N -Methylated Cyclic RGD Peptides as Highly Active and Selective ?? V ?? 3 Integrin Antagonists

来自 Semantic Scholar

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阅读量：

154

作者：

Michael A. Dechantsreiter，Eckart Planker，Barbara Math，Elisabeth Lohof，Horst Kessler

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摘要：

The alpha(V)beta(3) integrin receptor plays an important role in and -induced . The in vivo inhibition of this receptor by or by containing the RGD sequence may in the future be used to selectively suppress these diseases. Here we investigate the influence of N-of the active and selective alpha(V)beta(3) antagonist cyclo(RGDfV) (L1) on biological activity. Cyclo(RGDf-N(Me)V-) (P5) was found to be even more active than L1 and is one of the most active and selective compounds in inhibiting to the alpha(V)beta(3) integrin. Its high-resolution, three-dimensional structure in was determined by techniques, distance geometry calculations, and molecular dynamics calculations, providing more insight into the structure-activity relationship.

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关键词：

complexation membranes neurotransmitters polycyclic heterocyclic compounds

DOI：

10.1021/jm970832g

被引量：

785

年份：

1999