{"id":1288,"date":"2024-01-26T12:27:54","date_gmt":"2024-01-26T04:27:54","guid":{"rendered":"https:\/\/www.huanglab.org.cn\/wordpress\/?p=1288"},"modified":"2024-01-26T12:47:19","modified_gmt":"2024-01-26T04:47:19","slug":"%e4%b8%87%e7%89%a9%e7%9a%86%e5%8f%afdock%ef%bc%9a%e5%85%ab%e9%9d%a2%e9%92%8c%e7%ac%bc%e6%8b%93%e5%b1%95%e8%8d%af%e7%89%a9%e5%8c%96%e5%ad%a6%e6%96%b0%e7%a9%ba%e9%97%b4","status":"publish","type":"post","link":"https:\/\/www.huanglab.org.cn\/wordpress\/?p=1288","title":{"rendered":"\u4e07\u7269\u7686\u53efDock\uff1a\u516b\u9762\u948c\u7b3c\u62d3\u5c55\u836f\u7269\u5316\u5b66\u65b0\u7a7a\u95f4"},"content":{"rendered":"\n<div class=\"wp-block-image\"><figure class=\"aligncenter size-large is-resized\"><a href=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/wangqing2024.jpg\"><img loading=\"lazy\" src=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/wangqing2024-768x1024.jpg\" alt=\"\" class=\"wp-image-1280\" width=\"330\" height=\"440\" srcset=\"https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/wangqing2024-768x1024.jpg 768w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/wangqing2024-225x300.jpg 225w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/wangqing2024-1152x1536.jpg 1152w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/wangqing2024-1536x2048.jpg 1536w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/wangqing2024.jpg 1600w\" sizes=\"(max-width: 330px) 100vw, 330px\" \/><\/a><figcaption>\u672c\u6587\u7684\u7b2c\u4e00\u4f5c\u8005\uff0c\u738b\u60c5 \u535a\u58eb<\/figcaption><\/figure><\/div>\n\n\n\n<p><strong>\u82f1\u6587\u539f\u9898\uff1a<\/strong>Structure-based Identification of Organoruthenium Compounds as Nanomolar Antagonists of Cannabinoid Receptors<\/p>\n\n\n\n<div class=\"wp-block-image\"><figure class=\"aligncenter size-full is-resized\"><a href=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f0.png\"><img loading=\"lazy\" src=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f0.png\" alt=\"\" class=\"wp-image-1290\" width=\"-96\" height=\"-51\" srcset=\"https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f0.png 715w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f0-300x162.png 300w\" sizes=\"(max-width: 715px) 100vw, 715px\" \/><\/a><\/figure><\/div>\n\n\n\n<p><strong>\u901a\u8baf\u4f5c\u8005\uff1a<\/strong>Jianhui Huang, Niu Huang<\/p>\n\n\n\n<p><strong>\u4f5c\u8005\uff1a<\/strong>Qing Wang, Xuegang Fu, Yuting Yan, Tao Liu, Yuting Xie, Xiaoqing Song, Yu Zhou, Min Xu, Ping Wang, Peng Fu<\/p>\n\n\n\n<p><strong>\u80cc\u666f\u4ecb\u7ecd<\/strong><\/p>\n\n\n\n<p>\u65b0\u836f\u7814\u53d1\u7684\u5931\u8d25\u7387\u5c45\u9ad8\u4e0d\u4e0b\uff0c\u5e02\u573a\u7ade\u4e89\u5f02\u5e38\u6fc0\u70c8\uff0c\u9776\u6807\u67af\u7aed\u662f\u91cd\u8981\u539f\u56e0\u3002\u6269\u5145\u836f\u7269\u65b0\u9776\u6807\uff0c\u4e00\u65b9\u9762\u9700\u8981\u66f4\u6df1\u5165\u7684\u751f\u7269\u5b66\u7814\u7a76\uff0c\u53e6\u4e00\u65b9\u9762\u5219\u9700\u8981\u66f4\u5e7f\u9614\u7684\u5316\u5b66\u7a7a\u95f4\u3002\u76ee\u524d\u9ad8\u901a\u91cf\u7ec4\u5408\u5316\u5b66\u548cDNA\u7f16\u7801\u5316\u5408\u7269\u5e93\u7b49\u65b0\u6280\u672f\u5728\u52aa\u529b\u62d3\u5c55\u5c0f\u5206\u5b50\u5316\u5408\u7269\u5e93\uff0c\u4f46\u4e3b\u8981\u8fd8\u662f\u5c40\u9650\u5728C\u3001H\u3001O\u3001N\u3001P\u3001S\u3001F\u3001Cl\u548cBr\u7b49\u5e38\u89c1\u7684\u5316\u5b66\u5143\u7d20\u4e2d\u3002\u4f46\u7eb5\u89c2\u5143\u7d20\u5468\u671f\u8868\uff0c70%\u4ee5\u4e0a\u662f\u91d1\u5c5e\u5143\u7d20\uff0c\u53ef\u91d1\u5c5e\u836f\u7269\u5374\u8fdc\u4e0d\u53ca\u4f20\u7edf\u7684\u6709\u673a\u836f\u7269\u666e\u904d\u3002\u662f\u91d1\u5c5e\u5143\u7d20\u4e0d\u80fd\u6210\u836f\u5417\uff1f\u4e0d\u662f\u7684\uff0c\u6bd4\u5982\u5927\u5bb6\u719f\u77e5\u7684\u94c2\u7c7b\u836f\u7269\uff0c\u81ea\u7f8e\u56fd\u751f\u7269\u7269\u7406\u5b66\u6559\u6388Rosenberg\u610f\u5916\u53d1\u73b0\u5176\u5177\u6709\u6291\u5236\u7ec6\u83cc\u5206\u88c2\u80fd\u529b\uff0c\u4f5c\u4e3a\u6297\u764c\u5316\u7597\u836f\u7269\u5728\u4e34\u5e8a\u4e0a\u5e94\u7528\u4ee5\u6765\uff0c\u81f3\u4eca\u4ecd\u662f\u591a\u79cd\u764c\u75c7\u6cbb\u7597\u7684\u4e00\u7ebf\u836f\u7269\uff0c\u662fTKi\u6216\u8005PD-1\u6297\u4f53\u7b49\u603b\u60f3\u903e\u8d8a\u7684\u9ad8\u5c71\u3002\u53e6\u5916\uff0c\u548c\u4f20\u7edf\u5c0f\u5206\u5b50\u836f\u7269\u4e0e\u9776\u6807\u4f5c\u7528\u65b9\u5f0f\u76f8\u6bd4\uff0c\u91d1\u5c5e\u836f\u7269\u4e0e\u9776\u6807\u7684\u4f5c\u7528\u65b9\u5f0f\u53ef\u80fd\u5e26\u6765\u65b0\u7684\u836f\u7269\u8bbe\u8ba1\u65b0\u89c6\u89d2\u3002\u6bd4\u5982\u5728\u751f\u7269\u4f53\u5185\uff0c\u987a\u94c2\u6613\u53d1\u751f\u914d\u4f53\u4ea4\u6362\uff0c\u901a\u8fc7\u4e0eDNA\u78b1\u57fa\u914d\u4f4d\u53d1\u6325\u6291\u5236\u80bf\u7624\u7ec6\u80deDNA\u590d\u5236\u7684\u4f5c\u7528\u3002\u800c\u4e14\uff0c\u5728\u4e09\u7ef4\u7acb\u4f53\u7a7a\u95f4\u4e0a\uff0c\u4f5c\u4e3a\u6709\u673a\u5316\u5408\u7269\u4e2d\u5fc3\u7684\u78b3\u539f\u5b50\uff0c\u53ea\u80fd\u91c7\u53d6\u7ebf\u6027\uff08sp\uff09\u3001\u5e73\u9762\uff08sp2\uff09\u548c\u56db\u9762\u4f53\uff08sp3\uff09\u7684\u51e0\u4f55\u6784\u578b\u3002\u76f8\u6bd4\u4e4b\u4e0b\uff0c\u91d1\u5c5e\u539f\u5b50\u7684\u51e0\u4f55\u7ed3\u6784\u66f4\u52a0\u591a\u6837\uff0c\u53ef\u4ee5\u91c7\u53d6\u516b\u9762\u4f53\u751a\u81f3\u662f\u66f4\u590d\u6742\u7684\u51e0\u4f55\u6784\u578b\u3002\u5229\u7528\u6709\u673a\u948c\u5316\u5408\u7269\u7684\u7a7a\u95f4\u7acb\u4f53\u590d\u6742\u6027\uff0cMeggers\u7b49\u4eba\u8bbe\u8ba1\u4e86\u4e00\u7cfb\u5217\u9ad8\u6d3b\u6027\u4e14\u5177\u6709\u9ad8\u9009\u62e9\u6027\u7684\u6fc0\u9176\u6291\u5236\u5242\u3002\u8fd9\u4e0e\u987a\u94c2\u7684\u914d\u4f53\u4ea4\u6362\u673a\u5236\u4e0d\u540c\uff0c\u948c\u539f\u5b50\u8d77\u5230\u4e86\u7c7b\u4f3c\u4e8e&#8221;\u516b\u9762\u4f53\u78b3&#8221;\u7684\u4f5c\u7528\uff0c\u901a\u8fc7\u4e0e\u4e0d\u540c\u7684\u914d\u4f53\u87af\u5408\u5f62\u6210\u9002\u5e94\u7279\u5b9a\u6fc0\u9176\u7ed3\u5408\u53e3\u888b\u7684\u72ec\u7279\u5f62\u72b6\uff0c\u800c\u975e\u76f4\u63a5\u4e0e\u9776\u6807\u5206\u5b50\u4f5c\u7528\u3002\u53d7\u91d1\u5c5e\u914d\u5408\u7269\u7acb\u4f53\u7ed3\u6784\u590d\u6742\u6027\u7684\u542f\u53d1\uff0c\u8be5\u7814\u7a76\u5229\u7528\u516b\u9762\u4f53\u6709\u673a\u948c\u5316\u5408\u7269\uff0c\u901a\u8fc7\u53cd\u5411\u5206\u5b50\u5bf9\u63a5\u7b49\u8ba1\u7b97\u65b9\u6cd5\uff0c\u4ee5\u8fdc\u4f4e\u4e8e\u9ad8\u901a\u91cf\u7ec4\u5408\u5316\u5b66\u548cDNA\u7f16\u7801\u5316\u5408\u7269\u5e93\u7684\u6210\u672c\u5c31\u53ef\u4ee5\u53bb\u63a2\u7d22\u5206\u5b50\u8bbe\u8ba1\u4e2d\u5148\u524d\u96be\u4ee5\u89e6\u53ca\u7684\u5316\u5b66\u7a7a\u95f4\uff0c\u4ece\u800c\u4e3a\u63a2\u7d22\u65b0\u9776\u6807\u63d0\u4f9b\u66f4\u591a\u53ef\u80fd\u6027\u3002<\/p>\n\n\n\n<p><strong>\u6587\u7ae0\u4eae\u70b9<\/strong><\/p>\n\n\n\n<p>1. 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type=\"1\"><li>\u53cd\u5411\u5bf9\u63a5\u627e\u5bfb\u6f5c\u5728\u7ed3\u5408\u9776\u6807<\/li><\/ol>\n\n\n\n<p>\u4e3a\u4e86\u52a0\u5feb\u9879\u76ee\u7684\u63a8\u8fdb\uff0c\u8be5\u7814\u7a76\u4ee5\u4e00\u7c7b\u62e5\u6709\u4e30\u5bcc\u5316\u5b66\u5408\u6210\u7ecf\u9a8c\u7684\u534a\u5939\u5fc3\u948c\uff08II\uff09\u914d\u5408\u7269\u4f5c\u4e3a\u8d77\u70b9\u3002\u4e3a\u4e86\u627e\u5bfb\u6b64\u7c7b\u542b\u948c\u9aa8\u67b6\u7684\u6f5c\u5728\u7ed3\u5408\u53e3\u888b\uff0c\u8be5\u7814\u7a76\u5c06\u4e00\u5bf9\u521a\u6027\u4e14\u758f\u6c34\u7684\u542b\u948c\u5f02\u6784\u4f53\uff08(<em>R<\/em>)-<strong>1<\/strong>\u548c(<em>S<\/em>)-<strong>1<\/strong>\uff09\u53cd\u5411\u5bf9\u63a5\u5230\u4ecePDB\u6570\u636e\u5e93\u4e2d\u63d0\u53d6\u76847670\u4e2a\u9ad8\u8d28\u91cf\u86cb\u767d\u8d28\u7ed3\u5408\u53e3\u888b\u4e2d\uff08\u56fe1\uff09\u3002\u4e3a\u65b9\u4fbf\u540e\u7eed\u4f7f\u7528\u9aa8\u67b6\u8dc3\u8fc1\u7684\u7b56\u7565\u8fdb\u884c\u7ed3\u6784\u4f18\u5316\uff0c\u8be5\u7814\u7a76\u4e3b\u8981\u6839\u636e\u5bf9\u63a5\u4f4d\u7f6e\u4e0e\u76f8\u5e94\u5171\u6676\u914d\u4f53\u7684\u758f\u6c34\u9aa8\u67b6\u7684\u91cd\u53e0\u7a0b\u5ea6\u5bf9\u6253\u5206\u6392\u540d\u9760\u524d\u7684\u7ed3\u5408\u53e3\u888b\u8fdb\u884c\u4e86\u8fc7\u6ee4\u3002\u968f\u540e\u7ecf\u8fc7\u53ef\u89c6\u5316\u5206\u6790\uff0c\u53d1\u73b0\u5728CB1\u4e2d\uff0c\u542b\u948c\u5f02\u6784\u4f53\u975e\u4f46\u4e0e\u5176\u5171\u6676\u914d\u4f53\u7684\u758f\u6c34\u9aa8\u67b6\u5f88\u597d\u5730\u91cd\u53e0\uff0c\u8fd8\u80fd\u4e0e\u7ed3\u5408\u53e3\u888b\u4e2d\u7684\u6c28\u57fa\u9178\u6b8b\u57fa\u5f62\u6210\u6709\u5229\u7684\u758f\u6c34\u548c\u03c0-\u03c0\u5806\u79ef\u76f8\u4e92\u4f5c\u7528\uff08\u56fe2\uff09\u3002\u53c8\u8003\u8651\u5230\u540e\u7eed\u7ed3\u6784\u4fee\u9970\u7684\u53ef\u5408\u6210\u6027\u4ee5\u53ca\u751f\u7269\u5b9e\u9a8c\u6d4b\u5b9a\u7684\u53ef\u884c\u6027\uff0c\u6700\u7ec8\u9009\u62e9\u5927\u9ebb\u7d20\u53d7\u4f53\u8fdb\u884c\u57fa\u4e8e\u7ed3\u6784\u7684\u4f18\u5316\u8bbe\u8ba1\u3002<\/p>\n\n\n\n<div class=\"wp-block-image\"><figure class=\"aligncenter size-large is-resized\"><a href=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f1.png\"><img loading=\"lazy\" src=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f1-1024x919.png\" alt=\"\" class=\"wp-image-1259\" width=\"807\" height=\"723\" srcset=\"https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f1-1024x919.png 1024w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f1-300x269.png 300w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f1-768x689.png 768w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f1.png 1052w\" sizes=\"(max-width: 807px) 100vw, 807px\" \/><\/a><figcaption><strong>\u56fe1 <\/strong>\u53d1\u73b0\u5177\u6709\u751f\u7269\u6d3b\u6027\u7684\u6709\u673a\u948c\u5316\u5408\u7269\u7684\u6d41\u7a0b\u56fe\u3002<\/figcaption><\/figure><\/div>\n\n\n\n<div class=\"wp-block-image\"><figure class=\"aligncenter size-full is-resized\"><a href=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f2.png\"><img loading=\"lazy\" src=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f2.png\" alt=\"\" class=\"wp-image-1260\" width=\"825\" height=\"381\" srcset=\"https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f2.png 851w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f2-300x139.png 300w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f2-768x356.png 768w\" sizes=\"(max-width: 825px) 100vw, 825px\" \/><\/a><figcaption><strong>\u56fe2<\/strong> \u542b\u948c\u5f02\u6784\u4f53 (<em>R<\/em>)-<strong>1<\/strong>\u548c (<em>S<\/em>)-<strong>1<\/strong>\u5728CB1\u7ed3\u5408\u53e3\u888b\u4e2d\u7684\u5bf9\u63a5\u4f4d\u7f6e\u3002\u5b50\u56feA\u3001B\u7684PDB\u7f16\u53f7\u5206\u522b\u4e3a5XR8\u548c5XRA\u3002\u5171\u6676\u914d\u4f53\u4ee5\u68d5\u8272\u68cd\u72b6\u6a21\u578b\u8868\u793a\uff0c(<em>R<\/em>)-<strong>1<\/strong>\u548c (<em>S<\/em>)-<strong>1<\/strong>\u5206\u522b\u4ee5\u84dd\u8272\u548c\u9ec4\u8272\u7403\u68cd\u6a21\u578b\u8868\u793a\u3002<\/figcaption><\/figure><\/div>\n\n\n\n<ul><li>\u9488\u5bf9\u5927\u9ebb\u7d20\u53d7\u4f53\u8fdb\u884c\u57fa\u4e8e\u7ed3\u6784\u7684\u4f18\u5316\u8bbe\u8ba1<\/li><\/ul>\n\n\n\n<p>\u5927\u9ebb\u7d20\u53d7\u4f53\u5305\u542bCB1\u548cCB2\u4e24\u4e2a\u4e9a\u578b\uff0c\u4e8c\u8005\u4e4b\u95f4\u7684\u5e8f\u5217\u540c\u4e00\u6027\u7ea6\u4e3a43%\u3002\u5728\u7ade\u4e89\u6027\u653e\u5c04\u914d\u4f53\u5b9e\u9a8c\u4e2d\uff0c\u57fa\u672c\u9aa8\u67b6\u5316\u5408\u7269<strong>1<\/strong>\u548c\u5176\u5bf9\u4f1e\u82b1\u70ef\u884d\u751f\u7269<strong>2<\/strong>\u5bf9CB1\u548cCB2\u5747\u672a\u663e\u793a\u51fa\u7ed3\u5408\u6d3b\u6027\uff08<em>K<\/em><sub>i<\/sub> &gt; 40000 nM\uff09\u3002\u7531\u4e8e\u8fd9\u4e24\u4e2a\u5316\u5408\u7269\u53ea\u5360\u636e\u7ed3\u5408\u53e3\u888b\u7684\u4e00\u5c0f\u90e8\u5206\uff0c\u6ca1\u6709\u7ed3\u5408\u6d3b\u6027\u662f\u610f\u6599\u4e4b\u4e2d\u7684\u3002\u4e3a\u6a21\u62df\u7ed3\u6676\u914d\u4f53\u7684\u7ed3\u6784\uff0c\u8be5\u7814\u7a76\u5728\u6709\u673a\u948c\u9aa8\u67b6\u7684\u4e0d\u540c\u4f4d\u7f6e\u5f15\u5165\u4e86\u76f8\u4f3c\u957f\u5ea6\u7684\u8102\u80aa\u94fe\u3002\u5e86\u5e78\u7684\u662f\uff0c\u5316\u5408\u7269<strong>3<\/strong>\u3001<strong>4<\/strong>\u548c<strong>5<\/strong>\u5bf9CB1\u548cCB2\u5747\u8868\u73b0\u51fa\u4e00\u5b9a\u7ed3\u5408\u6d3b\u6027\uff0c\u5176\u4e2d\u6d3b\u6027\u6700\u597d\u7684\u5316\u5408\u7269<strong>5<\/strong>\u5bf9CB1\u548cCB2\u7684<em>K<\/em><sub>i<\/sub>\u503c\u5206\u522b\u4e3a200\u548c165 nM\uff08\u56fe 3\uff09\u3002\u968f\u540e\u7684\u9499\u6d41\u529f\u80fd\u5b9e\u9a8c\u8868\u660e\u5316\u5408\u7269<strong>5<\/strong>\u5bf9\u5927\u9ebb\u7d20\u53d7\u4f53\u8868\u73b0\u51fa\u5fae\u6469\u5c14\u7ea7\u522b\u7684\u62ee\u6297\u6d3b\u6027\uff08\u5bf9CB1\u548cCB2\u7684IC<sub>50<\/sub>\u503c\u5206\u522b\u4e3a7439\u548c1700 nM\uff09\u3002\u968f\u540e\u4e3a\u964d\u4f4e\u67d4\u6027\u8102\u80aa\u94fe\u5e26\u6765\u7684\u71b5\u7684\u635f\u5931\uff0c\u8be5\u7814\u7a76\u57fa\u4e8e\u5316\u5408\u7269<strong>5<\/strong>\u5728\u62ee\u6297\u5242\u7ed3\u5408\u7684CB2\u5171\u6676\u7ed3\u6784\u4e2d\u7684\u5bf9\u63a5\u4f4d\u7f6e\uff0c\u5c1d\u8bd5\u7528\u82ef\u73af\u53d6\u4ee3\u8102\u80aa\u94fe\uff0c\u5e76\u5229\u7528\u5206\u5b50\u751f\u6210\u7684\u65b9\u6cd5\u5728\u82ef\u73af\u5bf9\u4f4d\u751f\u6210\u4e0d\u540c\u7684\u53d6\u4ee3\u57fa\u3002\u5728\u7ecfMM\/GBSA\u91cd\u6253\u5206\u4ee5\u53ca\u76f8\u4e92\u4f5c\u7528\u5206\u6790\u540e\uff0c\u9009\u62e9\u5e76\u5408\u6210\u4e86\u5e26\u6709\u6b63\u4e01\u57fa\u7684\u5316\u5408\u7269<strong>6<\/strong>\u548c<strong>7<\/strong>\u8fdb\u884c\u5b9e\u9a8c\u9a8c\u8bc1\u3002\u4e0e\u5316\u5408\u7269<strong>5<\/strong>\u76f8\u6bd4\uff0c\u5316\u5408\u7269<strong>6<\/strong>\u548c<strong>7<\/strong>\u5206\u522b\u5bf9CB2\u548cCB1\u7684\u7ed3\u5408\u6d3b\u6027\u67093\u500d\u5de6\u53f3\u7684\u63d0\u5347\u3002\u5316\u5408\u7269<strong>7<\/strong>\u5728\u9499\u6d41\u5b9e\u9a8c\u4e2d\u5bf9CB1\uff08IC<sub>50<\/sub> = 3133 nM\uff09\u548cCB2\uff08IC<sub>50<\/sub> = 2135 nM\uff09\u4e5f\u8868\u73b0\u51fa\u62ee\u6297\u4f5c\u7528\u3002\u968f\u540e\uff0c\u4e3a\u4e86\u63a2\u7a76\u5316\u5408\u7269\u7684\u7ed3\u5408\u7279\u6027\uff0c\u8be5\u7814\u7a76\u5408\u6210\u4e86\u4e00\u7cfb\u5217\u5316\u5408\u7269<strong>7<\/strong>\u7684\u884d\u751f\u7269\uff0c\u5bf9R2\u53d6\u4ee3\u57fa\u7684\u94fe\u957f\u5ea6\u548c\u5421\u5576\u73af\u4e0a\u4e0d\u540c\u4f4d\u7f6e\u7684R1\u53d6\u4ee3\u57fa\u8fdb\u884c\u4e86\u6784\u6548\u5173\u7cfb\u7814\u7a76\u3002\u5bf9\u4e8eCB1\uff0c\u7f29\u77ed\u6216\u5ef6\u957fR2\u53d6\u4ee3\u57fa\u7684\u94fe\u957f\u5ea6\u5747\u4f1a\u5bfc\u81f4\u7ed3\u5408\u6d3b\u6027\u660e\u663e\u964d\u4f4e\uff086~49\u500d\uff09\uff1b\u5728\u5421\u5576\u73af\u7684\u4e0d\u540c\u4f4d\u7f6e\u5f15\u5165F\u3001Cl\u3001Me\u6216CF<sub>3<\/sub>\u4e5f\u4f1a\u5bfc\u81f4\u7ed3\u5408\u6d3b\u6027\u6709\u4e0d\u540c\u7a0b\u5ea6\u7684\u964d\u4f4e\uff082~35\u500d\uff09\uff0c\u5176\u4e2d\u4f53\u79ef\u8f83\u5c0f\u7684F\u539f\u5b50\u5bf9\u6d3b\u6027\u5f71\u54cd\u6700\u5c0f\uff0c\u4f53\u79ef\u8f83\u5927\u7684CF<sub>3<\/sub>\u5bf9\u6d3b\u6027\u5f71\u54cd\u6700\u5927\u3002\u5bf9\u4e8eCB2\uff0c\u9664\u4e86\u53bb\u6389\u6b63\u4e01\u57fa\u7684\u5316\u5408\u7269<strong>8<\/strong> (16\u500d)\u3001\u4ee5\u53caCF<sub>3<\/sub>\u53d6\u4ee3\u7684\u5316\u5408\u7269<strong>16<\/strong>\u548c<strong>19<\/strong>\uff083\u500d\uff09\u6709\u660e\u663e\u7684\u6d3b\u6027\u964d\u4f4e\u5916\uff0c\u5176\u4ed6\u884d\u751f\u7269\u5bf9\u7ed3\u5408\u6d3b\u6027\u5f71\u54cd\u8f83\u5c0f\uff08&lt; 2\u500d\uff09\u3002\u8fd9\u4e9b\u884d\u751f\u7269\u5bf9CB1\u548cCB2\u7684\u7ed3\u5408\u6d3b\u6027\u5f71\u54cd\u7684\u7a0b\u5ea6\u4e0d\u540c\uff0c\u4f7f\u5f97\u4e00\u4e9b\u5316\u5408\u7269\u5bf9CB2\u6709\u8f83\u9ad8\u7684\u9009\u62e9\u6027\uff0c\u5c24\u5176\u662f\u5421\u5576\u73af\u7b2c4\u4f4d\u7684Cl\uff08\u5316\u5408\u7269<strong>14<\/strong>\uff0c18\u500d\u9009\u62e9\u6027\uff09\u548cMe\u53d6\u4ee3\uff08\u5316\u5408\u7269<strong>15<\/strong>\uff0c13\u500d\u9009\u62e9\u6027\uff09\u3002\u7531\u4e8eCB1\u548cCB2\u62ee\u6297\u5242\u7ed3\u5408\u53e3\u888b\u7684\u5927\u5c0f\u548c\u5f62\u72b6\u5b58\u5728\u5dee\u5f02\uff0c\u8fd9\u4e9b\u5316\u5408\u5bf9CB1\u548cCB2\u7684\u91c7\u7528\u4e86\u4e0d\u540c\u7684\u9884\u6d4b\u7ed3\u5408\u6a21\u5f0f\u3002\u4f46\u603b\u4f53\u800c\u8a00\uff0c\u5316\u5408\u7269\u5bf9CB1\u548cCB2\u7684\u9884\u6d4b\u7ed3\u5408\u6a21\u5f0f\u4e0e\u89c2\u5bdf\u5230\u7684\u6784\u6548\u5173\u7cfb\u4fdd\u6301\u4e00\u81f4\uff08\u8be6\u60c5\u89c1\u539f\u6587\uff09\u3002<\/p>\n\n\n\n<div class=\"wp-block-image\"><figure class=\"aligncenter size-large\"><a href=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f3.png\"><img loading=\"lazy\" width=\"1024\" height=\"472\" src=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f3-1024x472.png\" alt=\"\" class=\"wp-image-1296\" srcset=\"https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f3-1024x472.png 1024w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f3-300x138.png 300w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f3-768x354.png 768w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f3.png 1309w\" sizes=\"(max-width: 1024px) 100vw, 1024px\" \/><\/a><figcaption><strong>\u56fe3\u5316\u5408\u72695\u5728CB1\uff08A\uff1a PDB ID 5TGZ\uff09\u548cCB2\uff08B: PDB ID: 5ZTY\uff09\u7ed3\u5408\u53e3\u888b\u4e2d\u7684\u5bf9\u63a5\u4f4d\u7f6e\u3002<\/strong><\/figcaption><\/figure><\/div>\n\n\n\n<p><\/p>\n\n\n\n<ul><li>\u7ed3\u5408\u5927\u4e14\u758f\u6c34\u7684\u7ed3\u5408\u53e3\u888b<\/li><\/ul>\n\n\n\n<p>\u8003\u8651\u5230\u6b64\u7c7b\u91d1\u5c5e\u6709\u673a\u948c\u5316\u5408\u7269\u662f\u758f\u6c34\u7684\uff0c\u7814\u7a76\u8005\u731c\u60f3\u5b83\u4eec\u5f88\u6709\u53ef\u80fd\u7ed3\u5408\u5728\u5176\u4ed6\u5927\u4e14\u758f\u6c34\u6027\u7684\u7ed3\u5408\u53e3\u888b\u4e2d\u3002\u56e0\u6b64\uff0c\u7814\u7a76\u8005\u5c06\u5316\u5408\u7269<strong>7<\/strong>\u53cd\u5411\u5bf9\u63a5\u5230\u4ee5\u4e00\u5b9a\u6807\u51c6\u7b5b\u9009\u51fa\u7684155\u4e2a\u5927\u4e14\u758f\u6c34\u6027\u7684\u7ed3\u5408\u53e3\u888b\u4e2d\u3002\u7c7b\u4f3c\u5730\uff0c\u6839\u636e\u4e0e\u5171\u7ed3\u6676\u914d\u4f53\u7684\u91cd\u53e0\u7a0b\u5ea6\uff0c\u5c06\u5bf9\u63a5\u4f4d\u7f6e\u8fdb\u884c\u4e86\u7b5b\u9009\u3002\u7531\u4e8e\u5316\u5408\u7269<strong>7<\/strong>\u7684\u542b\u948c\u9aa8\u67b6\u5f88\u597d\u5730\u5951\u5408\u572815-LOX-2\u7684\u7ed3\u5408\u53e3\u888b\u4e2d\uff0c\u5e76\u4e14\u5176\u8102\u80aa\u94fe\u4e0e\u5171\u7ed3\u6676\u914d\u4f53\u7684\u671d\u5411\u7c7b\u4f3c\uff0c\u8be5\u7814\u7a76\u6700\u7ec8\u6311\u900915-LOX-2\u8fdb\u884c\u5b9e\u9a8c\u9a8c\u8bc1\uff08\u56fe4A\uff09\u3002\u5728\u8fdb\u884c\u5355\u70b9\u7b5b\u9009\u540e\uff0c\u5242\u91cf-\u53cd\u5e94\u5b9e\u9a8c\u7ed3\u679c\u8868\u660e\u5316\u5408\u7269<strong>5<\/strong>\u3001<strong>7<\/strong>\u548c<strong>18<\/strong>\u5747\u5bf915-LOX-2\u8868\u73b0\u51fa\u5fae\u6469\u5c14\u7ea7\u522b\u7684\u6291\u5236\u6d3b\u6027\uff08\u56fe4B\uff09\u3002<\/p>\n\n\n\n<p>\u53e6\u5916\uff0c\u4e3a\u4e86\u6392\u9664\u6b64\u7c7b\u5316\u5408\u7269\u7684\u7ed3\u5408\u6d3b\u6027\u662f\u7531\u80f6\u4f53\u805a\u96c6\u5bfc\u81f4\u7684\u975e\u7279\u5f02\u6027\u7ed3\u5408\u9020\u6210\u7684\uff0c\u7814\u7a76\u8005\u7b5b\u9009\u4e86\u5316\u5408\u7269<strong>7<\/strong>\u5bf9\u591a\u4e2a\u9776\u70b9\u7684\u7ed3\u5408\u6d3b\u6027\uff0c\u5305\u62ec\u4e0e\u5927\u9ebb\u7d20\u53d7\u4f53\u5177\u6709\u4e00\u5b9a\u5e8f\u5217\u76f8\u4f3c\u6027\u76843\u4e2aGPCR\u86cb\u767d\uff08LPA1\u3001 MCR4\u548cD1R\uff09\u3001\u4ee5\u53ca3\u4e2a\u5b9e\u9a8c\u5ba4\u5185\u90e8\u53ef\u7528\u7684\u9176\uff085-LOX\u3001SHP2\u548cCOMT\uff09\u3002\u7ed3\u679c\u8868\u660e\uff0c\u5316\u5408\u7269\u5bf9\u8fd9\u4e9b\u9776\u70b9\u5747\u6ca1\u6709\u7ed3\u5408\u6d3b\u6027\uff0c\u8bf4\u660e\u6b64\u7c7b\u5316\u5408\u7269\u5bf9\u5927\u9ebb\u7d20\u53d7\u4f53\u548c15-LOX-2\u7684\u7ed3\u5408\u6d3b\u6027\u4e0d\u662f\u975e\u7279\u5f02\u6027\u7ed3\u5408\u9020\u6210\u7684\u3002<\/p>\n\n\n\n<div class=\"wp-block-image\"><figure class=\"aligncenter size-large\"><a href=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f4.png\"><img loading=\"lazy\" width=\"1024\" height=\"416\" src=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f4-1024x416.png\" alt=\"\" class=\"wp-image-1298\" srcset=\"https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f4-1024x416.png 1024w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f4-300x122.png 300w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f4-768x312.png 768w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2024\/01\/f4.png 1219w\" sizes=\"(max-width: 1024px) 100vw, 1024px\" \/><\/a><figcaption><strong>\u56fe4<\/strong> \uff08A\uff09\u5316\u5408\u7269<strong>7<\/strong>\u5bf915-LOX-2\u7684\u5bf9\u63a5\u4f4d\u7f6e\uff1b\uff08B\uff0915-LOX-2\u9176\u6d3b\u6027\u6d4b\u5b9a\u7684\u5242\u91cf-\u53cd\u5e94\u66f2\u7ebf\u3002<\/figcaption><\/figure><\/div>\n\n\n\n<p><\/p>\n\n\n\n<p><strong>\u603b\u7ed3\u4e0e\u5c55\u671b<\/strong><\/p>\n\n\n\n<p>\u53d7\u91d1\u5c5e\u914d\u5408\u7269\u7acb\u4f53\u7ed3\u6784\u590d\u6742\u6027\u7684\u542f\u53d1\uff0c\u7814\u7a76\u8005\u5c1d\u8bd5\u7528\u516b\u9762\u4f53\u6709\u673a\u948c\u5316\u5408\u7269\u6765\u6269\u5c55\u5e38\u89c1\u6709\u673a\u5316\u5408\u7269\u7684\u5316\u5b66\u7a7a\u95f4\u3002\u901a\u8fc7\u53cd\u5411\u5206\u5b50\u5bf9\u63a5\u7b49\u57fa\u4e8e\u7ed3\u6784\u7684\u836f\u7269\u8bbe\u8ba1\u624b\u6bb5\uff0c\u8be5\u7814\u7a76\u6210\u529f\u5730\u5c06\u4e00\u4e2a\u521a\u6027\u7684\u516b\u9762\u4f53\u6709\u673a\u948c\u9aa8\u67b6\u4f18\u5316\u4e3a\u4e00\u7cfb\u5217\u5bf9\u5927\u9ebb\u7d20\u53d7\u4f53\u5177\u6709\u7eb3\u6469\u5c14\u7ea7\u522b\u7ed3\u5408\u4eb2\u548c\u529b\u7684\u542b\u948c\u5316\u5408\u7269\u3002\u5176\u4e2d\u591a\u4e2a\u5316\u5408\u7269\u5bf9CB2\u8868\u73b0\u51fa\u9ad8\u9009\u62e9\u6027\uff0c\u8868\u660e\u53ef\u4ee5\u5229\u7528\u91d1\u5c5e\u914d\u5408\u7269\u7684\u5f62\u72b6\u590d\u6742\u6027\u5b9e\u73b0\u9776\u70b9\u7279\u5f02\u6027\u3002\u540c\u65f6\uff0c\u5176\u4e2d\u591a\u4e2a\u5316\u5408\u7269\u5bf915-LOX-2\u8868\u73b0\u51fa\u5fae\u6469\u5c14\u6291\u5236\u6d3b\u6027\uff0c\u8bf4\u660e\u6b64\u7c7b\u6709\u673a\u948c\u5316\u5408\u7269\u53ef\u4ee5\u4f5c\u4e3a\u4e00\u7c7b\u4f18\u52bf\u9aa8\u67b6\u7ed3\u6784\u7ed3\u5408\u5230\u5927\u4e14\u758f\u6c34\u6027\u7684\u86cb\u767d\u7ed3\u5408\u53e3\u888b\u4e2d\u3002\u7efc\u4e0a\uff0c\u8be5\u7814\u7a76\u81f3\u5c11\u5728\u5206\u5b50\u548c\u7ec6\u80de\u6c34\u5e73\u4e0a\u5c55\u793a\u4e86\u91d1\u5c5e\u914d\u5408\u7269\u5728\u836f\u7269\u5f00\u53d1\u4e2d\u7684\u6f5c\u529b\u3002\u503c\u5f97\u4e00\u63d0\u7684\u662f\uff0c\u8be5\u7814\u7a76\u7684\u91cd\u70b9\u5e76\u4e0d\u662f\u5f00\u53d1CB1\u6216CB2\u62ee\u6297\u5242\uff0c\u800c\u662f\u63d0\u4f9b\u4e00\u79cd\u7528\u4e8e\u63a2\u7d22\u91d1\u5c5e\u914d\u5408\u7269\u5316\u5b66\u7a7a\u95f4\u7684\u57fa\u4e8e\u7ed3\u6784\u7684\u836f\u7269\u8bbe\u8ba1\u7b56\u7565\u3002\u5229\u7528\u8fd9\u4e00\u7b56\u7565\uff0c\u53ef\u4ee5\u5c1d\u8bd5CSD\u6570\u636e\u5e93\u4e2d\u4e0d\u540c\u7c7b\u578b\u7684\u91d1\u5c5e\u6709\u673a\u5316\u5408\u7269\uff0c\u901a\u8fc7\u5728\u836f\u7269\u8bbe\u8ba1\u4e2d\u5f15\u5165\u65b0\u5143\u7d20\uff0c\u62d3\u5c55\u65b0\u7684\u5316\u5b66\u7a7a\u95f4\uff0c\u4ece\u800c\u4fc3\u8fdb\u66f4\u591a\u65b0\u9776\u70b9\u7684\u63a2\u7d22\u3002<\/p>\n\n\n\n<p><strong><a href=\"https:\/\/pubs.acs.org\/doi\/10.1021\/acs.jcim.3c01282\" target=\"_blank\" rel=\"noreferrer noopener\">\u539f\u6587\u94fe\u63a5<\/a><\/strong><\/p>\n","protected":false},"excerpt":{"rendered":"<p>\u82f1\u6587\u539f\u9898\uff1aStructure-based Identification of Organoruthenium Compounds as Nanomolar Antagonists of Cannabinoid Receptors \u901a\u8baf\u4f5c\u8005\uff1aJianhui Huang, Niu Huang \u4f5c\u8005\uff1aQing Wang, Xuegang Fu, Yuting Yan, Tao Liu, Yuting Xie, Xiaoqing Song, Yu Zhou, Min Xu, Ping Wang, Peng Fu \u80cc\u666f\u4ecb\u7ecd 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