Re-Evaluating the Mechanism of Action of α,β-Unsaturated Carbonyl DUB Inhibitors b-AP15 and VLX1570: A Paradigmatic Example of Unspecific Protein Cross-linking with Michael Acceptor Motif-Containing Drugs

Author:

Ward Jennifer A.123ORCID,Pinto-Fernandez Adan24,Cornelissen Loïc5,Bonham Sarah2,Díaz-Sáez Laura12,Riant Olivier5ORCID,Huber Kilian V. M.12ORCID,Kessler Benedikt M.2,Feron Olivier4,Tate Edward W.3ORCID

Affiliation:

1. Structural Genomics Consortium, Nuffield Department of Medicine, University of Oxford, Oxford OX3 7DQ, U.K.

2. Target Discovery Institute, Nuffield Department of Medicine, University of Oxford, Oxford OX3 7FZ, U.K.

3. Department of Chemistry, Imperial College London, Molecular Sciences Research Hub, White City Campus, London W12 0BZ, U.K.

4. Pole of Pharmacology and Therapeutics (FATH), Institut de Recherche Expérimentale et Clinique (IREC), UCLouvain, 57 Avenue Hippocrate B1.57.04, Brussels B-1200, Belgium

5. Institute of Condensed Matter and Nanosciences, MOST Division, Place Louis Pasteur, UCLouvain, Louvain-la-Neuve B-1348, Belgium

Funder

Myeloma UK

Institute of Chemical Biology EPSRC CDT (Imperial College London)

Brussels-Capital Region

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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