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  • Title: Non-peptide RGD surrogates which mimic a Gly-Asp beta-turn: potent antagonists of platelet glycoprotein IIb-IIIa.
    Author: Fisher MJ, Gunn B, Harms CS, Kline AD, Mullaney JT, Nunes A, Scarborough RM, Arfsten AE, Skelton MA, Um SL, Utterback BG, Jakubowski JA.
    Journal: J Med Chem; 1997 Jun 20; 40(13):2085-101. PubMed ID: 9207949.
    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.
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