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Citation

BibTex format

@article{Panyain:2020:10.1021/jacs.0c04527,
author = {Panyain, N and Godinat, A and Lanyon-Hogg, T and Lachiondo-Ortega, S and Will, EJ and Soudy, C and Mondal, M and Mason, K and Elkhalifa, S and Smith, L and Harrigan, JA and Tate, EW},
doi = {10.1021/jacs.0c04527},
journal = {Journal of the American Chemical Society},
pages = {12020--12026},
title = {Discovery of a potent and selective covalent inhibitor and activity-based probe for the deubiquitylating enzyme UCHL1, with anti-fibrotic activity},
url = {http://dx.doi.org/10.1021/jacs.0c04527},
volume = {142},
year = {2020}
}
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RIS format (EndNote, RefMan)

TY  - JOUR
AB  - Ubiquitin carboxy-terminal hydrolase L1 (UCHL1) is a deubiquitylating enzyme which is proposed as a potential therapeutic target in neurodegeneration, cancer, and liver and lung fibrosis. Herein we report the discovery of the most potent and selective UCHL1 probe (IMP-1710) to date based on a covalent inhibitor scaffold and apply this probe to identify and quantify target proteins in intact human cells. IMP-1710 stereoselectively labels the catalytic cysteine of UCHL1 at low nanomolar concentration in cells. We further demonstrate that potent and selective UCHL1 inhibitors block pro-fibrotic responses in a cellular model of idiopathic pulmonary fibrosis, supporting the potential of UCHL1 as a potential therapeutic target in fibrotic diseases.
AU  - Panyain,N
AU  - Godinat,A
AU  - Lanyon-Hogg,T
AU  - Lachiondo-Ortega,S
AU  - Will,EJ
AU  - Soudy,C
AU  - Mondal,M
AU  - Mason,K
AU  - Elkhalifa,S
AU  - Smith,L
AU  - Harrigan,JA
AU  - Tate,EW
DO  - 10.1021/jacs.0c04527
EP  - 12026
PY  - 2020///
SN  - 0002-7863
SP  - 12020
TI  - Discovery of a potent and selective covalent inhibitor and activity-based probe for the deubiquitylating enzyme UCHL1, with anti-fibrotic activity
T2  - Journal of the American Chemical Society
UR  - http://dx.doi.org/10.1021/jacs.0c04527
UR  - https://pubs.acs.org/doi/10.1021/jacs.0c04527
UR  - http://hdl.handle.net/10044/1/80205
VL  - 142
ER  -
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Contact

Prof. Ed Tate
GSK Chair in Chemical Biology
Department of Chemistry
Molecular Sciences Research Hub, White City Campus,
82 Wood Lane, London, W12 0BZ

e.tate@imperial.ac.uk
Tel: +44 (0)20 759 + ext 43752 or 45821