Receptor-bound conformation of an alpha(5)beta(1) integrin antagonist by (15)N-edited 2D transferred nuclear overhauser effects |
| |
Authors: | Zhang Li Mattern Ralph-Heiko Malaney Timothy I Pierschbacher Michael D Goodman Murray |
| |
Institution: | Department of Chemistry and Biochemistry, University of California at San Diego, 6223 Pacific Hall, La Jolla, CA 92093-0343, USA. |
| |
Abstract: | We report the results of (15)N-edited 2D transferred NOE experiments of the partially (15)N-labeled alpha(5)beta(1) antagonist cMpa(15)N-Arg-(15)N-Gly-(15)N-Asp-(15)N-Asp-(15)N-Val-Cys]-NH(2) (Mpa denotes mercaptopropionic acid) in the presence of the native alpha(5)beta(1) receptor. The alpha(5)beta(1) integrin receptor is believed to be involved in tumor metastasis and the rational design of alpha(5)beta(1) integrin antagonist is therefore of considerable interest. Our experiments provide insight into the alpha(5)beta(1) receptor-bound conformation of the antagonist cMpaRGDDVC]-NH2 and will be important for the design of novel antagonists. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|