Multiple N-Methylation by a Designed Approach Enhances Receptor Selectivity
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- 作者：Jayanta Chatterjee ; Oded Ovadia ; Grit Zahn ; Luciana Marinelli ; Amnon Hoffman ; Chaim Gilon ; Horst Kessler
- 刊名：Journal of Medicinal Chemistry
- 出版年：2007
- 出版时间：November 29, 2007
- 年：2007
- 卷：50
- 期：24
- 页码：5878 - 5881
- 全文大小：159K
- 年卷期：v.50,no.24(November 29, 2007)
- ISSN：1520-4804
文摘
An unselective cyclic peptide integrin ligand was sequentially N-methylated by a designed approach, where only the externallyoriented (solvent exposed) amide bonds were N-methylated. TheN-methylation resulted in tremendous enhancement in selectivity amongthe different integrin receptor subtypes (51, v3, and IIb3).Conformational and docking studies were performed, which suggestedthat the receptor selectivity is principally caused by reduced backboneflexibility due to N-methylation.