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Table 1 Representative targets within the lipid metabolism pathway for anti-cancer drug development

From: Lipid metabolism reprogramming and its potential targets in cancer

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, 125,126,127,128,129,130,131,132,133,134,135,136,137,138]
ACCs TOFA, soraphen A, ND-646 Lung, ovarian cancer, head and neck squamous cell carcinoma Xenografts [179,180,181,182,183,184,185]
ACLY SB-204990, bempedoic acid, BMS303141 Lung, prostate, and ovarian cancer Xenografts [152, 162, 165]
FASN Cerulenin Ovarian cancer, breast cancer Xenografts [179, 194,195,196]
  C75 Breast, GBM, renal, and mesothelioma cancer Xenografts [34, 179, 188, 197,198,199,200,201,202,203]
  TVB-2640 Solid malignant tumors Phase I (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, 212,213,214,215, 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, 230,231,232]
CPT1 Etomoxir, perhexiline Leukemia, prostate and breast cancer Xenografts, transgenic mice [248,249,250, 271, 272]
CD36 Anti-CD36 antibodies Oral cancer Xenografts [24,25,26]
  1. 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