{"id":1099,"date":"2021-10-31T21:29:34","date_gmt":"2021-10-31T13:29:34","guid":{"rendered":"https:\/\/www.huanglab.org.cn\/wordpress\/?p=1099"},"modified":"2021-11-01T16:40:16","modified_gmt":"2021-11-01T08:40:16","slug":"%e5%9f%ba%e4%ba%8epde3a-slfn12%e5%a4%8d%e5%90%88%e7%89%a9%e7%bb%93%e6%9e%84%e7%9a%84%e8%82%bf%e7%98%a4%e7%bb%86%e8%83%9e%e5%87%8b%e4%ba%a1%e8%af%b1%e5%af%bc%e5%89%82%e7%9a%84%e8%ae%be%e8%ae%a1","status":"publish","type":"post","link":"https:\/\/www.huanglab.org.cn\/wordpress\/?p=1099","title":{"rendered":"\u57fa\u4e8ePDE3A-SLFN12\u590d\u5408\u7269\u7ed3\u6784\u7684\u80bf\u7624\u7ec6\u80de\u51cb\u4ea1\u8bf1\u5bfc\u5242\u7684\u8bbe\u8ba1"},"content":{"rendered":"<p><a href=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2021\/10\/NC_news_pic.png\"><img loading=\"lazy\" class=\"alignnone size-medium wp-image-1106\" src=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2021\/10\/NC_news_pic-300x140.png\" alt=\"\" width=\"300\" height=\"140\" srcset=\"https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2021\/10\/NC_news_pic-300x140.png 300w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2021\/10\/NC_news_pic-1024x479.png 1024w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2021\/10\/NC_news_pic-768x359.png 768w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2021\/10\/NC_news_pic-1536x718.png 1536w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2021\/10\/NC_news_pic-2048x957.png 2048w\" sizes=\"(max-width: 300px) 100vw, 300px\" \/><\/a><\/p>\n<p>\u8fd1\u5e74\u6765\uff0cde Waal\u3001\u738b\u6653\u4e1c\u56e2\u961f\u3001\u5b89\u7136\u7b49\u4eba\u76f8\u7ee7\u53d1\u73b0\u5c0f\u5206\u5b50DNMDP\u3001\u9ad8\u6d53\u5ea6\u96cc\u4e8c\u9187\u3001\u5929\u7136\u4ea7\u7269nauclefine\u3001PDE3\u6291\u5236\u5242anagrelide\u53ef\u4ee5\u4fc3\u8fdbPDE3A\uff08phosphodiesterase 3A\uff09\u548cSLFN12\uff08Schlafen family member 12\uff09\u4f9d\u8d56\u7684\u7ec6\u80de\u51cb\u4ea1\u3002\u968f\u540e\uff0c\u6e05\u534e\u5927\u5b66\u738b\u5b8f\u4f1f\u56e2\u961f\u89e3\u6790\u4e86\u5c0f\u5206\u5b50\u5316\u5408\u7269DNMDP\uff0cnauclefine\uff0canagrelide\u7ed3\u5408\u7684PDE3A-SLFN12\u590d\u5408\u7269\u7ed3\u6784\u3002\u5176\u4e2d\u7684PDE3A-SLFN12-anagrelide\u590d\u5408\u7269\u7ed3\u6784\u663e\u793a\uff0c\u7ed3\u5408\u4e8ePDE3A\u50ac\u5316\u53e3\u888b\u7684\u5c0f\u5206\u5b50\u5316\u5408\u7269anagrelide\u4f5c\u4e3a\u5206\u5b50\u80f6\u6c34\uff0c\u201c\u521b\u9020\u201d\u4e86PDE3A\u7684\u758f\u6c34\u754c\u9762\uff0c\u4ece\u800c\u4e0eSLFN12\u7684\u77ed\u87ba\u65cb\uff08E552-I558\uff09\u7ed3\u5408\uff0c\u5c06\u4e24\u79cd\u86cb\u767d\u8d28\u201c\u7c98\u5408\u201d\u5728\u4e00\u8d77\uff0c\u8bf1\u5bfc\u4e86PDE3A\u548cSLFN12\u5f62\u6210\u7a33\u5b9a\u7684\u4e09\u5143\u590d\u5408\u7269\u3002<\/p>\n<p>\u901a\u8fc7\u6df1\u5165\u5206\u6790PDE3A-SLFN12-anagrelide\u7684\u4e09\u5143\u590d\u5408\u7269\uff0c\u9ec4\u725b\u56e2\u961f\u6ce8\u610f\u5230anagrelide\u76847\u4f4d\u6c2f\u539f\u5b50\u4e0ePDE3A\u7684T844\u3001F972\u3001L910\u7b49\u6b8b\u57fa\u548cSLFN12\u7684I557\u3001I558\u7b49\u6b8b\u57fa\u5f62\u6210\u5e7f\u6cdb\u7684\u758f\u6c34\u76f8\u4e92\u4f5c\u7528\uff08Fig. A\uff09\u3002\u56e0\u6b64\u63a8\u6d4b\uff0c7\u4f4d\u6c2f\u539f\u5b50\u5bf9anagrelide\u5206\u5b50\u80f6\u7684\u4f5c\u7528\u6709\u91cd\u8981\u8d21\u732e\uff0c\u5bf9anagrelide\u51cb\u4ea1\u8bf1\u5bfc\u6d3b\u6027\u4e5f\u81f3\u5173\u91cd\u8981\u3002\u57fa\u4e8ePDE3A-SLFN12-anagrelide\u7684\u4e09\u5143\u590d\u5408\u7269\u7ed3\u6784\u548canagrelide 7\u4f4d\u6c2f\u539f\u5b50\u7684\u8ba4\u77e5\uff0c\u9ec4\u725b\u56e2\u961f\u4f7f\u7528OpenGrowth\u7a0b\u5e8f\u81ea\u52a8\u5bf9anagrelide 7\u4f4d\u7684\u53d6\u4ee3\u57fa\u8fdb\u884c\u91c7\u6837\uff0c\u671f\u671b\u83b7\u5f97\u65b0\u578b\u7684\u53d6\u4ee3\u57fa\u80fd\u4fc3\u8fdbPDE3A\u548cSLFN12\u4e4b\u95f4\u7684\u76f8\u4e92\u4f5c\u7528\uff0c\u8fdb\u800c\u63d0\u9ad8\u5c0f\u5206\u5b50\u5316\u5408\u7269\u7684\u51cb\u4ea1\u8bf1\u5bfc\u6d3b\u6027\u3002\u968f\u540e\u4f7f\u7528MM-GB\/SA\u81ea\u7531\u80fd\u8ba1\u7b97\u5bf9\u751f\u6210\u7684anagrelide\u7c7b\u4f3c\u7269\u8fdb\u884c\u4eb2\u548c\u529b\u6392\u540d\u3002\u5176\u4e2d\u6392\u540d\u9760\u524d\u7684\u4ee57\u4f4d\u53d6\u4ee3\u57fa\u4e3a\u82b3\u73af\uff0c\u5c24\u5176\u662f\u82ef\u73af\u6216\u8005\u53d6\u4ee3\u82ef\u73af\u4e3a\u4e3b\u3002\u540c\u65f6\uff0c\u57fa\u4e8e\u5bf9\u7ed3\u5408\u6a21\u5f0f\u7684\u7406\u89e3\uff0c\u56e2\u961f\u6210\u5458\u6311\u9009\u4e86\u4e00\u6279\u758f\u6c34\u6027\u7684\u53d6\u4ee3\u57fa\uff08\u5305\u62ec\u82ef\u57fa\uff09\u4f5c\u4e3a\u4f18\u9009\u5206\u5b50\u3002\u8be5\u8ba1\u7b97\u6d41\u7a0b\u5341\u5206\u9ad8\u6548\uff0c\u4e00\u5171\u751f\u6210\u3001\u8bc4\u4ef7\u4e86200\u4e2aanagrelide 7\u4f4d\u53d6\u4ee3\u57fa\u7684\u5206\u5b50\uff0c\u5355\u683810\u5c0f\u65f6\u5185\u5373\u53ef\u5b8c\u6210\uff08Fig. B\uff09\u3002<\/p>\n<p>\u968f\u540e\uff0c\u9f50\u6e58\u5175\u56e2\u961f\u53c2\u8003\u8ba1\u7b97\u56e2\u961f\u7684\u7ed3\u679c\uff0c\u5408\u6210\u4e86anagrelide 7 \u4f4d\u5177\u6709\u4e0d\u540c\u758f\u6c34\u6027\u53d6\u4ee3\u7684anagrelide\u7c7b\u4f3c\u7269\uff0c\u5305\u62ec\u82b3\u73af\u6216\u8102\u80aa\u94fe\u3002\u4ee4\u4eba\u9f13\u821e\u7684\u662f\uff0c\u82ef\u73af\u53d6\u4ee3\u7684A4\u8868\u73b0\u51fa\u4f18\u5f02\u7684\u51cb\u4ea1\u8bf1\u5bfc\u6d3b\u6027\uff0cIC50\u8fbe\u52300.56 nM\uff0c\u4e0eanagrelide\u76f8\u6bd4\uff0c\u6d3b\u6027\u63d0\u9ad8\u4e86\u8fd112\u500d\uff0c\u7532\u82ef\u57fa\u53d6\u4ee3\u7684\u7c7b\u4f3c\u7269\uff08A6\uff09\u53d6\u5f97\u4e86\u6700\u6709\u6548\u7684\u51cb\u4ea1\u8bf1\u5bfc\u6d3b\u6027\uff08IC50 = 0.30 nM\uff09\uff0c\u6bd4anagrelide\u63d0\u9ad8\u7ea622\u500d\uff08Fig. C\uff09\u3002\u66f4\u91cd\u8981\u7684\u662f\uff0c\u5316\u5408\u7269A6\u5728\u4f53\u5185\u663e\u793a\u51fa\u6bd4anagrelide\u66f4\u597d\u7684\u80bf\u7624\u751f\u957f\u6291\u5236\u4f5c\u7528\u3002<\/p>\n<p>\u8be5\u5de5\u4f5c\u7531\u738b\u6653\u4e1c\u56e2\u961f\u8054\u5408\u738b\u5b8f\u4f1f\u56e2\u961f\u3001\u9ec4\u725b\u56e2\u961f\u548c\u9f50\u6e58\u5175\u56e2\u961f\u5171\u540c\u5b8c\u6210\u3002\u9ec4\u725b\u56e2\u961f\u7684\u738b\u5143\u52cb\u535a\u58eb\u5b8c\u6210\u4e86\u8ba1\u7b97\u548c\u5206\u5b50\u8bbe\u8ba1\u7684\u5de5\u4f5c\u3002\u8bba\u6587\u53d1\u8868\u4e8eNature Communications\u6742\u5fd7\u4e0a\u9898\u4e3a<\/p>\n<p>&nbsp;<\/p>\n<p><a href=\"https:\/\/www.nature.com\/articles\/s41467-021-26546-8.pdf\">Structure of PDE3A\u2013SLFN12 Complex and Structure-based Design for A Potent Apoptosis Inducer of Tumor Cells<\/a><\/p>\n<p>Jie Chen, Nan Liu, Yinpin Huang, Yuanxun Wang, Yuxing Sun, Qingcui Wu, Dianrong Li, Shuanhu Gao, Hong-Wei Wang, Niu Huang, Xiangbing Qi &amp; Xiaodong Wang<\/p>\n","protected":false},"excerpt":{"rendered":"<p>\u8fd1\u5e74\u6765\uff0cde Waal\u3001\u738b\u6653\u4e1c\u56e2\u961f\u3001\u5b89\u7136\u7b49\u4eba\u76f8\u7ee7\u53d1\u73b0\u5c0f\u5206\u5b50DNMDP\u3001\u9ad8\u6d53\u5ea6\u96cc\u4e8c\u9187\u3001\u5929\u7136\u4ea7\u7269nauclefine\u3001PDE3\u6291\u5236\u5242anagrelide\u53ef\u4ee5\u4fc3\u8fdbPDE3A\uff08phosphodiesterase 3A\uff09\u548cSLFN12\uff08Schlafen family member 12\uff09\u4f9d\u8d56\u7684\u7ec6\u80de\u51cb\u4ea1\u3002\u968f\u540e\uff0c\u6e05\u534e\u5927\u5b66\u738b\u5b8f\u4f1f\u56e2\u961f\u89e3\u6790\u4e86\u5c0f\u5206\u5b50\u5316\u5408\u7269DNMDP\uff0cnauclefine\uff0canagrelide\u7ed3\u5408\u7684PDE3A-SLFN12\u590d\u5408\u7269\u7ed3\u6784\u3002\u5176\u4e2d\u7684PDE3A-SLFN12-anagrelide\u590d\u5408\u7269\u7ed3\u6784\u663e\u793a\uff0c\u7ed3\u5408\u4e8ePDE3A\u50ac\u5316\u53e3\u888b\u7684\u5c0f\u5206\u5b50\u5316\u5408\u7269anagrelide\u4f5c\u4e3a\u5206\u5b50\u80f6\u6c34\uff0c\u201c\u521b\u9020\u201d\u4e86PDE3A\u7684\u758f\u6c34\u754c\u9762\uff0c\u4ece\u800c\u4e0eSLFN12\u7684\u77ed\u87ba\u65cb\uff08E552-I558\uff09\u7ed3\u5408\uff0c\u5c06\u4e24\u79cd\u86cb\u767d\u8d28\u201c\u7c98\u5408\u201d\u5728\u4e00\u8d77\uff0c\u8bf1\u5bfc\u4e86PDE3A\u548cSLFN12\u5f62\u6210\u7a33\u5b9a\u7684\u4e09\u5143\u590d\u5408\u7269\u3002 \u901a\u8fc7\u6df1\u5165\u5206\u6790PDE3A-SLFN12-anagrelide\u7684\u4e09\u5143\u590d\u5408\u7269\uff0c\u9ec4\u725b\u56e2\u961f\u6ce8\u610f\u5230anagrelide\u76847\u4f4d\u6c2f\u539f\u5b50\u4e0ePDE3A\u7684T844\u3001F972\u3001L910\u7b49\u6b8b\u57fa\u548cSLFN12\u7684I557\u3001I558\u7b49\u6b8b\u57fa\u5f62\u6210\u5e7f\u6cdb\u7684\u758f\u6c34\u76f8\u4e92\u4f5c\u7528\uff08Fig. A\uff09\u3002\u56e0\u6b64\u63a8\u6d4b\uff0c7\u4f4d\u6c2f\u539f\u5b50\u5bf9anagrelide\u5206\u5b50\u80f6\u7684\u4f5c\u7528\u6709\u91cd\u8981\u8d21\u732e\uff0c\u5bf9anagrelide\u51cb\u4ea1\u8bf1\u5bfc\u6d3b\u6027\u4e5f\u81f3\u5173\u91cd\u8981\u3002\u57fa\u4e8ePDE3A-SLFN12-anagrelide\u7684\u4e09\u5143\u590d\u5408\u7269\u7ed3\u6784\u548canagrelide 7\u4f4d\u6c2f\u539f\u5b50\u7684\u8ba4\u77e5\uff0c\u9ec4\u725b\u56e2\u961f\u4f7f\u7528OpenGrowth\u7a0b\u5e8f\u81ea\u52a8\u5bf9anagrelide 7\u4f4d\u7684\u53d6\u4ee3\u57fa\u8fdb\u884c\u91c7\u6837\uff0c\u671f\u671b\u83b7\u5f97\u65b0\u578b\u7684\u53d6\u4ee3\u57fa\u80fd\u4fc3\u8fdbPDE3A\u548cSLFN12\u4e4b\u95f4\u7684\u76f8\u4e92\u4f5c\u7528\uff0c\u8fdb\u800c\u63d0\u9ad8\u5c0f\u5206\u5b50\u5316\u5408\u7269\u7684\u51cb\u4ea1\u8bf1\u5bfc\u6d3b\u6027\u3002\u968f\u540e\u4f7f\u7528MM-GB\/SA\u81ea\u7531\u80fd\u8ba1\u7b97\u5bf9\u751f\u6210\u7684anagrelide\u7c7b\u4f3c\u7269\u8fdb\u884c\u4eb2\u548c\u529b\u6392\u540d\u3002\u5176\u4e2d\u6392\u540d\u9760\u524d\u7684\u4ee57\u4f4d\u53d6\u4ee3\u57fa\u4e3a\u82b3\u73af\uff0c\u5c24\u5176\u662f\u82ef\u73af\u6216\u8005\u53d6\u4ee3\u82ef\u73af\u4e3a\u4e3b\u3002\u540c\u65f6\uff0c\u57fa\u4e8e\u5bf9\u7ed3\u5408\u6a21\u5f0f\u7684\u7406\u89e3\uff0c\u56e2\u961f\u6210\u5458\u6311\u9009\u4e86\u4e00\u6279\u758f\u6c34\u6027\u7684\u53d6\u4ee3\u57fa\uff08\u5305\u62ec\u82ef\u57fa\uff09\u4f5c\u4e3a\u4f18\u9009\u5206\u5b50\u3002\u8be5\u8ba1\u7b97\u6d41\u7a0b\u5341\u5206\u9ad8\u6548\uff0c\u4e00\u5171\u751f\u6210\u3001\u8bc4\u4ef7\u4e86200\u4e2aanagrelide 7\u4f4d\u53d6\u4ee3\u57fa\u7684\u5206\u5b50\uff0c\u5355\u683810\u5c0f\u65f6\u5185\u5373\u53ef\u5b8c\u6210\uff08Fig. B\uff09\u3002 \u968f\u540e\uff0c\u9f50\u6e58\u5175\u56e2\u961f\u53c2\u8003\u8ba1\u7b97\u56e2\u961f\u7684\u7ed3\u679c\uff0c\u5408\u6210\u4e86anagrelide 7 \u4f4d\u5177\u6709\u4e0d\u540c\u758f\u6c34\u6027\u53d6\u4ee3\u7684anagrelide\u7c7b\u4f3c\u7269\uff0c\u5305\u62ec\u82b3\u73af\u6216\u8102\u80aa\u94fe\u3002\u4ee4\u4eba\u9f13\u821e\u7684\u662f\uff0c\u82ef\u73af\u53d6\u4ee3\u7684A4\u8868\u73b0\u51fa\u4f18\u5f02\u7684\u51cb\u4ea1\u8bf1\u5bfc\u6d3b\u6027\uff0cIC50\u8fbe\u52300.56 nM\uff0c\u4e0eanagrelide\u76f8\u6bd4\uff0c\u6d3b\u6027\u63d0\u9ad8\u4e86\u8fd112\u500d\uff0c\u7532\u82ef\u57fa\u53d6\u4ee3\u7684\u7c7b\u4f3c\u7269\uff08A6\uff09\u53d6\u5f97\u4e86\u6700\u6709\u6548\u7684\u51cb\u4ea1\u8bf1\u5bfc\u6d3b\u6027\uff08IC50 = 0.30 nM\uff09\uff0c\u6bd4anagrelide\u63d0\u9ad8\u7ea622\u500d\uff08Fig. C\uff09\u3002\u66f4\u91cd\u8981\u7684\u662f\uff0c\u5316\u5408\u7269A6\u5728\u4f53\u5185\u663e\u793a\u51fa\u6bd4anagrelide\u66f4\u597d\u7684\u80bf\u7624\u751f\u957f\u6291\u5236\u4f5c\u7528\u3002 \u8be5\u5de5\u4f5c\u7531\u738b\u6653\u4e1c\u56e2\u961f\u8054\u5408\u738b\u5b8f\u4f1f\u56e2\u961f\u3001\u9ec4\u725b\u56e2\u961f\u548c\u9f50\u6e58\u5175\u56e2\u961f\u5171\u540c\u5b8c\u6210\u3002\u9ec4\u725b\u56e2\u961f\u7684\u738b\u5143\u52cb\u535a\u58eb\u5b8c\u6210\u4e86\u8ba1\u7b97\u548c\u5206\u5b50\u8bbe\u8ba1\u7684\u5de5\u4f5c\u3002\u8bba\u6587\u53d1\u8868\u4e8eNature Communications\u6742\u5fd7\u4e0a\u9898\u4e3a &nbsp; Structure of PDE3A\u2013SLFN12 Complex and Structure-based Design for A Potent Apoptosis Inducer of Tumor Cells Jie Chen, Nan Liu, Yinpin Huang, Yuanxun Wang, Yuxing Sun, Qingcui Wu, Dianrong Li, Shuanhu Gao, Hong-Wei 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