The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics
Crucitti, Giuliana Cuzzucoli
Faculty of Sciences. Biology
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences. Pharmacy
, p. 1954-1958
University of Antwerp
KLK4 is a serine protease from the kallikrein family that is involved in cancer progression. The diphenyl phosphonate warhead is intended to bind irreversibly with serine proteases, but unexpectedly, very potent KLK4 diphenyl phosphonate inhibitors were discovered with reversible inhibition kinetics.