Table 1.

Targeting lipid metabolism with small-molecule agents to modulate cancer cell death.

Target	Reagents	Drug development stage	Effects	Mechanisms	Cancer types	References
HMGCR	Statins	Pre-clinical and clinical	Cholesterol synthesis↓, Apoptosis↑	Mevalonate pathway↓	Glioma, lung cancer	[44,148,149,157,178]
LXR	GW3965	Pre-clinical	Cholesterol efflux↑, cell death↑	LDLR degradation, ABCA1↑	Glioblastoma, pancreatic cancer and ccRCC	[8,150,151]
	T0901317	Pre-clinical	Apoptosis↑	AKT↓, caspase-3↑	Melanoma, prostate cancer	[8,[150], [151], [152], [153]]
	LXR623	Pre-clinical	Cholesterol↓, apoptosis↑	LDLR↓, ABCA1↑	ccRCC	[[151], [152], [153]]
	SR9243	Pre-clinical	Apoptosis↑	SREBP-1c, FASN, SCD1↓	ccRCC	[151]
SOAT1	Avasimibe	Pre-clinical	Fatty acid production and LDL uptake↓, apoptosis↑	SREBP1↓	Prostate cancer, glioblastoma, pancreatic cancer, liver cancer	[44,151,157,178]
FASN	TVB-3166	Pre-clinical	Lipid biosynthesis↓, apoptosis↑	PI3K-AKT-mTOR, β-catenin, c-Myc↓	Non-small cell lung cancer	[51]
ACC	ND-654	Pre-clinical	Lipogenesis↓, apoptosis↑	ACC phosphorylation↓	Liver cancer	[160]
–	Valproic acid	Pre-clinical	Lipogenesis↓, apoptosis↑	CEBPα/SREBP-1 pathway↓	Prostate cancer	[161]
–	CPI-613	Pre-clinical	Lipid metabolism↓, autophagy, apoptosis ↑	AMPK-ACC signaling↑	Pancreatic cancer	[162]
–	VD3+ T0901317		Cholesterol accumulation↓, apoptosis↑	ABCA1-CHOP-BCL-2↑	Breast cancer	[154]
CPT-1	CTPi + PMCTi	Pre-clinical	Fatty acid production↓, mitochondrial-dependent apoptosis↑	/	Liver cancer	[163]

↓: Downregulation; ↑: Upregulation; -: Not determined.