Table 1.
Representative targets within the lipid metabolism pathway for anti-cancer drug development
| Target protein | Inhibitor | Type of cancer | Preclinical model | Clinical trial | References |
|---|---|---|---|---|---|
| SCAP | – | GBM | Xenografts | – | [55] |
| SREBPs | Fatostatin, betulin, PF-429242, xanthohumol | GBM, prostate, liver, skin, melanoma, colorectal, bile duct, pancreatic, and breast cancer | Xenografts | – | [28, 125–138] |
| ACCs | TOFA, soraphen A, ND-646 | Lung, ovarian cancer, head and neck squamous cell carcinoma | Xenografts | – | [179–185] |
| ACLY | SB-204990, bempedoic acid, BMS303141 | Lung, prostate, and ovarian cancer | Xenografts | – | [152, 162, 165] |
| FASN | Cerulenin | Ovarian cancer, breast cancer | Xenografts | – | [179, 194–196] |
| C75 | Breast, GBM, renal, and mesothelioma cancer | Xenografts | – | [34, 179, 188, 197–203] | |
| TVB-2640 | Solid malignant tumors | – | Phase I | Clinicaltrials.gov (NCT02223247), [191] | |
| TVB-3166 | Lung, ovary, and pancreatic cancer | Xenografts | – | [264] | |
| C93 | Ovarian and lung cancer | Xenografts | – | [265, 266] | |
| C247 | Breast cancer | – | [267] | ||
| Orlistat | Prostate cancer and melanoma | Xenografts | – | [192, 193] | |
| Triclosan | Breast cancer | Xenografts | – | [268, 269] | |
| LDLR | – | GBM | – | – | [27, 219] |
| SCD1 | BZ36, A939572, MF-438 | Prostate, renal cancer | Xenografts | – | [124, 212–215, 270] |
| LXR | GW3965, LXR-623 | GBM | Xenografts | – | [27, 238, 239] |
| SR9243 | Prostate cancer | Xenografts | [242] | ||
| SOAT1 (or ACAT1) | K604, ATR-101, avasimibe | GBM, prostate and pancreatic cancer | Xenografts | – | [28, 230–232] |
| CPT1 | Etomoxir, perhexiline | Leukemia, prostate and breast cancer | Xenografts, transgenic mice | – | [248–250, 271, 272] |
| CD36 | Anti-CD36 antibodies | Oral cancer | Xenografts | – | [24–26] |
ACCs acetyl-CoA carboxylases, ACLY ATP citrate lyase, CD36 cluster of differentiation 36, also known as fatty acid translocase (FAT), CPT1 carnitine palmitoyltransferase 1, FASN fatty acid synthase, GBM glioblastoma multiforme, LDLR low-density lipoprotein receptor, LXR liver X receptor, SCAP SREBP cleavage-activating protein, SREBPs sterol regulatory element-binding proteins