439948-77-3Relevant articles and documents
Arylamide derivatives as allosteric inhibitors of the integrin α2β1/type I collagen interaction
Yin, Hang,Gerlach, Lars Ole,Miller, Meredith W.,Moore, David T.,Liu, Dahui,Vilaire, Gaston,Bennett, Joel S.,DeGrado, William F.
, p. 3380 - 3382 (2006)
We herein report a group of allosteric inhibitors of integrin α2β1 based on an arylamide scaffold. Compound 4 showed an IC50 of 4.80 μM in disrupting integrin I-domain/collagen binding in an ELISA. These arylamide compound
Arylamide derivatives as peptidomimetic inhibitors of calmodulin
Yin, Hang,Frederick, Kendra K.,Liu, Dahui,Wand, A. Joshua,DeGrado, William F.
, p. 223 - 225 (2007/10/03)
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 Ki 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. (1H,15N)-HSQC NMR spectroscopy experiments suggested that 1 binds to CaM in an analogous fashion to that of smMLCK.