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Title:

The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics

Document type:
Article
Author(s):
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.
Journal title abbreviation:
MedChemComm
Year:
2015
Journal volume:
6
Journal issue:
11
Pages contribution:
1954-1958
Language:
eng
Print-ISSN:
2040-2503
TUM Institution:
Frauenklinik und Poliklinik
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