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Nonpeptide RGD antagonists: a novel class of mimetics, the 5,8-disubstituted 1-azabicyclo[5.2.0]nonan-2-one lactam
Article de revue   Avec comité de lecture

Nonpeptide RGD antagonists: a novel class of mimetics, the 5,8-disubstituted 1-azabicyclo[5.2.0]nonan-2-one lactam

Erika Bourguet, Jean-Louis Banères, Joseph Parello, Xavier Lusinchi, Jean-Pierre Girard et Jean-Pierre Vidal
Bioorganic & medicinal chemistry letters, Vol.13(9), pp.1561-1564
05/05/2003
PMID: 12699755

Résumé

Amino Acid Motifs Bridged Bicyclo Compounds - chemical synthesis Bridged Bicyclo Compounds - pharmacology Drug Design Fibronectins - chemistry Integrin alpha5beta1 - chemistry Lactams - chemical synthesis Lactams - chemistry Lactams - pharmacology Molecular Mimicry Oligopeptides - antagonists & inhibitors Oligopeptides - chemistry Stereoisomerism
The 1-azabicyclo[5.2.0]nonan-2-one lactam 1 adequately substituted on both cycles A and B as scaffolds mimics the conformationally constrained beta-turn of the tripeptide RGD signaling motif of fibronectin. Using an in vitro assay, we establish that trans diastereoisomer 1b dissociates a soluble fibronectin-integrin alpha(5)beta(1) complex at concentrations comparable to those of a linear RGDS peptide as a competitor.

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1 Consultations de la notice

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