PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 30390556-0 2019 Study on the inhibitory effect of furafylline and troleandomycin in the 7-methoxyresorufin-O-demethylase and nifedipine oxidase activities in hepatic microsomes from four poultry species using high-performance liquid chromatography coupled with fluorescence and ultraviolet detection. Troleandomycin 50-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 109-127 30390556-1 2019 The present study reports the in vitro studies with furafylline and troleandomycin (TAO) as specific inhibitors of activities 7-methoxyresorufin-O-demethylase (MROD) and nifedipine oxidase, catalyzed by cytochrome P450 1 A2 (CYP1 A2) and 3A4 human enzymes, respectively, in hepatic microsomes of quail, duck, turkey and chicken. Troleandomycin 68-82 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 170-188 29785610-10 2018 Troleandomycin and verapamil displayed quasi-irreversible MDI of CYP3A4; MIC formation was observed, while no formation of CYP-dependent GSH adducts occurred. Troleandomycin 0-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 65-71 26970587-8 2016 Addition of CYP3A family-specific inhibitors, troleandomycin and azamulin, almost completely inhibited production of 20,24R(OH)2D3, 20,24S(OH)2D3 and 20,25(OH)2D3 by human liver microsomes, further supporting that CYP3A4 plays the major role in 20(OH)D3 metabolism by microsomes. Troleandomycin 46-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 214-220 19307295-2 2009 Over half of the compounds tested (14 of 24) were identified as time-dependent inhibitors of CYP3A4 and high mRNA/activity ratios (>10) were consistent with CYP3A4 time-dependent inhibition for compounds such as troleandomycin, ritonavir, and verapamil. Troleandomycin 215-229 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-99 24889073-5 2014 The predominant role of CYP3A4 was further supported by a dramatic inhibition of metabolite formation in the presence of the CYP3A4 substrates troleandomycin and ketoconazole. Troleandomycin 143-157 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 24-30 24889073-5 2014 The predominant role of CYP3A4 was further supported by a dramatic inhibition of metabolite formation in the presence of the CYP3A4 substrates troleandomycin and ketoconazole. Troleandomycin 143-157 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-131 24335510-8 2014 Ketoconazole and troleandomycin showed similar inhibitory potencies toward c3A4 and h3A4, whereas non-h3A4 inhibitors did not inhibit c3A4 activity. Troleandomycin 17-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-79 21622627-11 2011 CYP3A4 was important for enniatin B metabolism in human microsomes as shown by 80% inhibition and impaired metabolite formation in the presence of troleandomycin. Troleandomycin 147-161 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 21576599-7 2011 Furthermore, treatment of the cells with troleandomycin, a specific inhibitor of CYP3A, significantly reduced cellular 25-hydroxycholesterol concentrations. Troleandomycin 41-55 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-86 20876785-7 2011 Among a panel of 10 chemical inhibitors tested, only ketoconazole and troleandomycin (CYP3A-specific chemical inhibitors) significantly inhibited the formation of MII by 45 and 95%, respectively. Troleandomycin 70-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-91 19616568-10 2009 This was further confirmed by significant inhibition of primaquine hemotoxicity by the selective CYP inhibitors, namely thiotepa (CYP2B6), fluoxetine (CYP2D6) and troleandomycin (CYP3A4). Troleandomycin 163-177 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 179-185 19307295-2 2009 Over half of the compounds tested (14 of 24) were identified as time-dependent inhibitors of CYP3A4 and high mRNA/activity ratios (>10) were consistent with CYP3A4 time-dependent inhibition for compounds such as troleandomycin, ritonavir, and verapamil. Troleandomycin 215-229 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 160-166 19293388-7 2009 Human CYP3A inhibitors erythromycin (0.5 mM), ketoconazole (0.5 microM), and troleandomycin (0.01-1 mM), but not the CYP2C inhibitor, sulfaphenazole (3 microM), significantly inhibited the depletion of NFV in hepatic S-9 fractions and expressed rhesus CYP3A64 enzyme. Troleandomycin 77-91 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 6-11 19149415-5 2008 Triacetyloleandomycin, a specific inhibitor of human CYP3A4, inhibited the metabolism of lovastatin in pig and human liver microsomes. Troleandomycin 0-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-59 18505790-6 2008 CYP3A4 activity was significantly increased by rifampin (9.7-fold), nafcillin and dicloxacillin (5.9-fold), and weakly induced (2-fold) by tetracycline, sufisoxazole, troleandomycin, and clindamycin. Troleandomycin 167-181 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 18573861-8 2008 Metabolism of 17-OHPC was significantly inhibited by the CYP3A4 inhibitors ketoconazole and troleandomycin in HLM and FHH. Troleandomycin 92-106 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-63 16679385-6 2006 Tienilic acid selectively inhibited CYP2C9-dependent diclofenac 4"-hydroxylation activity, and erythromycin, troleandomycin, and fluoxetine inhibited CYP3A4-dependent midazolam 1"-hydroxylation in a time- and concentration-dependent manner. Troleandomycin 109-123 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 150-156 17207564-6 2007 Further, CYP3A4/7 inhibitor triacetyloleandomycin did not prevent, but rather potentiated, alachlor cytotoxicity. Troleandomycin 28-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 9-15 15557344-7 2005 CYP3A4 and 3A5 were equipotently inhibited by troleandomycin, whereas ketoconazole was an order of magnitude more potent toward CYP3A4. Troleandomycin 46-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 15764719-5 2005 Moreover, ketoconazole and troleandomycin, specific inhibitors of CYP3A4 metabolism, demonstrated a significant inhibition of laquinimod metabolism. Troleandomycin 27-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-72 16416302-3 2006 METHODS: The in vitro kinetic constants of CYP3A inactivation (K (I) and k (inact)) were estimated by varying the time of pre-incubation and the concentration of troleandomycin, erythromycin, clarithromycin, roxithromycin or azithromycin. Troleandomycin 162-176 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-48 15054565-6 2004 Complete inhibition of PPC hydroxylation was achieved by combined addition of the CYP3A4-specific inhibitor triacetyloleandomycin (TAO) and a monoclonal, inhibitory antibody (mAb) directed against CYP2C8, 9, 18 and 19, except for the (R)-4"-hydroxylation that was, however, inhibited by ~80% using TAO alone. Troleandomycin 108-129 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 82-88 15546903-7 2005 24-Hydroxylase activity in recombinant CYP3A4 and pooled human liver microsomes showed dose-dependent inhibition by ketoconazole, troleandomycin, alpha-naphthoflavone, and isoniazid, known inhibitors of CYP3A4. Troleandomycin 130-144 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-45 15546903-7 2005 24-Hydroxylase activity in recombinant CYP3A4 and pooled human liver microsomes showed dose-dependent inhibition by ketoconazole, troleandomycin, alpha-naphthoflavone, and isoniazid, known inhibitors of CYP3A4. Troleandomycin 130-144 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 203-209 15746066-8 2005 Troleandomycin and ketoconazole, both inhibitors of CYP3A, markedly reduced PNU-159682 formation by HLMs; the reaction was also concentration-dependently inhibited by a monoclonal antibody to CYP3A4/5. Troleandomycin 0-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 192-198 15356306-5 2004 The CYP3A inhibitors used in the study were nitroimidazole antifungal agents, diltiazem, verapamil, and troleandomycin; each doubles, at least, the area under the time-concentration curve for a CYP3A substrate. Troleandomycin 104-118 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-9 15356306-5 2004 The CYP3A inhibitors used in the study were nitroimidazole antifungal agents, diltiazem, verapamil, and troleandomycin; each doubles, at least, the area under the time-concentration curve for a CYP3A substrate. Troleandomycin 104-118 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 194-199 15184267-6 2004 Therefore, three chemical inhibitors were used in the experiments: ellipticine against CYP1A1, furafylline against CYP1A2, and troleandomycin against CYP3A4. Troleandomycin 127-141 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 150-156 12936704-6 2003 Normorphine formation decreased when incubated in the presence of troleandomycin or quercetin (by 46 and 33-36%, respectively), which further corroborates the contribution of CYP3A4 and CYP2C8. Troleandomycin 66-80 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 175-181 15268978-7 2004 In an individual liver microsome sample with a high CYP3A protein content, troleandomycin and ketoconazole inhibited norhydromorphone formation by 80%. Troleandomycin 75-89 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-57 14652237-12 2003 In vitro, troleandomycin, an inhibitor of CYP3A4, inhibited the demethylation of tamoxifen to N-desmethyl-tamoxifen by 78% (95% CI = 65% to 91%), and quinidine, an inhibitor of CYP2D6, reduced the subsequent hydroxylation of N-desmethyl-tamoxifen to endoxifen by 79% (95% CI = 50% to 108%). Troleandomycin 10-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 42-48 15005856-14 2004 Activity in recombinant CYP3A4 and pooled liver microsomes was dose-dependently inhibited by ketoconazole, troleandomycin, isoniazid, and alpha-naphthoflavone, known inhibitors of CYP3A4. Troleandomycin 107-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 24-30 15005856-14 2004 Activity in recombinant CYP3A4 and pooled liver microsomes was dose-dependently inhibited by ketoconazole, troleandomycin, isoniazid, and alpha-naphthoflavone, known inhibitors of CYP3A4. Troleandomycin 107-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 180-186 14678348-6 2004 Formation of all metabolites was observed with expressed recombinant CYP3A4, inhibited by troleandomycin (65, 77 and 35%, respectively, P < 0.05) and associated with CYP3A4 expression (rs = 0.612, rs = 0.585 and rs = 0.430, P < 0.01, respectively). Troleandomycin 90-104 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-75 15618724-4 2003 The CL(int) of CAM was markedly reduced by selective inhibitors of CYP3A4 (ketoconazole and troleandomycin) and by polyclonal antibodies raised against CYP3A4/5 in human liver microsomes. Troleandomycin 92-106 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 67-73 12848784-7 2003 Whereas inhibitors that are selective for CYP2D6, CYP2C9 or CYP1A2 did not significantly inhibit the oxidative metabolism of SVA, the CYP3A4/5 inhibitor troleandomycin markedly (about 90%) inhibited SVA metabolism. Troleandomycin 153-167 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 134-140 12433801-4 2002 In human microsomes, inhibition of total metabolism by the CYP3A-selective inhibitors ketoconazole, troleandomycin, and 6",7"-dihydroxybergamottin, each at 10 micro M concentration, was 83 to 95%, whereas inhibition with inhibitors selective for other p450 isozymes was minimal. Troleandomycin 100-114 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 59-64 12160484-16 2002 The metabolism of V11294 (8 micro M) to V10331, V10332 and V11689 was markedly inhibited by the CYP3A mechanism-based inhibitor troleandomycin. Troleandomycin 128-142 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 96-101 12180536-4 2002 Furafylline (CYP1A2) and sulfaphenazole (CYP2C9) inhibited the N-demethylation to a lesser extent while quinidine (CYP2D6) or troleandomycine (CYP3A4) had no effect. Troleandomycin 126-141 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 143-149 12162853-8 2002 8-Hydroxylation was inhibited by the addition of CYP3A4 antibodies as well as troleandomycin, a specific inhibitor of CYP3A4. Troleandomycin 78-92 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 118-124 15618694-8 2002 The formations of both BAY o 3199 and BAY r 9425 in the human intestinal microsomes were inhibited by pretreatment with troleandomycin (TAO) and antiserum against CYP3A4. Troleandomycin 120-134 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 163-169 11409940-9 2001 The production of this metabolite was inhibited following CYP3A4 inhibition by troleandomycin in human liver microsomes, and markedly enhanced following CYP3A induction by dexamethasone in rat liver microsomes. Troleandomycin 79-93 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-64 11752104-6 2002 Omeprazole (a CYP2C19 substrate) at a high concentration and triacetyloleandomycin (a selective inhibitor of CYP3A4) substantially inhibited O-dealkylation of fluoxetine. Troleandomycin 61-82 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 109-115 11504799-8 2001 CYP3A4 inhibitors (troleandomycin and ketoconazole) inhibited EDDP and EMDP formation by >70%. Troleandomycin 19-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 11454734-9 2001 Tramadol metabolism in human liver microsomes to M1 and M2 was markedly inhibited by the CYP2D6 inhibitor quinidine and the CYP3A4 inhibitor troleandomycin, respectively. Troleandomycin 141-155 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 124-130 11409940-9 2001 The production of this metabolite was inhibited following CYP3A4 inhibition by troleandomycin in human liver microsomes, and markedly enhanced following CYP3A induction by dexamethasone in rat liver microsomes. Troleandomycin 79-93 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-63 11428655-7 2001 The 5-OHN formation was also inhibited by the CYP3A4 inhibitors ketoconazole and troleandomycin, but not significantly inhibited by several other P450 inhibitors. Troleandomycin 81-95 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 46-52 11730569-8 2001 The reaction was minimally inhibited by coincubation with chemical probe, inhibitor of CYP3A4 (triacetyloleandomycin, TAO). Troleandomycin 95-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-93 11741520-7 2001 Using furafyllin and troleandomycin to inhibit CYP1A2 and CYP3A4 in liver microsomes, it was found that the 2-hydroxylation had been inhibited about the same amount. Troleandomycin 21-35 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-64 11259570-6 2001 LAAM and nor-LAAM metabolism was inhibited by the CYP3A4-selective inhibitors troleandomycin, erythromycin, ketoconazole, and midazolam. Troleandomycin 78-92 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-56 11259984-3 2001 RESULTS: Troleandomycin, a CYP3A4 inhibitor, markedly reduced the oxidation of terfenadine (26% of controls) in human liver microsomes, but showed only a marginal inhibition on the oxidation of astemizole (81% of controls). Troleandomycin 9-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-33 11038155-5 2000 The 7alpha- and 7beta-hydroxy-Delta(8)-THC microsomal alcohol oxygenase activities in human liver were significantly inhibited by addition of 100 microM troleandomycin, 1 microM ketoconazole, and anti-CYP3A antibody, although these activities were not inhibited by 1 microM 7, 8-benzoflavone and 50 microM sulfaphenazole. Troleandomycin 153-167 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 201-206 11125847-3 2000 Resveratrol, erythromycin and troleandomycin inactivated CYP3A4 at a similar rate (as reflected by k(inact)) whereas the binding affinity to CYP3A4 (as reflected by K(I)) was in the order of: troleandomycin > erythromycin > resveratrol. Troleandomycin 30-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-63 11125847-3 2000 Resveratrol, erythromycin and troleandomycin inactivated CYP3A4 at a similar rate (as reflected by k(inact)) whereas the binding affinity to CYP3A4 (as reflected by K(I)) was in the order of: troleandomycin > erythromycin > resveratrol. Troleandomycin 30-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 141-147 11125847-3 2000 Resveratrol, erythromycin and troleandomycin inactivated CYP3A4 at a similar rate (as reflected by k(inact)) whereas the binding affinity to CYP3A4 (as reflected by K(I)) was in the order of: troleandomycin > erythromycin > resveratrol. Troleandomycin 192-206 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 141-147 11125847-4 2000 (K(I) and k(inact) for CYP3A4 inactivation by resveratrol, erythromycin and troleandomycin are 20 microM and 0.20 min(-1), 5.3 microM and 0.12 min(-1) and 0.18 microM and 0.15 min(-1), respectively.) Troleandomycin 76-90 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 23-29 11501186-8 2000 Inhibition experiments showed that troleandomycin (100 mumol.L-1) and diethyldithiocarbamate (100 mumol.L-1), as potent CYP3A4 and CYP2E1 inhibitors, respectively, reduced the formation rate of CG by 81.1% and 47.23%, while quinidine (10 mumol.L-1), furafylline (20 mumol.L-1), and sulfaphenazole (10 mumol.L-1), which were inhibitors towards CYP2D6, 1A2 and 2C9/10, respectively, did not display significant inhibition. Troleandomycin 35-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 120-126 10923859-11 2000 Rifalazil-32-hydroxylation in microsomes was completely inhibited by CYP3A4-specific inhibitors (fluconazole, ketoconazole, miconazole, troleandomycin) and drugs metabolized by CYP3A4 such as cyclosporin A and clarithromycin, indicating that the enzyme responsible for the rifalazil-32-hydroxylation is CYP3A4. Troleandomycin 136-150 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-75 10901707-4 2000 Troleandomycin inhibited the N-deethylation of lidocaine by about 50% at 800 microM lidocaine, suggesting that the role of CYP3A4 may be more important than that of CYP1A2 at high lidocaine concentrations. Troleandomycin 0-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 123-129 20575842-5 2000 Since variation exists in the human population with respect to the catalytic activity of CYP 3A isozymes, which are the principal cocaine N -demethylators in humans, inhibition of CYP 3A by troleandomycin in the rat may be useful as a model of the human cocaine "poor metabolizer" phenotype. Troleandomycin 190-204 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 20575842-5 2000 Since variation exists in the human population with respect to the catalytic activity of CYP 3A isozymes, which are the principal cocaine N -demethylators in humans, inhibition of CYP 3A by troleandomycin in the rat may be useful as a model of the human cocaine "poor metabolizer" phenotype. Troleandomycin 190-204 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 180-186 10926350-7 2000 The macrolide antibacterials clarithromycin, erythromycin and troleandomycin are inhibitors of CYP3A4 and should not be used in conjunction with cisapride. Troleandomycin 62-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-101 10923859-11 2000 Rifalazil-32-hydroxylation in microsomes was completely inhibited by CYP3A4-specific inhibitors (fluconazole, ketoconazole, miconazole, troleandomycin) and drugs metabolized by CYP3A4 such as cyclosporin A and clarithromycin, indicating that the enzyme responsible for the rifalazil-32-hydroxylation is CYP3A4. Troleandomycin 136-150 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 177-183 10923859-11 2000 Rifalazil-32-hydroxylation in microsomes was completely inhibited by CYP3A4-specific inhibitors (fluconazole, ketoconazole, miconazole, troleandomycin) and drugs metabolized by CYP3A4 such as cyclosporin A and clarithromycin, indicating that the enzyme responsible for the rifalazil-32-hydroxylation is CYP3A4. Troleandomycin 136-150 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 177-183 10570031-7 1999 Studies using the CYP3A4 inhibitors ketoconazole, troleandomycin, and erythromycin suggested a role for CYP3A4 in the formation of 2-, 8-, and 12-hydroxyNVP. Troleandomycin 50-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 18-24 10692561-4 2000 The contributions of each human P450 to overall liver microsomal N-dechloroethylation were calculated using a recently described relative substrate-activity factor method, and were found to be in excellent agreement with the results of inhibition studies using the CYP3A inhibitor troleandomycin and an inhibitory monoclonal antibody to CYP2B6. Troleandomycin 281-295 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 265-270 10725304-9 2000 The strongest inhibition of bupivacaine metabolism was obtained for troleandomycin (-95% at 50 microM), a specific CYP3A inhibitor. Troleandomycin 68-82 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-120 10570031-7 1999 Studies using the CYP3A4 inhibitors ketoconazole, troleandomycin, and erythromycin suggested a role for CYP3A4 in the formation of 2-, 8-, and 12-hydroxyNVP. Troleandomycin 50-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 104-110 10647912-7 1999 The formation of both metabolites was markedly decreased by ketoconazole, miconazole or troleandomycin (TAO), CYP3A-selective inhibitors, and also was inhibited by anti-CYP3A antibodies. Troleandomycin 88-102 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 169-174 10647912-7 1999 The formation of both metabolites was markedly decreased by ketoconazole, miconazole or troleandomycin (TAO), CYP3A-selective inhibitors, and also was inhibited by anti-CYP3A antibodies. Troleandomycin 104-107 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 169-174 10417492-8 1999 Cycloguanil formation was inhibited significantly by omeprazole (CYP2C19/3A), troleandomycin (CYP3A), diethyldithiocarbamate (CYP2E1/3A), furafylline (CYP1A2), and (S)-mephenytoin. Troleandomycin 78-92 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 94-99 10484078-8 1999 The CYP3A inhibitor troleandomycin and an anti-CYP3A IgG inhibited the activity slightly. Troleandomycin 20-34 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-9 10454485-1 1999 Diltiazem (DTZ) N-demethylation occurs by cytochrome P-450 (CYP) 3A based on the following observations: 1) a single enzyme Michaelis-Menten model of metabolite formation, 2) high correlations of DTZ N-demethylation activity to other CYP3A activities, 3) inhibition of DTZ N-demethylation activity by triacetyloleandomycin, and 4) DTZ N-demethylation activity by expressed CYP3A enzymes only. Troleandomycin 301-322 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 42-67 10548453-4 1999 The formation of 4-hydroxyalprazolam and 1"-hydroxyalprazolam at an alprazolam concentration of 62.5 microM were reduced by the prototypic CYP3A inhibitor, troleandomycin (50 microM), by 97 and 9900 respectively. Troleandomycin 156-170 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 139-144 10411567-3 1999 Sulfoxide formation was determined to be cytochrome P-450 (CYP) 3A4-dependent by correlation with CYP3A4-marker nifedipine oxidase activity, inhibition by cyclosporin A and troleandomycin, and inhibition of R- (70%) and S- (64%) sulfoxide formation by anti-3A antibody. Troleandomycin 173-187 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-67 10216279-9 1999 Troleandomycin, a selective inhibitor of CYP3A enzymes, inhibited 6alpha-hydroxylation of taurochenodeoxycholic acid almost completely at a 10 microM concentration. Troleandomycin 0-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-46 9929520-8 1999 Quinidine almost completely inhibited the CYP2D6-mediated de-esterification at the concentration of 1 x 10(-6) M. Ketoconazole and troleandomycin inhibited the CYP3A4-mediated reaction in a dose-related manner. Troleandomycin 131-145 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 160-166 10359460-5 1999 Troleandomycin (CYP3A inhibitor) and furafylline (CYP1A2 inhibitor) inhibited CLZ N-oxidation in human liver microsomes by 23.2+/-12.1% and 7.8+4.3%, respectively, whereas CLZ N-demethylation was inhibited by 17.5+/-13.9% and 25.6+/-16.5%, respectively. Troleandomycin 0-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 16-21 10233205-7 1999 Selective chemical inhibitors of CYP3A (troleandomycin, ketoconazole) and monoclonal human CYP3A4 antibodies significantly inhibited (P<0.05) the formation of EDDP in a concentration dependent manner by up to 80%. Troleandomycin 40-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 33-38 9931427-13 1999 Troleandomycin, a specific inhibitor of CYP3A4 and 3A5, inhibited the 25-hydroxylase activity of pooled human liver microsomes by more than 90% at 50 microM. Troleandomycin 0-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-46 9806945-0 1998 Comparative studies of in vitro inhibition of cytochrome P450 3A4-dependent testosterone 6beta-hydroxylation by roxithromycin and its metabolites, troleandomycin, and erythromycin. Troleandomycin 147-161 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 46-65 9884161-3 1998 Selective inhibitors-4-methylpyrazole (CYP2E1), furafylline (CYP1A2), and troleandomycin (CYP3A4)-also decreased microsomal ethanol oxidation in the livers of 18 organ donors. Troleandomycin 74-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-96 9806945-5 1998 Recombinant human CYP3A4 in a baculovirus system coexpressing NADPH-P450 reductase was very active in catalyzing the N-demethylation of roxithromycin, M1, and M2, as well as troleandomycin, erythromycin, and M3. Troleandomycin 174-188 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 18-24 9806945-6 1998 The order for inhibition of CYP3A4-dependent testosterone 6beta-hydroxylation activities by these macrolide antibiotics in the recombinant CYP3A4 system was estimated to be troleandomycin > erythromycin >/= M3 >/= M2 > M1 >/= roxithromycin. Troleandomycin 173-187 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 28-34 9806945-6 1998 The order for inhibition of CYP3A4-dependent testosterone 6beta-hydroxylation activities by these macrolide antibiotics in the recombinant CYP3A4 system was estimated to be troleandomycin > erythromycin >/= M3 >/= M2 > M1 >/= roxithromycin. Troleandomycin 173-187 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 139-145 9618413-4 1998 Anti-CYP3A antibodies, as well as the specific CYP3A inhibitors troleandomycin and erythromycin, inhibited small intestinal metabolism of sirolimus, confirming that, as in the liver, CYP3A enzymes are responsible for sirolimus metabolism in the small intestine. Troleandomycin 64-78 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 47-52 9845092-11 1998 CYP 3A involvement was confirmed by the use of the CYP 3A specific inhibitor, triacetyloleandomycin (TAO), which repressed the formation of AQM to 13% of the uninhibited value and abolished completely the formation of AQ4. Troleandomycin 78-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 9845092-11 1998 CYP 3A involvement was confirmed by the use of the CYP 3A specific inhibitor, triacetyloleandomycin (TAO), which repressed the formation of AQM to 13% of the uninhibited value and abolished completely the formation of AQ4. Troleandomycin 78-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 51-57 9845092-11 1998 CYP 3A involvement was confirmed by the use of the CYP 3A specific inhibitor, triacetyloleandomycin (TAO), which repressed the formation of AQM to 13% of the uninhibited value and abolished completely the formation of AQ4. Troleandomycin 101-104 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 9845092-11 1998 CYP 3A involvement was confirmed by the use of the CYP 3A specific inhibitor, triacetyloleandomycin (TAO), which repressed the formation of AQM to 13% of the uninhibited value and abolished completely the formation of AQ4. Troleandomycin 101-104 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 51-57 9825830-6 1998 Ketoconazole and troleandomycin, inhibitors of CYP3A4, inhibited competitively both haloperidol and CPHP formation, with a Ki value lower than 0.2 microM for ketoconazole and lower than 0.3 microM for troleandomycin. Troleandomycin 17-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 47-53 9825830-6 1998 Ketoconazole and troleandomycin, inhibitors of CYP3A4, inhibited competitively both haloperidol and CPHP formation, with a Ki value lower than 0.2 microM for ketoconazole and lower than 0.3 microM for troleandomycin. Troleandomycin 201-215 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 47-53 9698291-9 1998 However, significant inhibition by ketoconazole and troleandomycin indicates that NPC formation in patients may be influenced by coadministration of drugs with known anti-CYP3A activities. Troleandomycin 52-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 171-176 9618413-4 1998 Anti-CYP3A antibodies, as well as the specific CYP3A inhibitors troleandomycin and erythromycin, inhibited small intestinal metabolism of sirolimus, confirming that, as in the liver, CYP3A enzymes are responsible for sirolimus metabolism in the small intestine. Troleandomycin 64-78 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 47-52 9523995-3 1998 Through studies with isoform selective chemical inhibitors, CYP3A4 was implicated as the low Km enzyme from 89.0+/-11.2% inhibition of lisofylline 4,5-diol formation by troleandomycin at 50 microM substrate and CYP2A6 was implicated as the high Km enzyme. Troleandomycin 169-183 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-66 9681669-6 1998 Troleandomycin, a relatively selective probe for CYP3A enzymes, inhibited the CYP3A4-mediated oxidation of reduced haloperidol in a dose-dependent manner. Troleandomycin 0-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 49-54 9681669-6 1998 Troleandomycin, a relatively selective probe for CYP3A enzymes, inhibited the CYP3A4-mediated oxidation of reduced haloperidol in a dose-dependent manner. Troleandomycin 0-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-84 9600717-7 1998 Troleandomycin, a specific inhibitor of CYP 3A4, inhibited adinazolam N-demethylation with an IC50 of 1.96 microM. Troleandomycin 0-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-47 9604298-11 1998 The metabolism of ZAL to DZAL in human liver microsomes was inhibited to 6-15% of control by 5-50 microM of the mechanism-based CYP3A inhibitor troleandomycin. Troleandomycin 144-158 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 128-133 9394028-11 1997 Inhibition studies have indicated that triacetyloleandomycin, a CYP3A specific inhibitor, almost completely inhibited the formation of both of these tazofelone metabolites. Troleandomycin 39-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-69 9113345-11 1997 Troleandomycin, a mechanism based CYP3A3/4 inhibitor, inhibited MEM formation by an average maximum of 46%, with an IC50 varying from 1 to 2.6 microM. Troleandomycin 0-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 9152594-7 1997 The CYP3A inhibitor troleandomycin was used to inhibit the formation of PCP metabolites. Troleandomycin 20-34 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-9 9321513-4 1997 Gestodene and triacetyloleandomycin (selective for CYP3A enzymes) inhibited the demethylations of both antiprogestins by up to 77%. Troleandomycin 14-35 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 51-56 9278210-3 1997 METHODS: Healthy subjects were given troleandomycin (TAO), a selective inhibitor of CYP3A, 250 mg daily for 2 days before a single oral dose of 100 mg IMI was administered. Troleandomycin 37-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-89 9223567-8 1997 The CYP3A4 inhibitors ketoconazole and troleandomycin decreased microsomal DTZ oxidation, but inhibitors or substrates of CYP2C, CYP2D and CYP2E1 produced no inhibition. Troleandomycin 39-53 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-10 8886604-9 1996 The formation of 4-OH-ropivacaine, 2-OH-methyl-ropivacaine, and PPX was markedly inhibited in the presence of troleandomycin, an inhibitor of CYP3A. Troleandomycin 110-124 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 142-147 9131945-4 1997 The activity at the low affinity site was eliminated by triacetyloleandomycin and ketoconazole, selective inhibitors of CYP3A4, such that the kinetics were then described by a two-site model comprising two Michaelis-Menten functions. Troleandomycin 56-77 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 120-126 8960070-8 1997 Chemical inhibition of CYP3A4 by preincubation with gestodene (40 microM) or troleandomycin (40 microM) reduced the formation of 3DMC and 2DMC by 70 and 80%, respectively, whereas quinidine, diethyldithiocarbamate, and sulfaphenazole had no inhibitory effect. Troleandomycin 77-91 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 23-29 8968357-10 1996 Ketoconazole and troleandomycin (inhibitors of CYP3A4) inhibited the 3-hydroxylation of quinine by human liver microsomes with respective mean IC50 values of 0.026 microM and 28.9 microM. Troleandomycin 17-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 47-53 9029057-5 1997 Ketoconazole and troleandomycin, selective inhibitors of cytochrome P4503A4 (CYP3A4), were potent inhibitors for all oxidative metabolites of saquinavir. Troleandomycin 17-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-75 9029057-5 1997 Ketoconazole and troleandomycin, selective inhibitors of cytochrome P4503A4 (CYP3A4), were potent inhibitors for all oxidative metabolites of saquinavir. Troleandomycin 17-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 77-83 9023313-8 1997 The CYP3A4 inhibitors ketoconazole and triacetyloleandomycin decreased the observed rate of microsomal parathion oxidation, but chemicals known to interact preferentially with other human CYP were essentially noninhibitory. Troleandomycin 39-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-10 8765473-4 1996 The CYP3A inhibitors gestodene, triacetyloleandomycin, and 17 alpha-ethynylestradiol inhibited mifepristone demethylation and hydroxylation by 70-80%; antibodies to CYP3A4 inhibited these reactions by approximately 82 and 65%, respectively. Troleandomycin 32-53 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-9 8765473-4 1996 The CYP3A inhibitors gestodene, triacetyloleandomycin, and 17 alpha-ethynylestradiol inhibited mifepristone demethylation and hydroxylation by 70-80%; antibodies to CYP3A4 inhibited these reactions by approximately 82 and 65%, respectively. Troleandomycin 32-53 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 165-171 8820426-10 1996 Preincubation of Caco-2 cell monolayers with troleandomycin, a specific inhibitor for the microsomal CYP3A protein, reduced the formation of the metabolite M-17, suggesting that an enzyme that functionally resembles CYP3A is responsible for the formation of this metabolite. Troleandomycin 45-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 101-106 8818573-6 1996 Preincubation with troleandomycin (50 microM), or gestodene (50 microM) inhibitors of CYP3A4, decreased the rate of production of norcodeine by 60 and 45% compared to control values, respectively. Troleandomycin 19-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-92 8627581-5 1996 A role for CYP3A4 in the formation of the three major metabolites (tirilazad hydroxylase activity) was established in human liver microsomal preparations: 1) Tirilazad hydroxylation was potently inhibited by troleandomycin and ketoconazole, specific inhibitors of CYP3A4. Troleandomycin 208-222 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 11-17 8627581-5 1996 A role for CYP3A4 in the formation of the three major metabolites (tirilazad hydroxylase activity) was established in human liver microsomal preparations: 1) Tirilazad hydroxylation was potently inhibited by troleandomycin and ketoconazole, specific inhibitors of CYP3A4. Troleandomycin 208-222 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 264-270 8820421-4 1996 Ketoconazole and troleandomycin, both selective inhibitors for cytochrome P450 3A4 (CYP3A4), markedly inhibited the formation of all oxidative metabolites of MK-639; whereas other inhibitors (furafylline, sulfaphenazole, quinidine, S-mephenytoin, and diethyldithiocarbamate) had little effect on MK-639 metabolism. Troleandomycin 17-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-82 8820421-4 1996 Ketoconazole and troleandomycin, both selective inhibitors for cytochrome P450 3A4 (CYP3A4), markedly inhibited the formation of all oxidative metabolites of MK-639; whereas other inhibitors (furafylline, sulfaphenazole, quinidine, S-mephenytoin, and diethyldithiocarbamate) had little effect on MK-639 metabolism. Troleandomycin 17-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-90 8820426-10 1996 Preincubation of Caco-2 cell monolayers with troleandomycin, a specific inhibitor for the microsomal CYP3A protein, reduced the formation of the metabolite M-17, suggesting that an enzyme that functionally resembles CYP3A is responsible for the formation of this metabolite. Troleandomycin 45-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 216-221 7586950-3 1995 Troleandomycin (40 mumol/L) inhibited hydroxylamine formation at 100 mumol/L dapsone by 50%; diethyldithiocarbamate (150 mumol/L) and tolbutamide (400 mumol/L) inhibited at 5 mumol/L dapsone by 50% and 20%, respectively, suggesting that the low-affinity isozyme is CYP3A4 and the high-affinity isozymes are 2E1 and 2C. Troleandomycin 0-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 265-271 8615885-8 1996 Rabbit polyclonal antibodies raised against the rat CYP3A1 enzyme (5 mg IgG/nmol P450) and troleandomycin (0.5 microM), a specific inhibitor of CYP3A4, decreased the formation of DCL by 53 and 75%, respectively, when added to 1.42 microM loratadine microsomal incubations. Troleandomycin 91-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 144-150 8712396-6 1996 Gestodene and troleandomycin (chemical inhibitors of CYP3A4) and antibody to CYP3A4 inhibited N-dealkylation of fentanyl and sufentanil. Troleandomycin 14-28 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-59 8548776-5 1996 The formation of hydroxydocetaxel was strongly reduced by CYP3A inhibitors such as ketoconazole, midazolam, erythromycin, testosterone, orphenadrine, and troleandomycin, whereas quinidine (CYP2D6), hexobarbital, tolbutamide, and mephenytoin (CYP2C) had no or little effect. Troleandomycin 154-168 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-63 8689938-9 1995 The metabolism of tacrolimus by human small intestine was inhibited by anti-CYP3A, troleandomycin, and erythromycin, indicating that, as in the liver, CYP3A enzymes are the major enzymes for tacrolimus metabolism in the human small intestine. Troleandomycin 83-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 151-156 7587944-8 1995 Involvement of the CYP3A(4) in terfenadine metabolism was further confirmed by the following studies: a) inhibition of terfenadine alcohol formation by ketoconazole and troleandomycin, two specific inhibitors of CYP3A(4), and b) time course of terfenadine alcohol formation by cloned human CYP3A(4). Troleandomycin 169-183 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 19-27 7503788-4 1995 Oxidation of O6-benzylguanine also occurred with pooled human liver microsomes and was inhibited by both furafylline and troleandomycin, selective inhibitors of CYP1A2 and CYP3A4, respectively. Troleandomycin 121-135 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 172-178 7587944-8 1995 Involvement of the CYP3A(4) in terfenadine metabolism was further confirmed by the following studies: a) inhibition of terfenadine alcohol formation by ketoconazole and troleandomycin, two specific inhibitors of CYP3A(4), and b) time course of terfenadine alcohol formation by cloned human CYP3A(4). Troleandomycin 169-183 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 212-220 7587944-8 1995 Involvement of the CYP3A(4) in terfenadine metabolism was further confirmed by the following studies: a) inhibition of terfenadine alcohol formation by ketoconazole and troleandomycin, two specific inhibitors of CYP3A(4), and b) time course of terfenadine alcohol formation by cloned human CYP3A(4). Troleandomycin 169-183 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 212-220 8054246-13 1994 The extents of inhibition by R,S-mephenytoin, troleandomycin and the two antibodies varied with the immunoreactive CYP3A content of the microsomes used. Troleandomycin 46-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-120 8001226-12 1994 Treatment of rats with troleandomycin (TAO), an inducer of CYP3A, followed by the dissociation of the TAO-CYP3A complex, elevated the covalent binding to liver microsomes approximately 3-fold. Troleandomycin 23-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-111 8001226-12 1994 Treatment of rats with troleandomycin (TAO), an inducer of CYP3A, followed by the dissociation of the TAO-CYP3A complex, elevated the covalent binding to liver microsomes approximately 3-fold. Troleandomycin 39-42 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-111 7628296-7 1995 The metabolism of IMM was also greatly inhibited (approximately 80%) by the CYP3A suicide substrate triacetyloleandomycin and a CYP3A inhibitory antibody, indicating the involvement of CYP3A proteins in the biotransformation of IMM. Troleandomycin 100-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-81 7720520-7 1995 Of the CYP3A4 inhibitor probes used, troleandomycin proved to be the most specific for testosterone 6 beta-hydroxylation. Troleandomycin 37-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 7-13 8161344-4 1994 The CYP3A4-specific inhibitor triacetyloleandomycin inhibited ifosfamide N-dechloroethylation by human liver microsomes with an IC50 of approximately 10 microM. Troleandomycin 30-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-10 2269307-13 1990 Microsomal suspensions containing P450 NF25 were also able to catalyze several oxidation reactions that were expected from the activities of the protein isolated from human liver, including nifedipine 1,4-oxidation, quinidine 3-hydroxylation and N-oxygenation, and N-demethylation of the macrolide antibiotics erythromycin and troleandomycin. Troleandomycin 327-341 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-43 7903909-7 1994 The formation of metabolite M4 was substantially reduced both by antibody directed against CYP3A and by the addition of CYP3A substrates such as orphenadrine, erythromycin, troleandomycin, and testosterone. Troleandomycin 173-187 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 120-125 8242617-11 1993 In contrast, troleandomycin, a selective inhibitor of CYP3A3 and -3A4, and anti-CYP3A IgG substantially inhibited microsomal ifosphamide hydroxylation but had little or no effect on microsomal cyclophosphamide hydroxylation. Troleandomycin 13-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 54-69 8242617-11 1993 In contrast, troleandomycin, a selective inhibitor of CYP3A3 and -3A4, and anti-CYP3A IgG substantially inhibited microsomal ifosphamide hydroxylation but had little or no effect on microsomal cyclophosphamide hydroxylation. Troleandomycin 13-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 54-59 32967779-5 2020 The observed differences were associated with different inhibitory/inactivation potentials of troleandomycin, erythromycin, clarithromycin and azithromycin, suggesting CYP3A4 Template also as a tool for drug-interaction mechanisms. Troleandomycin 94-108 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 168-174