Photoactivatable peptides based on BMS-197525: A potent antagonist of the human thrombin receptor (PAR-1)
Photoactivatable analogs of the human thrombin receptor (PAR-1) antagonist, N-trans-cinnamoyl-p-fluoroPhe-p-guandinoPhe-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.
Elliott, John T.,Hoekstra, William J.,Maryanoff, Bruce E.,Prestwich, Glenn D.