PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 30425102-0 2019 Structure of human cortisol-producing cytochrome P450 11B1 bound to the breast cancer drug fadrozole provides insights for drug design. Fadrozole 91-100 cytochrome P450 family 11 subfamily B member 1 Homo sapiens 38-58 30425102-4 2019 Here we report the X-ray crystal structure of human CYP11B1 (at 2.1 A resolution) in complex with fadrozole, a racemic compound normally used to treat breast cancer by inhibiting estrogen-producing CYP19A1. Fadrozole 98-107 cytochrome P450 family 11 subfamily B member 1 Homo sapiens 52-59 30425102-5 2019 Comparison of fadrozole-bound CYP11B1 with fadrozole-bound CYP11B2 revealed that despite conservation of the active-site residues, the overall structures and active sites had structural rearrangements consistent with distinct protein functions and inhibition. Fadrozole 14-23 cytochrome P450 family 11 subfamily B member 1 Homo sapiens 30-37 30425102-6 2019 Whereas fadrozole binds to both CYP11B enzymes by coordinating the heme iron, CYP11B2 binds to the R enantiomer of fadrozole, and CYP11B1 binds to the S enantiomer, each with distinct orientations and interactions. Fadrozole 8-17 cytochrome P450 family 11 subfamily B member 1 Homo sapiens 32-38 28759940-6 2017 Higher concentrations of FAD286 did not further reduce aldosterone concentrations, but showed a parallel reduction in corticosterone, cortisol and cortisone levels, reflecting additional inhibition of steroid-11beta-hydroxylase (CYP11B1). Fadrozole 25-31 cytochrome P450 family 11 subfamily B member 1 Homo sapiens 201-227 28759940-6 2017 Higher concentrations of FAD286 did not further reduce aldosterone concentrations, but showed a parallel reduction in corticosterone, cortisol and cortisone levels, reflecting additional inhibition of steroid-11beta-hydroxylase (CYP11B1). Fadrozole 25-31 cytochrome P450 family 11 subfamily B member 1 Homo sapiens 229-236 19622340-8 2009 FAD286, a reference CYP11B2 inhibitor, inhibited CYP11B2 and CYP11B1 activities with IC(50) values of 1.6+/-0.1 and 9.9+/-0.9 nM (mean+/-SEM, n=3-6), respectively. Fadrozole 0-6 cytochrome P450 family 11 subfamily B member 1 Homo sapiens 61-68 24899257-6 2014 Among them, compounds 14 and 23 showed good selectivity over the highly homologous CYP11B1, with selectivity factors (SF = IC50 CYP11B1/IC50 CYP11B2) around 170; thus, they are superior to fadrozole and LCI699 (SFs < 15). Fadrozole 189-198 cytochrome P450 family 11 subfamily B member 1 Homo sapiens 83-90 34247511-9 2021 LCI699 binding was compared with that of its analog fadrozole to both CYP11B enzymes. Fadrozole 52-61 cytochrome P450 family 11 subfamily B member 1 Homo sapiens 70-76 15985365-5 2005 Fadrozole and compounds 6, 9 and 10 were more potent towards CYP11B2 compared to CYP11B1 with IC(50) values in the nanomolar range. Fadrozole 0-9 cytochrome P450 family 11 subfamily B member 1 Homo sapiens 81-88