Abstract
[structure: see text]. A small library of cyclic RGD pseudopentapeptides incorporating stereoisomeric 6,5- and 7,5-fused bicyclic lactams was synthesized with the aim of developing active and selective integrin antagonists. The solid-phase synthesis and activity of these RGD derivatives is described. The approach led to two of the most active known inhibitors of alpha(V)beta3 receptor.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Antineoplastic Agents / chemical synthesis
-
Antineoplastic Agents / chemistry
-
Antineoplastic Agents / metabolism
-
Bridged Bicyclo Compounds / chemical synthesis*
-
Bridged Bicyclo Compounds / chemistry
-
Bridged Bicyclo Compounds / metabolism
-
Cyclization
-
Intercellular Signaling Peptides and Proteins
-
Kinetics
-
Lactams / chemical synthesis*
-
Lactams / chemistry
-
Lactams / metabolism
-
Molecular Structure
-
Oligopeptides / chemical synthesis*
-
Oligopeptides / chemistry
-
Oligopeptides / metabolism
-
Peptide Library
-
Peptides / metabolism
-
Platelet Aggregation Inhibitors / metabolism
-
Protein Structure, Secondary
-
Radioligand Assay
-
Receptors, Vitronectin / antagonists & inhibitors*
-
Receptors, Vitronectin / chemistry
Substances
-
Antineoplastic Agents
-
Bridged Bicyclo Compounds
-
Intercellular Signaling Peptides and Proteins
-
Lactams
-
Oligopeptides
-
Peptide Library
-
Peptides
-
Platelet Aggregation Inhibitors
-
Receptors, Vitronectin
-
echistatin
-
arginyl-glycyl-aspartic acid