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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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