Drugs interfering with cholesterol and CE synthesis and LXR activity. (A) Drugs interfering with cholesterol and CE synthesis. Statins block both cholesterol synthesis and isoprenoid formation (green), whereas ZAA blocks cholesterol synthesis, leaving intact isoprenoid formation (green). Avasimibe blocks formation of CEs by inhibiting the ACAT-1. HDL-NPs promote cellular cholesterol efflux and restrain cholesterol delivery by targeting scavenger receptor type B-1. (B) LXRs can be inhibited by sulfate oxysterols through the activity of sulfotransferase 2B1b (SULT2B1b) enzyme and by the inverse agonist SR9243. LXRs are activated by oxysterols generated through the activity of cholesterol hydroxylases (eg, ch25h, Cyp27a1, Cyp46a1) or auto-oxidation and by LXRβ-selective (RGX-104) and nonselective LXR agonists (T0901317, GW3965, DDA).