p53\u6291\u5236\u5242APG-115\u8bf1\u5bfccaspase\u4ecb\u5bfc\u7684GSDME\u9633\u6027\u764c\u7ec6\u80de\u7126\u4ea1\u3002\u672c\u7814\u7a76\u9996\u6b21\u63ed\u793a\u4e86APG-115\u5728\u8868\u8fbeGSDME\u7684\u764c\u7ec6\u80de\u4e2d\u80fd\u8bf1\u5bfc\u7ec6\u80de\u51cb\u4ea1\u548c\u7126\u4ea1\u3002GSDME\u4f9d\u8d56\u6027\u7126\u4ea1\u662fAPG-115\u9664\u6297\u80bf\u7624\u514d\u75ab\u5916\u7684\u4e00\u79cd\u672a\u88ab\u8ba4\u8bc6\u7684\u4f5c\u7528\u673a\u5236\uff0c\u8fd9\u5bf9MDM2-p53\u6291\u5236\u5242\u4e34\u5e8a\u7814\u7a76\u5177\u6709\u6f5c\u5728\u7684\u91cd\u8981\u610f\u4e49\u3002<\/p>\n

          MDM2 inhibitor alrizomadlin (APG-115) stabilizes p53 and synergizes with proteasome inhibitors in multiple myeloma<\/b><\/p>\n

          MDM2<\/b>\u6291\u5236\u5242<\/b>alrizomadlin (APG-115)<\/b>\u53ef\u7a33\u5b9a\u591a\u53d1\u6027\u9aa8\u9ad3\u7624\u4e2d\u7684<\/b>p53<\/b>\u5e76\u4e0e\u86cb\u767d\u9176\u4f53\u6291\u5236\u5242\u4ea7\u751f\u534f\u540c\u4f5c\u7528<\/b><\/p>\n

            \n
          • \u6458\u8981\u7f16\u53f7\uff1a5439<\/li>\n
          • \u7814\u7a76\u80cc\u666f\uff1a<\/li>\n<\/ul>\n

            \u5728\u7f8e\u56fd\uff0c\u591a\u53d1\u6027\u9aa8\u9ad3\u7624(MM)\u7ea6\u5360\u6240\u6709\u80bf\u7624\u76842%\u548c\u6240\u6709\u8840\u6db2\u6076\u6027\u80bf\u7624\u768418%\u3002\u65b0\u5f00\u53d1\u7684\u6cbb\u7597\u65b9\u6cd5(\u5982\u514d\u75ab\u8c03\u8282\u5242\u3001\u86cb\u767d\u9176\u4f53\u6291\u5236\u5242\u3001\u5355\u514b\u9686\u6297\u4f53)\u663e\u8457\u6539\u5584\u4e86\u6cbb\u7597\u7ed3\u679c\uff0c\u4f46MM\u4e0d\u53ef\u907f\u514d\u5730\u590d\u53d1\uff0c\u88ab\u8ba4\u4e3a\u662f\u4e0d\u53ef\u6cbb\u6108\u7684\u3002\u57fa\u56e0\u7ec4\u5206\u6790\u663e\u793a\uff0cTP53\u7f16\u7801\u80bf\u7624\u6291\u5236\u86cb\u767dp53\u5728MM\u60a3\u8005\u4e2d\u5f88\u5c11\u53d1\u751f\u7a81\u53d8\uff0c\u8fd9\u4e9b\u60a3\u8005\u4e2d\u7ea6\u670982%\u4e3aTP53\u91ce\u751f\u578b\u3002MDM2\u662f\u4e00\u79cd\u53ef\u901a\u8fc7\u86cb\u767d\u9176\u4f53\u964d\u89e3\u6291\u5236p53\u7684E3\u6cdb\u7d20\u8fde\u63a5\u9176\u3002\u86cb\u767d\u9176\u4f53\u6291\u5236\u5242\u53ef\u80fd\u6709\u52a9\u4e8e\u7a33\u5b9ap53\u5e76\u4e0eMDM2\u6291\u5236\u5242\u53d1\u6325\u534f\u540c\u4f5c\u7528\u3002\u56e0\u6b64\uff0c\u53ef\u6fc0\u6d3bp53\u7684MDM2\u6291\u5236\u5242\u53ef\u80fd\u662f\u6cbb\u7597MM\u7684\u4e00\u79cd\u6709\u5438\u5f15\u529b\u7684\u836f\u7269\u3002APG-115\u662f\u4e00\u6b3e\u4f5c\u7528\u4e8ep53\/MDM2\u76f8\u4e92\u4f5c\u7528\u7684\u5728\u7814\u65b0\u578b\u5c0f\u5206\u5b50\u836f\u7269\uff0c\u76ee\u524d\u6b63\u5728\u63a5\u53d7\u7528\u4e8e\u6cbb\u7597\u5b9e\u4f53\u7624\u548c\u8840\u6db2\u80bf\u7624\u7684\u4e34\u5e8a\u5f00\u53d1\u3002\u672c\u7814\u7a76\u65e8\u5728\u8bc4\u4f30APG-115\u662f\u5426\u80fd\u589e\u5f3a\u86cb\u767d\u9176\u4f53\u6291\u5236\u5242\u5728MM\u4e2d\u7684\u6297\u80bf\u7624\u4f5c\u7528\u3002<\/p>\n

              \n
            • \u7ed3\u8bba\uff1a<\/li>\n<\/ul>\n

              \u8be5\u7814\u7a76\u8868\u660e\uff0cMDM2\u6291\u5236\u5242APG-115\u4e0e\u86cb\u767d\u9176\u4f53\u6291\u5236\u5242\u8054\u5408\u5e94\u7528\u5bf9TP53\u91ce\u751f\u578b\u7684MM\u5177\u6709\u534f\u540c\u6297\u80bf\u7624\u4f5c\u7528\uff0c\u8fd9\u4e9b\u6570\u636e\u4e3a\u5728\u96be\u6cbb\u6027MM\u60a3\u8005\u4e2d\u8fdb\u4e00\u6b65\u8bc4\u4f30\u8be5\u65b0\u578b\u836f\u7269\u7684\u4e34\u5e8a\u7814\u7a76\u63d0\u4f9b\u4e86\u8bc1\u636e\u652f\u6301\u3002<\/p>\n

              FAK inhibitor APG-2449 and CDK4\/6 inhibitor palbociclib synergistically suppress mesothelioma tumor growth via autophagy induction<\/b><\/p>\n

              FAK<\/b>\u6291\u5236\u5242<\/b>APG-2449<\/b>\u4e0e<\/b>CDK4\/6<\/b>\u6291\u5236\u5242<\/b>palbociclib<\/b>\u901a\u8fc7\u8bf1\u5bfc\u81ea\u566c\u8fbe\u5230\u5bf9\u95f4\u76ae\u7624\u751f\u957f\u7684\u534f\u540c\u6291\u5236<\/b><\/p>\n

                \n
              • \u6458\u8981\u7f16\u53f7\uff1a2563<\/li>\n
              • \u7814\u7a76\u80cc\u666f\uff1a<\/li>\n<\/ul>\n

                \u6076\u6027\u95f4\u76ae\u7624\u662f\u4e00\u79cd\u7f55\u89c1\u4e14\u9ad8\u5ea6\u81f4\u547d\u7684\u6076\u6027\u80bf\u7624\uff0c\u51765\u5e74\u751f\u5b58\u7387\u4f4e\u4e8e10%\u3002\u5176\u4e2d\u6700\u5e38\u89c1\u7684\u57fa\u56e0\u7ec4\u5f02\u5e38\u662f\u5468\u671f\u86cb\u767d\u4f9d\u8d56\u6027\u6fc0\u9176\u6291\u5236\u52422A\/B (CDKN2A\/B)\u548c\u795e\u7ecf\u7ea4\u7ef4\u86cb\u767d2 (NF2)\u7684\u53d8\u5f02\u3002\u7814\u7a76\u8868\u660e\uff0c\u7f3a\u4e4fCDKN2A\/B\u6216NF2\u8868\u8fbe\u7684\u95f4\u76ae\u7624\u7ec6\u80de\u5bf9CDK4\/6\u6216\u5c40\u7076\u6027\u9ecf\u9644\u6fc0\u9176(FAK)\u6291\u5236\u654f\u611f\u3002\u5728\u672c\u7814\u7a76\u4e2d\uff0cAPG-2449\u4f5c\u4e3a\u4e00\u79cd\u4e34\u5e8a\u9636\u6bb5\u7684FAK\/ALK\/ROS1\u591a\u6fc0\u9176\u6291\u5236\u5242\uff0c\u4e0eCDK4\/6\u6291\u5236\u5242palbociclib\u8054\u5408\u4f7f\u7528\u8868\u73b0\u51fa\u6297\u80bf\u7624\u6d3b\u6027\u3002<\/p>\n

                  \n
                • \u7ed3\u8bba\uff1a<\/li>\n<\/ul>\n

                  \u8be5\u7814\u7a76\u8868\u660e\uff0cAPG-2449\u8054\u5408palbociclib\u53ef\u901a\u8fc7\u8bf1\u5bfc\u81ea\u566c\u548c\u589e\u5f3a\u7ec6\u80de\u8870\u8001\u7684\u65b9\u5f0f\u534f\u540c\u6291\u5236\u95f4\u76ae\u7624\u7684\u80bf\u7624\u751f\u957f\u3002\u4e34\u5e8a\u524d\u7814\u7a76\u663e\u793a\uff0cAPG-2449\u8054\u5408CDK4\/6\u6291\u5236\u5242\u53ef\u80fd\u5bf9\u4e8e\u95f4\u76ae\u7624\u5177\u6709\u6cbb\u7597\u6f5c\u529b\uff0c\u4e5f\u4e3a\u76f8\u5173\u4e34\u5e8a\u8bd5\u9a8c\u7684\u8bbe\u8ba1\u63d0\u4f9b\u7406\u8bba\u4f9d\u636e\u3002<\/p>\n

                  Preclinical development of embryonic ectoderm development (EED) inhibitor APG-5918\/EEDi-5273 for cancer therapy<\/b><\/p>\n

                  \u6297\u80bf\u7624\u836f\u7269<\/b>EED<\/b>\u6291\u5236\u5242<\/b>APG-5918\/EEDi-5273<\/b>\u7684\u4e34\u5e8a\u524d\u7814\u7a76<\/b><\/p>\n

                    \n
                  • \u6458\u8981\u7f16\u53f7\uff1a3939<\/li>\n
                  • \u7814\u7a76\u80cc\u666f\uff1a<\/li>\n<\/ul>\n

                    PRC2\u662f\u4e00\u79cd\u591a\u86cb\u767d\u590d\u5408\u7269\uff0c\u53ef\u50ac\u5316\u7ec4\u86cb\u767dH3\u5728\u8d56\u6c28\u917827\u4f4d\u70b9\u7684\u7532\u57fa\u5316(H3K27me3)\u3002\u8be5\u590d\u5408\u7269\u7531Zeste\u57fa\u56e0\u589e\u5f3a\u5b50\u4eba\u7c7b\u540c\u6e90\u72692 (EZH2)\u3001\u80da\u80ce\u5916\u80da\u5c42\u53d1\u80b2\u86cb\u767d(EED)\u548cZeste 12\u540c\u6e90\u72691\u6291\u5236\u56e0\u5b502 (SUZ12)\u7b49\u6838\u5fc3\u4e9a\u5355\u4f4d\u7ec4\u6210\u3002PRC2\u7684\u529f\u80fd\u5931\u8c03\u4e0e\u591a\u79cd\u764c\u75c7\u7684\u51fa\u73b0\u6709\u5173\u3002\u4f7f\u7528EZH2\u6291\u5236\u5242\u4ed6\u6cfd\u53f8\u4ed6\u6291\u5236PRC2\u529f\u80fd\u5df2\u88ab\u8bc1\u660e\u662f\u4e00\u79cd\u6210\u529f\u7684\u764c\u75c7\u6cbb\u7597\u7b56\u7565\u3002\u5c3d\u7ba1\u5982\u6b64\uff0cEZH2\u7684\u4e8c\u6b21\u7a81\u53d8\u53ef\u4ea7\u751f\u83b7\u5f97\u6027\u8010\u836f\uff0c\u4e14\u5176\u540c\u6e90\u7269EZH1\u4e5f\u5177\u6709\u7532\u57fa\u8f6c\u79fb\u9176\u6d3b\u6027\uff0c\u4ee5\u4e0a\u539f\u56e0\u4e00\u5b9a\u7a0b\u5ea6\u4e0a\u5bfc\u81f4EZH2\u6291\u5236\u5242\u6d3b\u6027\u53d7\u9650\u3002\u7531\u4e8eEED\u4e0eH3K27me3\u7ed3\u5408\u662f\u6fc0\u6d3bEZH2\u7532\u57fa\u8f6c\u79fb\u9176\u6d3b\u6027\u7684\u5148\u51b3\u6761\u4ef6\uff0c\u53d8\u6784\u9776\u5411EED\u662f\u6291\u5236PRC2\u7684\u4e00\u79cd\u65b0\u65b9\u6cd5\u3002\u5df2\u6709\u7814\u7a76\u53d1\u6587\u62a5\u9053\uff0cAPG-5918\/EEDi-5273\u662f\u4e00\u79cd\u65b0\u578b\u7684\u3001\u5177\u6709\u751f\u7269\u6d3b\u6027\u7684\u3001\u5f3a\u6548\u7684EED\u6291\u5236\u5242\u3002\u5728\u672c\u7814\u7a76\u4e2d\uff0c\u6211\u4eec\u5bf9APG-5918\u8fd9\u4e00\u6f5c\u5728\u7684\u80bf\u7624\u6cbb\u7597\u836f\u7269\u8fdb\u884c\u4e86\u8fdb\u4e00\u6b65\u4e34\u5e8a\u524d\u7814\u7a76\u3002<\/p>\n