| Literature DB >> 11738566 |
Robert S Meissner1, James J Perkins, Le T Duong, George D Hartman, William F Hoffman, Joel R Huff, Nathan C Ihle, Chih Tai Leu, Rose M Nagy, Adel Naylor-Olsen, Gideon A Rodan, Sevgi B Rodan, David B Whitman, Gregg A Wesolowski, Mark E Duggan.
Abstract
Mimetics of the RGD tripeptide are described that are potent, selective antagonists of the integrin receptor, alpha(v)beta(3). The use of the 5,6,7,8-tetrahydro[1,8]naphthyridine group as a potency-enhancing N-terminus is demonstrated. Two 3-substituted-3-amino-propionic acids previously contained in alpha(IIb)beta(3) antagonists were utilized to enhance binding affinity and functional activity for the targeted receptor. Further affinity increases were then achieved through the use of cyclic glycyl amide bond constraints.Entities:
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Year: 2002 PMID： 11738566 DOI： 10.1016/s0960-894x(01)00687-4
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823