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Peptidomimetic inhibitors of APC-Asef interaction block colorectal cancer migration

文献类型：期刊论文

作者Jiang, Haiming2; Deng, Rong2; Yang, Xiuyan2; Shang, Jialin2; Lu, Shaoyong2; Zhao, Yanlong2; Song, Kun2; Liu, Xinyi2; Zhang, Qiufen2,4; Chen, Guoqiang2,6,7
刊名NATURE CHEMICAL BIOLOGY
出版日期2017
卷号13期号:9页码:994-+
ISSN号1552-4450
关键词Patient-derived tumor xenograft gene expression profile Monte Carlo feature selection support vector machine rule learning algorithm
DOI10.1038/NCHEMBIO.2442
文献子类Article
英文摘要The binding of adenomatous polyposis coli (APC) to its receptor Asef relieves the negative intramolecular regulation of Asef and leads to aberrant cell migration in human colorectal cancer. Because of its crucial role in metastatic dissemination, the interaction between APC and Asef is an attractive target for anti-colorectal-cancer therapy. We rationally designed a series of peptidomimetics that act as potent inhibitors of the APC interface. Crystal structures and biochemical and cellular assays showed that the peptidomimetics in the APC pocket inhibited the migration of colorectal cells by disrupting APC-Asef interaction. By using the peptidomimetic inhibitor as a chemical probe, we found that CDC42 was the downstream GTPase involved in APC-stimulated Asef activation in colorectal cancer cells. Our work demonstrates the feasibility of exploiting APC-Asef interaction to regulate the migration of colorectal cancer cells, and provides what to our knowledge is the first class of protein-protein interaction inhibitors available for the development of cancer therapeutics targeting APC-Asef signaling.
学科主题Biochemistry & Molecular Biology
WOS关键词ADENOMATOUS POLYPOSIS-COLI ; PROTEIN-PROTEIN INTERACTIONS ; THERMAL SHIFT ASSAYS ; CELL-PENETRATING PEPTIDES ; ARMADILLO REPEAT DOMAIN ; ARGININE-RICH PEPTIDES ; TUMOR-SUPPRESSOR GENE ; DRUG DISCOVERY ; FUTURE-DIRECTIONS ; METASTASIS
语种英语
出版者NATURE PUBLISHING GROUP
WOS记录号WOS:000407929800017
版本出版稿
源URL[http://202.127.25.144/handle/331004/1077]  
专题中国科学院上海生命科学研究院营养科学研究所
作者单位1.Shanghai Jiao Tong Univ, State Key Lab Microbial Metab, Shanghai, Peoples R China;
2.Shanghai Jiao Tong Univ, Sch Med, Minist Educ, Dept Pathophysiol,Key Lab Cell Differentiat & Apo, Shanghai, Peoples R China;
3.Shanghai Jiao Tong Univ, Sch Med, Shanghai Key Lab Tumor Microenvironm & Inflammat, Dept Biochem & Mol Cell Biol,State Key Lab Oncoge, Shanghai, Peoples R China;
4.Shanghai Jiao Tong Univ, Sch Med, Med Bioinformat Ctr, Shanghai, Peoples R China;
5.Chinese Acad Sci, Shanghai Inst Ceram, State Key Lab High Performance Ceram & Superfine, Shanghai, Peoples R China;
6.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Hlth Sci, Shanghai, Peoples R China;
7.Shanghai Jiao Tong Univ, Sch Med, Shanghai, Peoples R China;
8.East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai, Peoples R China,
推荐引用方式
GB/T 7714		 Jiang, Haiming,Deng, Rong,Yang, Xiuyan,et al. Peptidomimetic inhibitors of APC-Asef interaction block colorectal cancer migration[J]. NATURE CHEMICAL BIOLOGY,2017,13(9):994-+.
APA Jiang, Haiming.,Deng, Rong.,Yang, Xiuyan.,Shang, Jialin.,Lu, Shaoyong.,...&,.(2017).Peptidomimetic inhibitors of APC-Asef interaction block colorectal cancer migration.NATURE CHEMICAL BIOLOGY,13(9),994-+.
MLA Jiang, Haiming,et al."Peptidomimetic inhibitors of APC-Asef interaction block colorectal cancer migration".NATURE CHEMICAL BIOLOGY 13.9(2017):994-+.

入库方式： OAI收割

来源：上海营养与健康研究所

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