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. 2022 Mar 14;13(6):1745–1757. doi: 10.7150/jca.63609

Table 1.

New approaches that target cholesterol metabolism in GBM

Drugs Targets Mechanisms References
PF-429242
Quercetin, phytol, retinol
MicroRNA-132
MicroRNA -29
S1P
SREBP-1
SIRT1
SREBP-1/SCAP
Inhibit lipid and cholesterol synthesis 19-23
Avasimibe
K604
L365260, YM022
SOAT1 Inhibit the cholesterol esterification, apoptotsis, inhibit Akt signaling 24,26,30,31
LXR-623, GW3965
4-7rr, 4-13,4-13rr
Efavirenz
MI-2
LXRs
LXRβ
CYP46A1
LSS
Reduce the uptake of cholesterol and promote cholesterol efflux 33,34,37,39
Pregnenolone Bcl-2, Fas/FasL Activate the extrinsic and intrinsic apoptotic pathways 49
Loperamide, pimozide
Archazolid B
Itraconazole
SMPD1
NPC1
SCP2
Disrupt the cellular cholesterol trafficking 67,68,71
i6A derivatives, CM223, ZOL FDPS Activate γδ T cells, inhibit EGFR and Akt/STAT3 signaling 77,78,82
Statins HMGCR
iGluRs
mGluRs
p38 MAPK pathway
Inhibit ERK1/2 and Akt signaling, Destroy cell membrane lipid rafts,
Apoptosis, inhibit the MT1-MMP expression, Block the fusion of autophagosomes and lysosomes
52,66,83-87

iGluRs: ionotropic glutamate receptors, mGluRs: metabotropic glutamate receptors. B cell lymphoma-2: Bcl-2, Fas: FS7-associated cell surface antigen, FasL: FS7-associated cell surface antigen ligand, LSS: Lanosterol synthase, MT1-MMP: Membrane-type 1 matrix metalloproteinase, CYP46A1: cytochrome P450 46A1, SMPD1: sphingomyelin phosphodiesterase 1.