Method of cell surface activation and inhibition

摘要

Disclosed are a peptide and its use in a method of screening test compounds as potential inhibitors of matrix metalloproteinases. The peptide consists of residues Trp 574 to Asp 656 in the TIMP-2 binding site of the C-terminal domain of gelatinase-A as shown by SEQ ID NO:19. The method comprises determining the inhibitory effect of a test compound in a competitive inhibition assay with said peptide in which a Ki/Kd=>1 is deemed an inhibitory effect of said test compound, and in which Ki is the inhibitor constant of said test compound and Kd is the dissociation constant of said peptide.