Non-peptide RGD surrogates which mimic a Gly-Asp β-turn: potent antagonists of platelet glycoprotein IIb-IIIa

…, JT Mullaney, A Nunes, RM Scarborough…

Index: Fisher, Matthew J.; Gunn, Bruce; Harms, Cathy S.; Kline, Allen D.; Mullaney, Jeffrey T.; Nunes, Anne; Scarborough, Robert M.; Arfsten, Ann E.; Skelton, Marshall A.; Um, Suzane L.; Utterback, Barbara G.; Jakubowski, Joseph A. Journal of Medicinal Chemistry, 1997 , vol. 40, # 13 p. 2085 - 2101

Full Text: HTML

Citation Number: 55

Abstract

Cyclic heptapeptide 1, which contains an Arg-Gly-Asp sequence, has good affinity for the platelet receptor GPIIb-IIIa and was chosen for study by 1H NMR techniques. The key RGD sequence of this molecule was found to reside in a conformationally defined type II'Gly-Asp β-turn, and this information was used in the design of simple non-peptide RGD mimics. Disubstituted isoquinolones, bearing an acidic side chain at position 2 and a basic side ...