The emerging role of deubiquitylating enzymes as therapeutic targets in cancer metabolism

Tu, Rongfu; Ma, Junpeng; Zhang, Peng; Kang, Ye; Xiong, Xiaofan; Zhu, Junsheng; Li, Miao; Zhang, Chengsheng

doi:10.1186/s12935-022-02524-y

Cancer Cell International

Table1 DUB inhibitors developed for cancer treatment

From: The emerging role of deubiquitylating enzymes as therapeutic targets in cancer metabolism

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	[113,114,115]
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, 118,119,120]
	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	[99,100,101, 125,126,127,128]
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]
USP14/UCHL5	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]
RPN11	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]

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ISSN: 1475-2867

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