Drug Development: Allosteric Inhibitors Hit USP7 Hard

Overview

Journal Nat Chem Biol

Specialties Biochemistry
Biology
Chemistry

Date 2018 Jan 17

PMID 29337966

Citations 6

Authors

Wei Zhang

Sachdev S Sidhu

Affiliations

Soon will be listed here.

Citing Articles

Targeting ubiquitin specific proteases (USPs) in cancer immunotherapy: from basic research to preclinical application.

Gao H, Yin J, Ji C, Yu X, Xue J, Guan X J Exp Clin Cancer Res. 2023; 42(1):225.

PMID: 37658402 PMC: 10472646. DOI: 10.1186/s13046-023-02805-y.

USP7 inhibition induces apoptosis in glioblastoma by enhancing ubiquitination of ARF4.

Pan T, Li X, Li Y, Tao Z, Yao H, Wu Y Cancer Cell Int. 2021; 21(1):508.

PMID: 34556124 PMC: 8461901. DOI: 10.1186/s12935-021-02208-z.

Structural and functional characterization of ubiquitin variant inhibitors for the JAMM-family deubiquitinases STAMBP and STAMBPL1.

Guo Y, Liu Q, Mallette E, Caba C, Hou F, Fux J J Biol Chem. 2021; 297(4):101107.

PMID: 34425109 PMC: 8449267. DOI: 10.1016/j.jbc.2021.101107.

Targeting the Ubiquitin-Proteasome System for Cancer Therapeutics by Small-Molecule Inhibitors.

LaPlante G, Zhang W Cancers (Basel). 2021; 13(12).

PMID: 34203106 PMC: 8235664. DOI: 10.3390/cancers13123079.

USP7 limits CDK1 activity throughout the cell cycle.

Galarreta A, Valledor P, Ubieto-Capella P, Lafarga V, Zarzuela E, Munoz J EMBO J. 2021; 40(11):e99692.

PMID: 33856059 PMC: 8167359. DOI: 10.15252/embj.201899692.

References

Ernst A, Avvakumov G, Tong J, Fan Y, Zhao Y, Alberts P . A strategy for modulation of enzymes in the ubiquitin system. Science. 2013; 339(6119):590-5. PMC: 3815447. DOI: 10.1126/science.1230161. View

Gabrielsen M, Buetow L, Nakasone M, Ahmed S, Sibbet G, Smith B . A General Strategy for Discovery of Inhibitors and Activators of RING and U-box E3 Ligases with Ubiquitin Variants. Mol Cell. 2017; 68(2):456-470.e10. PMC: 5655547. DOI: 10.1016/j.molcel.2017.09.027. View

Bedford L, Lowe J, Dick L, Mayer R, Brownell J . Ubiquitin-like protein conjugation and the ubiquitin-proteasome system as drug targets. Nat Rev Drug Discov. 2010; 10(1):29-46. PMC: 7097807. DOI: 10.1038/nrd3321. View

Zhang W, Sartori M, Makhnevych T, Federowicz K, Dong X, Liu L . Generation and Validation of Intracellular Ubiquitin Variant Inhibitors for USP7 and USP10. J Mol Biol. 2017; 429(22):3546-3560. DOI: 10.1016/j.jmb.2017.05.025. View

Colland F, Formstecher E, Jacq X, Reverdy C, Planquette C, Conrath S . Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells. Mol Cancer Ther. 2009; 8(8):2286-95. DOI: 10.1158/1535-7163.MCT-09-0097. View

Pozhidaeva A, Valles G, Wang F, Wu J, Sterner D, Nguyen P . USP7-Specific Inhibitors Target and Modify the Enzyme's Active Site via Distinct Chemical Mechanisms. Cell Chem Biol. 2017; 24(12):1501-1512.e5. DOI: 10.1016/j.chembiol.2017.09.004. View

Zhang W, Bailey-Elkin B, Knaap R, Khare B, Dalebout T, Johnson G . Potent and selective inhibition of pathogenic viruses by engineered ubiquitin variants. PLoS Pathog. 2017; 13(5):e1006372. PMC: 5451084. DOI: 10.1371/journal.ppat.1006372. View

Tavana O, Gu W . Modulation of the p53/MDM2 interplay by HAUSP inhibitors. J Mol Cell Biol. 2016; 9(1):45-52. PMC: 6310345. DOI: 10.1093/jmcb/mjw049. View

Zhang W, Wu K, Sartori M, Kamadurai H, Ordureau A, Jiang C . System-Wide Modulation of HECT E3 Ligases with Selective Ubiquitin Variant Probes. Mol Cell. 2016; 62(1):121-36. PMC: 4988125. DOI: 10.1016/j.molcel.2016.02.005. View

10.

Turnbull A, Ioannidis S, Krajewski W, Pinto-Fernandez A, Heride C, Martin A . Molecular basis of USP7 inhibition by selective small-molecule inhibitors. Nature. 2017; 550(7677):481-486. PMC: 6029662. DOI: 10.1038/nature24451. View

11.

Kategaya L, Di Lello P, Rouge L, Pastor R, Clark K, Drummond J . USP7 small-molecule inhibitors interfere with ubiquitin binding. Nature. 2017; 550(7677):534-538. DOI: 10.1038/nature24006. View