How cancer cells remodel lipid metabolism: strategies targeting transcription factors

Jeong, Do-Won; Lee, Seulbee; Chun, Yang-Sook

doi:10.1186/s12944-021-01593-8

Lipids in Health and Disease

Table 2 List of lipid-related drugs

From: How cancer cells remodel lipid metabolism: strategies targeting transcription factors

Target	Drug	Phase of development	Cancer type	Reference
FXR	GW4064	Preclinical	Eesophagus, liver and pancreatic cancer	[106,107,108,109]
FXR	Guggulsterone	Preclinical	Liver and pancreatic cancer	[106, 107]
LXR	GW3965	Preclinical	Glioblastoma	[74]
	LXR-623	Phase I	Glioblastoma	[110]
	SR9243	Preclinical	Colon cancer	[77]
	T0901317	Preclinical	Prostate cancer	[75]
PPARα	Fenofibrate	Preclinical	Breast, oral and prostate cancer, Melanoma	[111,112,113,114]
PPARα	Wy-14,643	Preclinical	Breast, colon, lung and liver cancer	[89, 115]
PPARβ/δ	SR13904	Preclinical	Lung cancer	[117]
PPARβ/δ	GW0742	Preclinical	Melanoma	[118, 119]
PPARγ	Thiazolidinedione	Phase III	Colon, pancreatic, liver and breast cancer, Liposarcoma	[121,122,123,124,125,126]
PPARγ	GW9662	Clinical	Bladder cancer	[128]
SREBPs	Sibilinin	Preclinical	Breast, head and neck, lung, and prostate cancer	[131,132,133,134,135]
	Betulin	Preclinical	HCC	[103]
	Fatostatin	Preclinical	Glioblastoma, osteosarcoma, breast and prostate cancer	[104, 136, 137]
	Compound 24	Preclinical	Glioblastoma	[105]
S1P/S2P	Nelfinavir	Phase II	Glioblastoma, liposarcoma, myeloma, lung, pancreatic, and prostate cancer	[139, 140, 175]
FAS	TVB-2640	Phase II	Lung, ovarian and breast cancer	[141]
	C75	Preclinical	Breast, colon, ovarian, and prostate cancer	[142, 144, 145, 176]
	Cerulenin	Preclinical	Colon and ovarian cancer	[143, 144]
	Orlistat	Approved for anti-obesity	Breast, colon and prostate cancer	[145, 146]
ACC	Soraphen A	Preclinical	Prostate cancer	[147]
	ND-646	Preclinical	Lung cancer	[148]
	TOFA	Preclinical	Breast, colon, lung, and prostate cancer	[149,150,151]
SCD	A939572	Preclinical	Clear cell renal cell carcinoma, Lung cancer	[152, 153]
SCD	CAY10566	Preclinical	Colon and ovarian cancer, glioblastoma, melanoma, HCC	[154,155,156,157]
HMGCR	Statin	Approved	Many cancers	[158,159,160,161,162,163, 165, 166]
HMGCR	Simvastatin	Preclinical	Prostate cancer	[164]
CD36	ABT-510	Phase I	Glioblastoma, melanoma and renal cell carcinoma	[167,168,169]
FABP5	dmrFABP5	Preclinical	Prostate cancer	[172]
	SBFI-102 and SBFI-103	Preclinical	Prostate cancer	[173]
	EI-05	Preclinical	Breast cancer	[174]

FXR Farnesoid X receptor; SREBP Sterol regulatory element-binding protein; S1P site-1 protease; LXR Liver X receptor; ChREBP Carbohydrate-response element-binding protein; PPARs Peroxisome proliferator-activated receptor; FASN Fatty acid synthase; ACC Acetyl-coenzyme A carboxylase; SCD Stearoyl-CoA desaturase; HCC Hepatocellular carcinoma; HMGCR β-Hydroxy β-methylglutaryl-CoA reductase

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ISSN: 1476-511X

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