PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 16190729-6 2005 In addition to the direct coordination of metyrapone to the heme iron, the hydrogen bond interaction between the inhibitor carbonyl group and the side chain of Ser119 also contributes significantly to stabilizing the CYP3A4-metyrapone complex. Metyrapone 224-234 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 217-223 22113809-9 2012 From the theozyme analysis of the X-ray structures for ketoconazole- and metyrapone-CYP3A4 complexes, the interaction free energy of the neighboring residues with each inhibitor in the active site is calculated to be about -3 kcal mol(-1) in water, whose the interaction energy and the desolvation free energy change are about -5 and 2 kcal mol(-1) , respectively. Metyrapone 73-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-90 19414330-5 2009 RESULTS: Three ligand accessible regions (region 1-3) were present in erythromycin-bound CYP3A4, and these dipole moments indicated the same features as ketoconazole- or metyrapone-bound CYP3A4 molecules. Metyrapone 170-180 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 19414330-5 2009 RESULTS: Three ligand accessible regions (region 1-3) were present in erythromycin-bound CYP3A4, and these dipole moments indicated the same features as ketoconazole- or metyrapone-bound CYP3A4 molecules. Metyrapone 170-180 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 187-193 16713641-5 2006 We used real time PCR to examine whether known and suspected CYP3A inducers (dexamethasone, metyrapone, rifampicin, and toxaphene) up-regulate steady state levels of hepatic CYP3A77 transcript to determine if induction patterns in female juvenile alligators are similar to those reported in other vertebrates and whether toxaphene, an organochlorine compound found in high concentrations in Lake Apopka alligators, induces this gene. Metyrapone 92-102 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 61-66 30676743-2 2019 This study investigated the interaction of recombinant CYP3A4 with a nonspecific inhibitor metyrapone, antifungal drug fluconazole, and protease inhibitor phenylmethanesulfonyl fluoride (PMSF). Metyrapone 91-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-61 30676743-3 2019 Metyrapone and fluconazole are classic type II ligands that inhibit CYP3A4 with medium strength by ligating to the heme iron, whereas PMSF, lacking the heme-ligating moiety, acts as a weak type I ligand and inhibitor of CYP3A4. Metyrapone 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-74 30676743-3 2019 Metyrapone and fluconazole are classic type II ligands that inhibit CYP3A4 with medium strength by ligating to the heme iron, whereas PMSF, lacking the heme-ligating moiety, acts as a weak type I ligand and inhibitor of CYP3A4. Metyrapone 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 220-226 19727863-7 2010 F215 and F220 are known as entrance blockers of channel-2 in metyrapone-bound CYP3A4. Metyrapone 61-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-84 17520814-5 2007 The metabolism of Z- and E-ajoenes in Caco-2 cell monolayers can be partially inhibited by vitamin C as an anti-oxidant, metyrapone as an inhibitor to subtype CYP3A of cytochrome P450 drug metabolism enzymes, and sodium azide as an inhibitor to ATP production. Metyrapone 121-131 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 159-164 15256616-0 2004 Crystal structures of human cytochrome P450 3A4 bound to metyrapone and progesterone. Metyrapone 57-67 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 28-47 15256616-4 2004 Here we report three crystal structures of CYP3A4: unliganded, bound to the inhibitor metyrapone, and bound to the substrate progesterone. Metyrapone 86-96 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-49 10611146-0 2000 Effect of the adrenal 11-beta-hydroxylase inhibitor metyrapone on human hepatic cytochrome P-450 expression: induction of cytochrome P-450 3A4. Metyrapone 52-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 122-142 15100175-8 2004 Finally, the role of these sites was examined in activation of CYP3A4 expression by rifampicin, metyrapone, clotrimazole, and phenobarbital. Metyrapone 96-106 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-69 10611146-4 2000 Addition of metyrapone to human hepatocyte cultures resulted in the induction of CYP3A4 expression. Metyrapone 12-22 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-87 10611146-5 2000 The pregnane X receptor (PXR), which has recently been shown to mediate the transcriptional induction of CYP3A4 expression in response to rifampicin, was activated by metyrapone in CV-1 cells transiently cotransfected with an expression vector encoding the human PXR and a reporter construct containing the everted repeat sequence that confers CYP3A4 induction responsiveness to inducers within its promoter. Metyrapone 167-177 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 105-111 10611146-5 2000 The pregnane X receptor (PXR), which has recently been shown to mediate the transcriptional induction of CYP3A4 expression in response to rifampicin, was activated by metyrapone in CV-1 cells transiently cotransfected with an expression vector encoding the human PXR and a reporter construct containing the everted repeat sequence that confers CYP3A4 induction responsiveness to inducers within its promoter. Metyrapone 167-177 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 344-350 10611146-6 2000 Metyrapone activated the human PXR at concentrations that also resulted in the induction of CYP3A4 in human cultured hepatocytes. Metyrapone 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 92-98 10611146-7 2000 Metyrapone treatment is therefore unlikely to result in the induction of CYP1A1 but may induce the expression of CYP3A4 in humans. Metyrapone 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 113-119 10917608-0 1999 The cytochrome P450 3A4 inducer metyrapone is an activator of the human pregnane X receptor. Metyrapone 32-42 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-23 10219967-11 1999 Metyrapone and sulfinpyrazone induced CYP3A4-dependent reporter gene expression, but induction was not enhanced by the glucocorticoid receptor. Metyrapone 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-44