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. 2020 Apr 6;21(7):2548. doi: 10.3390/ijms21072548

Table 3.

Summary of known DUB inhibitors that are targeted in cancer cells.

DUBs DUBs Inhibitors Therapeutic Targets Functional Effects References
USP8 9-Ethyloxyimino-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile Non-small cell lung cancer Downregulation of receptor tyrosine kinases including EGFR, ERBB2, ERBB3, and MET [160]
UCHL1 LDN-57444 Lung cancer cell line Inhibit proliferation [161]
UCHL1, UCHL3 TCID Multiple myeloma Induce apoptosis [162]
USP1 Pimozide Leukemic cell lines Promoted the degradation of ID1 [163]
USP1-UAF1 ML323 Non-small cell lung cancer and osteosarcoma cells Induced DNA damage [164]
USP1-UAF1 Pimozide and GW7647 Non–small cell lung cancer Inhibit cell proliferation [165]
USP2 ML346 Colorectal cancer nad mantle cell lymphoma Accelerate cyclin D1 degradation, cell cycle arrest [166]
USP2a/USP2b/USP5/USP8 AM146, RA-9 and RA-14 Breast, ovarian and cervical cancer cell lines Downregulation cell-cycle promoter, and upregulation of tumor suppressor [167]
USP5/IsoT, USP4 Vialinin A Basophilic leukemia cells Inhibit the release of TNFα [168]
USP7 HBX 41,108 Colorectal carcinoma Induced p53-dependent apoptosis [156]
USP7/USP47 P5091 and Compound 1 Multiple myeloma Induce apoptosis, inhibit tumor growth [169,170]
USP9X/USP5/USP24 WP1130 Mantle cell lymphoma Downregulation of antiapoptotic and upregulation of proapoptotic proteins, such as MCL-1 and p53 [171,172]
USP14/ UCHL5 AC17 Human lung cancer cells Inhibit NFκB pathway and reactive p53 [173]
USP14/UCHL5 b-AP15 (WO2013058691) Multiple myeloma/ colorectal carcinoma Downregulation of CDC25C, CDC2, and cyclin B1/ overexpression of the anti-apoptotic mediator Bcl-2 and anti-tumor activity [162,174]
USP14/UCHL5 VLX1570 Colon carcinoma cell Inhibit proteasome DUB activity [175]