PAR2 Modulators Derived from GB88.

  title={PAR2 Modulators Derived from GB88.},
  author={Mei-Kwan Yau and Ligong Liu and Jacky Y. Suen and Junxian Lim and R. H. Lohman and Yuhong Jiang and Adam J. Cotterell and Grant D Barry and Jeffrey Y W Mak and David A Vesey and Robert C Reid and David P. Fairlie},
  journal={ACS medicinal chemistry letters},
  volume={7 12},
PAR2 antagonists have potential for treating inflammatory, respiratory, gastrointestinal, neurological, and metabolic disorders, but few antagonists are known. Derivatives of GB88 (3) suggest that all four of its components bind at distinct PAR2 sites with the isoxazole, cyclohexylalanine, and isoleucine determining affinity and selectivity, while the C-terminal substituent determines agonist/antagonist function. Here we report structurally similar PAR2 ligands with opposing functions (agonist… CONTINUE READING


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