Title
The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics
Author
Faculty/Department
Faculty of Sciences. Biology
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences. Pharmacy
Publication type
article
Publication
Subject
Chemistry
Biology
Pharmacology. Therapy
Source (journal)
MedChemComm
Volume/pages
6(2015) :11 , p. 1954-1958
ISSN
2040-2503
ISI
000364154000005
Carrier
E
Target language
English (eng)
Full text (Publishers DOI)
Affiliation
University of Antwerp
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.
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