USP7 small-molecule inhibitors interfere with ubiquitin binding

Lorna Kategaya, Paola Di Lello, Lionel Rougé, Richard Pastor, Kevin R. Clark, Jason Drummond, Tracy Kleinheinz, Eva Lin, John-Paul Upton, Sumit Prakash, Johanna Heideker, Mark McCleland, Maria Stella Ritorto, Dario R. Alessi, Matthias Trost, Travis W. Bainbridge, Michael C. M. Kwok, Taylur P. Ma, Zachary Stiffler, Bradley Brasher, Yinyan Tang, Priyadarshini Jaishankar, Brian R. Hearn, Adam R. Renslo, Michelle R. Arkin, Frederick Cohen, Kebing Yu, Frank Peale, Florian Gnad, Matthew T. Chang, Christiaan Klijn, Elizabeth Blackwood, Scott E. Martin, William F. Forrest, James A. Ernst, Chudi Ndubaku, Xiaojing Wang, Maureen H. Beresini, Vickie Tsui, Carsten Schwerdtfeger, Robert A. Blake, Jeremy Murray, Till Maurer () and Ingrid E. Wertz ()
Additional contact information
Lorna Kategaya: Genentech
Paola Di Lello: Genentech
Lionel Rougé: Genentech
Richard Pastor: Genentech
Kevin R. Clark: Genentech
Jason Drummond: Genentech
Tracy Kleinheinz: Genentech
Eva Lin: Genentech
John-Paul Upton: Genentech
Sumit Prakash: Genentech
Johanna Heideker: Genentech
Mark McCleland: Genentech
Maria Stella Ritorto: MRC Protein Phosphorylation and Ubiquitylation Unit, School of Life Sciences, University of Dundee
Dario R. Alessi: MRC Protein Phosphorylation and Ubiquitylation Unit, School of Life Sciences, University of Dundee
Matthias Trost: Institute for Cell and Molecular Biosciences, Newcastle University
Travis W. Bainbridge: Genentech
Michael C. M. Kwok: Genentech
Taylur P. Ma: Proteomics, and Lipidomics, Genentech
Zachary Stiffler: Boston Biochem
Bradley Brasher: Boston Biochem
Yinyan Tang: University of California, San Francisco
Priyadarshini Jaishankar: University of California, San Francisco
Brian R. Hearn: University of California, San Francisco
Adam R. Renslo: University of California, San Francisco
Michelle R. Arkin: University of California, San Francisco
Frederick Cohen: Genentech
Kebing Yu: Proteomics, and Lipidomics, Genentech
Frank Peale: Genentech
Florian Gnad: Genentech
Matthew T. Chang: Genentech
Christiaan Klijn: Genentech
Elizabeth Blackwood: Genentech
Scott E. Martin: Genentech
William F. Forrest: Genentech
James A. Ernst: Genentech
Chudi Ndubaku: Genentech
Xiaojing Wang: Genentech
Maureen H. Beresini: Genentech
Vickie Tsui: Genentech
Carsten Schwerdtfeger: Boston Biochem
Robert A. Blake: Genentech
Jeremy Murray: Genentech
Till Maurer: Genentech
Ingrid E. Wertz: Genentech

Nature, 2017, vol. 550, issue 7677, 534-538

Abstract: The development of selective ubiquitin-specific protease-7 (USP7) inhibitors GNE-6640 and GNE-6776, which induce tumour cell death and reveal differential kinetics of Lys-48 and Lys-63-linked ubiquitin chain depolymerization by USP7.

Date: 2017
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DOI: 10.1038/nature24006

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