Related Experiment Video
Updated: Jul 30, 2026

Modification and Functionalization of the Guanidine Group by Tailor-made Precursors
Published on: April 27, 2017
Non-peptide RGD surrogates which mimic a Gly-Asp beta-turn: potent antagonists of platelet glycoprotein IIb-IIIa
M J Fisher1, B Gunn, C S Harms
1Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA.
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 beta-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 chain at position 6, were prepared and were found to have modest affinity for GPIIb-IIIa. Systematic modification of the basic residue contained in these molecules yielded compounds with high affinity for GPIIb-IIIa.
Related Concept Videos
Small GTPases - Ras and Rho
Three regulatory proteins control their activity:
Activation and Inactivation of G Proteins
GPCR Desensitization
GPCRs Regulate Adenylyl Cylase Activity
Two...
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Glucagon-like Receptor Agonists
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...

