Cytochrome P450 family 51 subfamily A member 1 (CYP51A1) (CYP51A1)

Cytochrome P450 family 51 subfamily A member 1 (CYP51A1), also known as lanosterol 14-alpha demethylase, is a highly conserved enzyme essential for the biosynthesis of cholesterol in humans [3, 9]. It catalyzes the oxidative removal of the 14-alpha-methyl group from lanosterol, a critical rate-limiting step in the sterol pathway [1, 6]. While it is the primary target for azole antifungal medications in pathogens, human CYP51A1 is a significant off-target for these drugs and is being investigated as a primary target for cholesterol-lowering and anti-cancer therapies [1, 4, 8]. Beyond its role in lipid metabolism, CYP51A1 is involved in regulating various forms of programmed cell death, such as apoptosis and ferroptosis, and its activity is often upregulated in tumors to support cell proliferation [2, 6]. Mutations in the CYP51A1 gene are linked to developmental disorders like Antley-Bixler syndrome and have been implicated in pregnancy-related pathologies [2, 7]. Therapeutic agents targeting this enzyme typically function by binding to its heme-containing active site, which inhibits catalytic activity and leads to the accumulation of sterol intermediates [4, 5]. Understanding the dual role of CYP51A1 in metabolism and cell signaling is crucial for developing selective inhibitors that minimize off-target toxicity while maximizing therapeutic efficacy [2, 8].

Other names

Lanosterol 14-alpha demethylaseLDMCP51CYP51CYPL1P450L1P450-14DMSterol 14-alpha demethylase