Photoactivatable peptides based on BMS-197525: a potent antagonist of the human thrombin receptor (PAR-1)

…, WJ Hoekstra, BE Maryanoff, GD Prestwich

Index: Elliott, John T.; Hoekstra, William J.; Maryanoff, Bruce E.; Prestwich, Glenn D. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 2 p. 279 - 284

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Citation Number: 24

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 ( ...