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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

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, 212,213,214,215, 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