The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics

Jeroen Van Soom; Giuliana Cuzzucoli Crucitti; Rafaela Gladysz; Pieter Van Der Veken; Roberto Di Santo; Ingmar Stuyver; Victoria Buck; Anne Marie Lambeir; Viktor Magdolen; Jurgen Joossens; Koen Augustyns

doi:10.1039/c5md00288e

The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics

Jeroen Van Soom, Giuliana Cuzzucoli Crucitti, Rafaela Gladysz, Pieter Van Der Veken, Roberto Di Santo, Ingmar Stuyver, Victoria Buck, Anne Marie Lambeir, Viktor Magdolen, Jurgen Joossens, Koen Augustyns

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

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.

Original language	English
Pages (from-to)	1954-1958
Number of pages	5
Journal	MedChemComm
Volume	6
Issue number	11
DOIs	https://doi.org/10.1039/c5md00288e
State	Published - 3 Sep 2015
Externally published	Yes

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10.1039/c5md00288e

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title = "The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics",

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.",

author = "{Van Soom}, Jeroen and {Cuzzucoli Crucitti}, Giuliana and Rafaela Gladysz and {Van Der Veken}, Pieter and {Di Santo}, Roberto and Ingmar Stuyver and Victoria Buck and Lambeir, {Anne Marie} and Viktor Magdolen and Jurgen Joossens and Koen Augustyns",

note = "Publisher Copyright: {\textcopyright} The Royal Society of Chemistry.",

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doi = "10.1039/c5md00288e",

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T1 - The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics

AU - Van Soom, Jeroen

AU - Cuzzucoli Crucitti, Giuliana

AU - Gladysz, Rafaela

AU - Van Der Veken, Pieter

AU - Di Santo, Roberto

AU - Stuyver, Ingmar

AU - Buck, Victoria

AU - Lambeir, Anne Marie

AU - Magdolen, Viktor

AU - Joossens, Jurgen

AU - Augustyns, Koen

PY - 2015/9/3

Y1 - 2015/9/3

N2 - 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.

AB - 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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U2 - 10.1039/c5md00288e

DO - 10.1039/c5md00288e

M3 - Article

AN - SCOPUS:84946553049

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VL - 6

SP - 1954

EP - 1958

JO - MedChemComm

JF - MedChemComm

IS - 11

ER -

The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics

Abstract

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