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个人信息Personal Information
教授
博士生导师
硕士生导师
性别：女
毕业院校：大连理工大学
学位：博士
所在单位：医学部
学科：化学生物学. 药理学. 细胞生物学
办公地点：Chemical complex building,D513
联系方式：zczhang@dlut.edu.cn 13942696903
电子邮箱：zczhang@dlut.edu.cn
Two-Face, Two-Turn alpha-Helix Mimetics Based on a Cross-Acridine Scaffold: Analogues of the Bim BH3 Domain
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论文类型：期刊论文
发表时间：2014-06-16
发表刊物：CHEMBIOCHEM
收录刊物：SCIE、PubMed、Scopus
卷号：15
期号：9
页面范围：1280-1285
ISSN号：1439-4227
关键字：acridines; helical structures; Mcl-1; peptidomimetics; two-face
摘要：The design of a cross-acridine scaffold mimicking the i, i+3, i+5, and i+7 residues distributed over a two-face, two-turn alpha-helix is described. Docking studies and 2D H-1, N-15 HSQC NMR spectroscopy provide compelling evidence that compound 3d accurately reproduces the arrangement of four hotspots in the Bim BH3 peptide to permit binding to the Mcl-1 and Bcl-2 proteins (K-i 0.079 and 0.056 mu m, respectively). Furthermore, the hotspot mutation could also be mimicked by individual or multiple deletions of side chains on the scaffold.