Table 1.

Effects of drugs interfering with cholesterol homeostasis on tumor and tumor-infiltrating immune cells

DrugTargetActivity on tumor cellsActivity on immune cells
Statins (mevastatin, lovastatin, atorvastatin, fluvastatin, rosuvastatin, simvastatin) HMGCR, Isoprenoid formation Apoptosis of leukemic cells (AML) and myeloma cells (MM) Blocking Rab5 prenylation leading to prolonged Ag presentation 
ZAA Squalene synthase Apoptosis of leukemic cells (AML) Increase CD11c+ DC activity, decrease of protumor neutrophils 
T0901317 LXR agonist Apoptosis of leukemic cells (CLL and BPDCN)  
GW3965 LXR agonist Apoptosis of BPDCN cells Expression of NK cell-activating ligands MICA and MICB and suppression of MDSCs 
DDA LXR partial agonist Lethal autophagy of leukemic cells (AML) Increased infiltration of CD3+ T cells and CD11c+ DCs 
Avasimibe ACAT-1 inhibitor Suppression of leukemic cell proliferation (CML) Enhanced TCR clustering and immunological synapse of CD8+ T cells 
HDL-NP Scavenger receptor type B-1 Apoptosis of DLBCL cells  
SR9243 LXR inverse agonist Apoptosis of tumor cells Increased CD11c+ DC and CD8+ T-cell activity 
RGX-104 LXRβ agonist  Suppression of MDSCs 
SULT2B1b LXR antagonist  Increased CD11c+ DC activity, decrease in protumor neutrophils 
DrugTargetActivity on tumor cellsActivity on immune cells
Statins (mevastatin, lovastatin, atorvastatin, fluvastatin, rosuvastatin, simvastatin) HMGCR, Isoprenoid formation Apoptosis of leukemic cells (AML) and myeloma cells (MM) Blocking Rab5 prenylation leading to prolonged Ag presentation 
ZAA Squalene synthase Apoptosis of leukemic cells (AML) Increase CD11c+ DC activity, decrease of protumor neutrophils 
T0901317 LXR agonist Apoptosis of leukemic cells (CLL and BPDCN)  
GW3965 LXR agonist Apoptosis of BPDCN cells Expression of NK cell-activating ligands MICA and MICB and suppression of MDSCs 
DDA LXR partial agonist Lethal autophagy of leukemic cells (AML) Increased infiltration of CD3+ T cells and CD11c+ DCs 
Avasimibe ACAT-1 inhibitor Suppression of leukemic cell proliferation (CML) Enhanced TCR clustering and immunological synapse of CD8+ T cells 
HDL-NP Scavenger receptor type B-1 Apoptosis of DLBCL cells  
SR9243 LXR inverse agonist Apoptosis of tumor cells Increased CD11c+ DC and CD8+ T-cell activity 
RGX-104 LXRβ agonist  Suppression of MDSCs 
SULT2B1b LXR antagonist  Increased CD11c+ DC activity, decrease in protumor neutrophils 

Ag, antigen; MDSC, myeloid-derived suppressor cell.

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