Arylamide derivatives as peptidomimetic inhibitors of calmodulin. Academic Article uri icon


  • [structure: see text] Many peptides bind to calmodulin (CaM) in a helical conformation. Here we describe a group of synthetic inhibitors of CaM based on an arylamide scaffold that is intended to mimic smMLCK, a CaM-binding helical peptide. Compound 1 showed a K(i) value of 7.10 +/- 1.48 nM in a fluorescence polarization assay that monitors the strong association of CaM and its peptide ligand mastoparan X. ((1)H,(15)N)-HSQC NMR spectroscopy experiments suggested that 1 binds to CaM in an analogous fashion to that of smMLCK.

published proceedings

  • Org Lett

author list (cited authors)

  • Yin, H., Frederick, K. K., Liu, D., Wand, A. J., & Degrado, W. F.

citation count

  • 34

complete list of authors

  • Yin, Hang||Frederick, Kendra K||Liu, Dahui||Wand, A Joshua||Degrado, William F

publication date

  • January 2006