The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics

Titel:: The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics
Dokumenttyp:: Article
Autor(en):: van Soom, J; Crucitti, GC; Gladysz, R; van der Veken, P; Di Santo, R; Stuyver, I; Buck, V; Lambeir, AM; Magdolen, V; Joossens, J; Augustyns, K
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.
Zeitschriftentitel:: MedChemComm
Jahr:: 2015
Band / Volume:: 6
Heft / Issue:: 11
Seitenangaben Beitrag:: 1954-1958
Sprache:: eng
Print-ISSN:: 2040-2503
TUM Einrichtung:: Frauenklinik und Poliklinik
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