11) Terbinafine inhibits squalene epoxidase
, an enzyme involved in the synthesis of ergosterol, which gives terbinafine both fungicidal and fungistatic activity.
as hypocholesterolemic drug target revisited.
Certain of these theaflavins have exhibited potent inhibition of the enzyme squalene epoxidase
, a key enzyme involved in the body's synthesis of cholesterol.
Fungicide; inhibits squalene epoxidase
, which decreases ergosterol synthesis and causes fungal cell death.
A number of enzymes, including [Beta]-lactamases, carboxypeptidases, and squalene epoxidase
, are under current study to develop inhibitors which may be useful medicinal agents and to gain insights into mechanisms of catalysis.
20) Terbinafine is thought to have fungicidal activity (21) by inhibiting squalene epoxidase, thereby causing cytotoxic accumulation of intracellular squalene.
Allylamine derivatives: new class of synthetic antifungal agents inhibiting fungal squalene epoxidase.
Cyp1b1 was best predicted by spleen tyrosine kinase (31%), squalene epoxidase
(16%), and nicotinamide adenine dinucleotide (NADH) dehydrogenase (Ndufc1) (14%).
mitochondrial CPT1, acyl-CoA thioester hydrolase, 3-hydroxy-3-methylglutamyl-CoA (HMG-CoA) reductase, squalene epoxidase
, farnesyl diphosphate (FPP)-transferase, FPP-synthase were upregulated, while acyl-CoA desaturase, acyl-CoA synthetase, and acyl-CoA oxidase 2 were downregulated) (Ratra et al 1998b).
Treatment with CPCA also resulted in regulation of a number of genes in the cholesterol and fatty acid pathways, including an upregulation of adipocyte lipid binding protein, squalene epoxidase, 7-dehydrocholesterol reductase, and downregulation of cholesterol hydroxylase 7 [alpha], lecithin-cholesterol acyltransferase, fatty acid desaturase, fatty acid amide hydrolase, and fatty acid binding proteins 1 and 7 (Table 3).
Accession number (a) Gene E00717 CYP1A1 NM_012940 CYP1B1 NM_012600 Malic enzyme NM_017014 Glutathione-S-transferase D83796 UDP-Glucuronosyltransferase 1 U36482 Erp29 AA964229 Tricarboxylate carrier J05030 Acyl-CoA dehydrogenase D16478 Enoyl-CoA hydratase K03249 Peroxisomal bifunctional enzyme J02749 Acetyl-CoA acyltransferase, 3-Oxo-acyl-CoA thiolase A, peroxisomal AI105060 Adipocyte lipid binding protein D37920 Squalene epoxidase AB016800 7-Dehydrocholesterol reductase J05509 Cholesterol hydroxylase 7 [alpha] NM_017024 Lecithin-cholesterol acyltransferase AB021980 Fatty acid desaturase NM_024132 Fatty acid amide hydrolase NM_012556 Fatty acid binding protein 1 NM_030832 Fatty acid binding protein 7 AW534367 Prohepcidin Cluster Accession number (a) Aroclor 1254 3-MC CPCA (Fig.