Table1.

DUB inhibitors developed for cancer treatment

DUB	Target	Inhibitor	Functions affected by the inhibitor	Cancer type	Stage	Refs.
USP1	PCNA and FANCD2	Pimozide	Synthetic lethal with cisplatin	NSCLC	Preclinical	[111]
	PCNA and FANCD2	GW7647	Synthetic lethal with cisplatin	NSCLC	Preclinical	[111]
	ID1	C527	Growth inhibition	multiple myeloma	Preclinical	[112]
	ID proteins	SJB3-019A	Inhibition of DNA Repair and triggering apoptosis	multiple myeloma and B-ALL	Preclinical	[85, 86]
	PCNA,FANCD2 and KPNA2	ML323	DNA damage and suppression of metastasis	Osteosarcoma, NSCLC and breast cancer	Preclinical	[79, 83]
USP2	cyclin D1	ML364	Cell cycle arrest	CRC and Mantle Cell Lymphoma	Preclinical	[90]
	cyclin D1	LCAHA	G0/G1 arrest	CRC	Preclinical	[89]
	FASN, MDM2, cyclin D1 and Aurora-A	6TG	Cell killing and drug resistance	BRCA2 defective tumours	Preclinical	[113–115]
USP7	MDM2	HBX41108	Inhibition of Cell Proliferation	CRC	Preclinical	[116]
	SYK	HBX19818	Cell death	AML	Preclinical	[117]
	PLK1,Maf and N-MYC	P5091	Cell cycle and cell death	Multiple cancers	Preclinical	[94, 118–120]
	MDM2	GNE6640/6776	Synergy with PIM kinase inhibition	Breast cancer and Osteosarcoma	Preclinical	[121]
	MDM2	FT671/827	Inhibition of tumor growth	Osteosarcoma and CRC	Preclinical	[122]
	MDM2/MDM4	XL188	Cell death	Ewing sarcoma	Preclinical	[123, 124]
USP7/USP47	N-MYC, YB-1 et al	P22077	Drug resistance	Multiple cancers	Preclinical	[99–101, 125–128]
USP9X	Not reported	Degrasyn	Gemcitabine resistance	Pancreatic cancer	Preclinical	[129]
USP14	AR proteins	IU1	Inhibition of proliferation	Breast cancer	Preclinical	[130]
USP14/UCHL5	CXCR4	VLX1570	ER Stress	Multiple myeloma, ALL	Preclinical	[104, 106, 131]
	Proteasome	Auranofin	Apoptosis	Multiple cancers	Phase II	[108, 109]
UCHL1	TβRI and SMAD2	6RK73	Inhibition of migration and extravasation	Breast cancer	Preclinical	[132]
CSN5	Cullin-RING E3 ubiquitin ligases	CSN5i-3	Inhibition of tumor growth	Large cell lymphoma and CRC	Preclinical	[133]
RPN11	Proteins at the 19S proteasome entry gate	O-phenanthroline	Apoptosis	Multiple myeloma	Preclinical	[134]
	Proteins at the 19S proteasome entry gate	Quinoline-8-thiol	ER stress	CRC	Preclinical	[110]
Pan DUBs	Global protein stability	PR-619	ER stress, G2/M cell cycle arrest and apoptosis	Multiple cancers	Preclinical	[126, 135, 136]