\u9976\u71cf\u6559\u6388\u4ece\u4e8b\u65b0\u836f\u53d1\u73b0\u7684\u5316\u5b66\u751f\u7269\u5b66\u7814\u7a76\uff0c\u957f\u671f\u81f4\u529b\u4e8e\u86cb\u767d\u8d28\u9776\u5411\u964d\u89e3\u6280\u672f\uff08PROTAC\uff09\u7684\u5f00\u53d1\u548c\u5e94\u7528\u3002\u7814\u7a76\u5de5\u4f5c\u4e3b\u8981\u56f4\u7ed5’\u6297\u91cd\u5927\u75be\u75c5\u5148\u5bfc\u5316\u5408\u7269\u7684\u53d1\u73b0\u548c\u4f18\u5316’\u5f00\u5c55\u3002\u4ee3\u8868\u6027\u8bba\u6587\u53d1\u8868\u4e8eNature Chemical Biology, Nature Communications, Cell Research, Leukemia, Journal of Medicinal Chemistry, Cell Discovery, Protein & Cell\u7b49\u56fd\u9645\u5b66\u672f\u671f\u520a\u3002\u53d7\u9080\u53c2\u7f16\u9996\u90e8PROTAC\u86cb\u767d\u964d\u89e3\u4e13\u8457”Protein Degradation with New Chemical Modalities”\u7684\u7f16\u5199\u3002\u9976\u71cf\u5b9e\u9a8c\u5ba4\u901a\u8fc7\u53d1\u5c55\u65b0\u578b\u5c0f\u5206\u5b50\u9776\u5411\u86cb\u767d\u964d\u89e3\u6280\u672f\u5e0c\u671b\u89e3\u51b3\u82e5\u5e72\u957f\u671f\u56f0\u6270\u7684\u751f\u7269\u5b66\u548c\u533b\u5b66\u95ee\u9898\uff0c\u5e76\u53d6\u5f97\u4e86\u4e00\u7cfb\u5217\u7684\u7814\u7a76\u8fdb\u5c55\uff1a1\uff09\u57fa\u4e8e\u9776\u5411\u86cb\u767d\u964d\u89e3\u6280\u672fPROTAC\u5efa\u7acbBRD4\u76f8\u5206\u79bb\u7814\u7a76\u65b0\u65b9\u6cd5\uff08Cell Discovery 2023\uff09\uff1b2\uff09\u63d0\u51fa\u4e86PROTAC\u548c\u5206\u5b50\u80f6\u534f\u540c\u5e94\u7528\u7684\u6a21\u5f0f\u3002\u6839\u636ePROTAC\u548c\u5206\u5b50\u80f6\u7684\u7279\u70b9\u9996\u6b21\u8bbe\u8ba1\u5408\u6210\u4e86\u65b0\u578b\u53cc\u9776\u3001\u53cc\u673a\u5236\u7684\u964d\u89e3\u5242\uff0c\u4e3a\u9776\u5411\u964d\u89e3\u6280\u672f\u7684\u53d1\u5c55\u63d0\u51fa\u4e86\u65b0\u7684\u601d\u8def\uff08Cell Research 2021\uff09\uff1b3\uff09\u5b9e\u73b0\u96be\u6210\u836f\u9776\u70b9\u7684\u836f\u7269\u5f00\u53d1\uff0c\u8bbe\u8ba1\u5408\u6210\u9996\u4f8b\u9009\u62e9\u6027CDK2\u964d\u89e3\u5242\uff0c\u5b9e\u73b0AML\u9ad8\u6548\u4e14\u4f4e\u6bd2\u7684\u5206\u5316\u6cbb\u7597\uff08Nature Chemical Biology 2021\uff09\uff1b4\uff09\u6784\u5efa\u9ad8\u6548\u7684BTK\u964d\u89e3\u5242\uff0c\u89e3\u51b3\u4e34\u5e8a\u4e2d\u51fa\u73b0\u7684Ibrutinib\u8010\u836f\u95ee\u9898\uff08Cell Research 2018\uff1bLeukemia 2019\uff09\uff1b5\uff09\u6784\u5efaPROTACs\u7cfb\u7edf\u6027\u6572\u9664\u6a21\u578b\uff0c\u5feb\u901f\u53ef\u9006\u5b9e\u73b0\u975e\u4eba\u7075\u957f\u7c7b\u52a8\u7269\u4f53\u5185\u86cb\u767d\u6572\u9664\uff08Cell Discovery 2019\uff09\u3002\u7814\u7a76\u75be\u75c5\u9886\u57df\u4e3b\u8981\u5305\u62ec\u6076\u6027\u80bf\u7624\uff0c\u611f\u67d3\u53ca\u8001\u5e74\u9000\u884c\u6027\u75be\u75c5\u3002\u91cd\u70b9\u7814\u7a76\u65b9\u5411\u5305\u62ec\u4ee5\u4e0b\u65b9\u9762\uff1a\u53d1\u5c55\u5c0f\u5206\u5b50\u9776\u5411\u86cb\u767d\u964d\u89e3\u6280\u672f\uff08PROTAC\/\u5206\u5b50\u80f6\u7b49\uff09\u8fdb\u884c\u9776\u5411\u86cb\u767d\u964d\u89e3\u53ca\u76f8\u5173\u836f\u7269\u7814\u7a76\uff1b\u4f9d\u636e\u86cb\u767d\u8d28\u4e09\u7ef4\u7ed3\u6784\u8fdb\u884c\u6297\u80bf\u7624\u3001\u6297\u611f\u67d3\u75be\u75c5\u5c0f\u5206\u5b50\u5316\u5408\u7269\u7684\u8bbe\u8ba1\u3001\u5408\u6210\u4e0e\u5f00\u53d1\uff1b\u5177\u6709\u9ad8\u751f\u7269\u6d3b\u6027\u5c0f\u5206\u5b50\u7684\u5316\u5b66\u5408\u6210\u53ca\u4f5c\u4e3a\u5206\u5b50\u63a2\u9488\u5e94\u7528\u4e8e\u5316\u5b66\u751f\u7269\u5b66\u7814\u7a76\u3002<\/p>\n
Professor Yi Rao is engaged in chemical biology research for new drug discovery, with long-term dedication to the development and application of protein targeting degradation technology (PROTAC). Research work mainly focuses on “discovery and optimization of lead compounds against major diseases”. Representative papers have been published in international academic journals such as Nature Chemical Biology, Nature Communications, Cell Research, Leukemia, Journal of Medicinal Chemistry, Cell Discovery, and Protein & Cell. Invited to participate in writing the first PROTAC protein degradation monograph “Protein Degradation with New Chemical Modalities”. The Rao Yi laboratory aims to solve several long-standing biological and medical problems through developing novel small molecule targeted protein degradation technologies, achieving a series of research advances: 1) Established a new method for BRD4 phase separation research based on targeted protein degradation technology PROTAC (Cell Discovery 2023); 2) Proposed a synergistic application mode of PROTAC and molecular glue. Based on the characteristics of PROTAC and molecular glue, first designed and synthesized a novel dual-target, dual-mechanism degrader, proposing new ideas for the development of targeted degradation technology (Cell Research 2021); 3) Achieved drug development for difficult-to-drug targets, designed and synthesized the first selective CDK2 degrader, achieving efficient and low-toxicity differentiation therapy for AML (Nature Chemical Biology 2021); 4) Constructed efficient BTK degraders to solve the Ibrutinib resistance problem in clinical practice (Cell Research 2018; Leukemia 2019); 5) Constructed PROTAC systematic knockout models, rapidly and reversibly achieving protein knockout in non-human primates (Cell Discovery 2019). Research disease areas mainly include malignant tumors, infections, and age-related degenerative diseases. Key research directions include: developing small molecule targeted protein degradation technologies (PROTAC\/molecular glue, etc.) for targeted protein degradation and related drug research; designing, synthesizing and developing anti-tumor and anti-infection small molecule compounds based on protein three-dimensional structures; chemical synthesis of highly bioactive small molecules and their application as molecular probes in chemical biology research.<\/p>\n
1. Y. Shi, Y. Liao, Q. Liu, Z. Ni, Z. Zhang, M. Shi, P. Li*, H. Li*, Y. Rao*, ‘BRD4-targeting PROTAC as a unique tool to study biomolecular condensates’, Cell Discovery, 2023, 9, DOI: 10.1038\/s41421-023-00544-0.
\n2. Z. Yang, Y. Sun, Z. Ni, C. Yang, Y. Tong, Y. Liu, H. Li and Y. Rao*, ‘Merging PROTAC and molecular glue for degrading BTK and GSPT1 proteins concurrently’, Cell Research, 2021, 25, 1315-1318.
\n3. L. Wang, X. Shao, T. Zhong, Y. Wu, A. Xu, X. Sun, H. Gao, Y. Liu, T. Lan, Y. Tong, X. Tao, W. Du, W. Wang, Y. Chen, T. Li, X. Meng, H. Deng, B. Yang, Q. He, M. Ying*, Y. Rao*, ‘Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy’, Nature Chemical Biology, 2021, 16.<\/p>\n","protected":false},"featured_media":0,"template":"","member_category":[],"class_list":["post-858","council_member","type-council_member","status-publish","hentry"],"acf":[],"_links":{"self":[{"href":"http:\/\/cnhupo.org.cn\/zh\/wp-json\/wp\/v2\/council_member\/858","targetHints":{"allow":["GET"]}}],"collection":[{"href":"http:\/\/cnhupo.org.cn\/zh\/wp-json\/wp\/v2\/council_member"}],"about":[{"href":"http:\/\/cnhupo.org.cn\/zh\/wp-json\/wp\/v2\/types\/council_member"}],"wp:attachment":[{"href":"http:\/\/cnhupo.org.cn\/zh\/wp-json\/wp\/v2\/media?parent=858"}],"wp:term":[{"taxonomy":"member_category","embeddable":true,"href":"http:\/\/cnhupo.org.cn\/zh\/wp-json\/wp\/v2\/member_category?post=858"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}