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.
The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics / van Soom, Jeroen; Cuzzucoli Crucitti, Giuliana; Gladysz, Rafaela; van der Veken, Pieter; Di Santo, Roberto; Stuyver, Ingmar; Buck, Victoria; Lambeir, Anne-Marie; Magdolen, Viktor; Joossens, Jurgen; Augustyns, Koen. - In: MEDCHEMCOMM. - ISSN 2040-2503. - STAMPA. - 6:11(2015), pp. 1954-1958. [10.1039/C5MD00288E]
The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics
Cuzzucoli Crucitti, Giuliana;Di Santo, Roberto;
2015
Abstract
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.| File | Dimensione | Formato | |
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