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Photoactivatable peptides based on BMS-197525: a potent antagonist of the human thrombin receptor (PAR-1)
J T Elliott1, W J Hoekstra, B E Maryanoff
1Department of Physiology and Biophysics, University at Stony Brook, NY 11794, USA.
Bioorganic & Medicinal Chemistry Letters
|February 18, 1999
Abstract:
Photoactivatable analogs of the human thrombin receptor (PAR-1) antagonist, N-trans-cinnamoyl-p-fluoroPhe-p-guanidinoPhe-Leu-Arg-NH2 (BMS-197525), were prepared with benzophenone substitutions in the N-terminal, Leu, or Arg position. The analogs retained antagonist activity (with reduced potency); the tritium-labeled isotopomers are potential photoaffinity labels for the receptor. C-Terminal extension of the analogs with ornithine(biotin) did not significantly alter antagonist potency.