PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 12419016-8 2002 Tamoxifen and N-desmethyltamoxifen exhibited time-dependent inactivation of testosterone 6beta-hydroxylation by cDNA-expressed CYP3A4 (+ cytochrome b5) yielding k(inact) and K(i) of 0.04 min(-1) and 0.2 micro M for tamoxifen and 0.08 min(-1) and 2.6 micro M for N-desmethyltamoxifen. testosterone 6beta 76-94 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 127-133 12185560-7 2002 Furthermore, significant correlation between CYP3A4 protein and V(max) of testosterone 6beta-hydroxylation (r=0.82, P<0.001) as well as CYP3A4 protein and its mRNA (r=0.52, P<0.01) was observed. testosterone 6beta 74-92 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-51 11717174-2 2001 DDB was found to be a strong inhibitor of testosterone 6beta-hydroxylation activity (CYP3A4) with a K(i) value of 0.27 +/- 0.21 microM. testosterone 6beta 42-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-91 11353747-6 2001 Furthermore, P450 MI-2 and P450 MI-3 were recognized by anti-CYP4F and anti-CYP3A antibodies, respectively, in immunoblot analysis and catalyzed leukotriene B(4) omega-hydroxylation and testosterone 6beta-hydroxylation, which are known to be mediated by CYP4F and CYP3A, respectively. testosterone 6beta 186-204 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-81 11717174-6 2001 This complex formation resulted in a time-dependent loss of CYP3A-catalyzed marker activity (testosterone 6beta-hydroxylation) in human liver microsomes. testosterone 6beta 93-111 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-65 9698298-4 1998 The BN N-dealkylation activities in 10 human liver microsomal preparations were strongly correlated with microsomal CYP3A-specific metabolic reactions, i.e. triazolam 1"-hydroxylation (r = 0.954), midazolam 1"-hydroxylation (r = 0.928), and testosterone 6beta-hydroxylation (r = 0.897). testosterone 6beta 241-259 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 116-121 10859150-2 2000 Microsomal CYP3A-mediated testosterone 6beta-hydroxylation was inhibited by the addition of a fruit juice (2.5%, v/v) from eight different grapefruit sources, two sweeties, three pomelos, and one sour orange, whereas no clear inhibition was observed with two sweet orange juices. testosterone 6beta 26-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 11-16 10771285-3 2000 Our results showed that CYP3A4/5 contributes to testosterone 6beta-hydroxylation, taxol phenol formation, diazepam 3-hydroxylation, diazepam N-demethylation, and aflatoxin B1 3-hydroxylation in human liver by 79.2%, 81.5%, 73. testosterone 6beta 48-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 24-30 10668853-10 2000 Baculovirus-directed cDNA expression revealed that the CYP3A4*2 P450 had a lower intrinsic clearance for the CYP3A4 substrate nifedipine compared with the wild-type enzyme but was not significantly different from the wild-type enzyme for testosterone 6beta-hydroxylation. testosterone 6beta 238-256 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-61 10668853-10 2000 Baculovirus-directed cDNA expression revealed that the CYP3A4*2 P450 had a lower intrinsic clearance for the CYP3A4 substrate nifedipine compared with the wild-type enzyme but was not significantly different from the wild-type enzyme for testosterone 6beta-hydroxylation. testosterone 6beta 238-256 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 109-115 10421615-2 1999 Here we report that Taxol increased CYP3A-dependent testosterone 6beta-hydroxylation in intact hepatocytes. testosterone 6beta 52-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-41 10216279-8 1999 There was also a strong correlation between 6alpha-hydroxylation of lithocholic acid, CYP3A levels and testosterone 6beta-hydroxylation (r2=0.7). testosterone 6beta 103-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-91 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. testosterone 6beta 45-63 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. testosterone 6beta 45-63 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 139-145 11523064-11 2000 Using the assay of testosterone 6beta-hydroxylation the CYP3A4 activity was decreased by L, S and F with IC(50) values of about 200 microM and a little more by C and A (IC(50) around 100 microM). testosterone 6beta 19-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 10950859-5 2000 High concentrations (100 microM) of vinorelbine inhibited CYP3A4 activity (testosterone 6beta-hydroxylation activity) by 45.2%. testosterone 6beta 75-93 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-64 10525096-4 1999 One and 5 microl (0.5 and 2.5 microM IgG(2a)) of the mAb mouse ascites in 1-ml incubation containing 20 pmol of CYP3A4 strongly inhibited the testosterone 6beta-hydroxylation by 95 and 99%, respectively, and, to a lesser extent, cross-inhibited CYP3A5 and CYP3A7 activity. testosterone 6beta 142-160 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 112-118 10525096-8 1999 The results showed that CYP3A4 and CYP3A5 contribute >95% to both testosterone 6beta-hydroxylation and diazepam 3-hydroxylation and 52 to 73% to diazepam N-demethylation, respectively. testosterone 6beta 69-87 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 24-30 10460798-3 1999 Cytochrome b(5) (b(5)) and apolipoprotein b(5) further enhanced the testosterone 6beta-hydroxylation activities of CYP3A4/NPR membranes after addition to either bacterial membranes or purified enzymes. testosterone 6beta 68-86 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-121 26239802-4 2015 Our findings indicated that meclizine directly inhibited testosterone 6beta-hydroxylation catalyzed by human liver microsomes, recombinant CYP3A4, and recombinant CYP3A5. testosterone 6beta 57-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 139-145 9491822-8 1998 DDC also inhibited testosterone 6beta-hydroxylation (CYP3A-mediated) in man and rat, and tolbutamide 4-hydroxylase activity in rat. testosterone 6beta 19-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-58 33790108-4 2021 ANF noncompetitively inhibited testosterone 6beta-hydroxylation mediated by both CYP3A4 and CYP3A5. testosterone 6beta 31-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-87 31102695-7 2019 Compared to lithocholic acid 3-oxidation, CYP3A-catalyzed testosterone 6beta-hydroxylation was inhibited to a lesser extent by alpha-tocotrienol, gamma-tocotrienol, delta-tocotrienol, and a tocotrienol-rich vitamin E mixture. testosterone 6beta 58-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 42-47 9278209-6 1997 RESULTS: Ritonavir was a very potent inhibitor of CYP3A4 mediated testosterone 6beta-hydroxylation (mean K(i) = 0.019 +/- 0.004 microM, mean +/- s.d. testosterone 6beta 66-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-56 9223567-12 1997 The IC50 value of DTZ against CYP3A4-mediated testosterone 6beta-hydroxylation (substrate concentration, 50 microM) was 120 microM. testosterone 6beta 46-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-36 8820421-6 1996 Consistent with this, an anti-rat CYP3A1 rabbit polyclonal antibody, which shows a cross-reactive inhibition of CYP3A4-dependent testosterone 6beta-hydroxylation in human liver microsomes, completely inhibited MK-639 metabolism. testosterone 6beta 129-147 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 112-118 8820421-10 1996 Kinetic analysis showed that MK-639 is a very potent competitive inhibitor for testosterone 6beta-hydroxylation, with a Ki value of approximately 0.5 mu M. Collectively, these results consistently indicate that CYP3A4 is the isoform responsible for the oxidative metabolism of MK-639 in human liver microsomes. testosterone 6beta 79-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 211-217 27934636-4 2017 The RAF value for CYP3A4 or CYP2C9 derived from a particular P450-selective probe reaction was applied to calculate RAF-scaled CLint for other probe reactions of the same P450 isoform in a crossover manner and compared with the measured HLM CLint When RAF derived from midazolam or nifedipine was used for CYP3A4, the ICR for testosterone 6beta-hydroxylation was 31 and 25, respectively, suggesting significantly diverse interactions of CYP3A4 probes with the testing systems. testosterone 6beta 326-344 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 18-24 27934636-4 2017 The RAF value for CYP3A4 or CYP2C9 derived from a particular P450-selective probe reaction was applied to calculate RAF-scaled CLint for other probe reactions of the same P450 isoform in a crossover manner and compared with the measured HLM CLint When RAF derived from midazolam or nifedipine was used for CYP3A4, the ICR for testosterone 6beta-hydroxylation was 31 and 25, respectively, suggesting significantly diverse interactions of CYP3A4 probes with the testing systems. testosterone 6beta 326-344 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 306-312 27934636-4 2017 The RAF value for CYP3A4 or CYP2C9 derived from a particular P450-selective probe reaction was applied to calculate RAF-scaled CLint for other probe reactions of the same P450 isoform in a crossover manner and compared with the measured HLM CLint When RAF derived from midazolam or nifedipine was used for CYP3A4, the ICR for testosterone 6beta-hydroxylation was 31 and 25, respectively, suggesting significantly diverse interactions of CYP3A4 probes with the testing systems. testosterone 6beta 326-344 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 306-312 24078287-10 2014 Moreover, the overexpression of miR-223 significantly reduced CYP3A4-catalyzed testosterone 6beta-hydroxylation activity and CYP2E1-catalyzed chlorzoxazone 6-hydroxylase activity but not CYP1A2-catalyzed 7-ethoxyresorufin O-deethylase activity. testosterone 6beta 79-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-68 25678418-6 2015 Some metabolic activities of CYP3A4, including dehydroepiandrosterone 7beta-/16alpha-hydroxylation, estrone 2-hydroxylation and testosterone 6beta-hydroxylation, were higher than those for polymorphically expressed CYP3A5. testosterone 6beta 128-146 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-35 22022918-7 2012 In addition, the formation of ilaprazole sulfone correlated well with CYP3A-catalysed testosterone 6beta-hydroxylation and midazolam 1"-hydroxylation in 20 different human liver microsome panels. testosterone 6beta 86-104 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 70-75 24256945-2 2014 Here, we show that b5 mutations E48G, E49G, D58G, and D65G have reduced capacity to stimulate CYP3A4-catalyzed progesterone and testosterone 6beta-hydroxylation or nifedipine oxidation. testosterone 6beta 128-146 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 94-100 22509825-5 2012 Correlation analyses showed a significant correlation between mirabegron metabolism and testosterone 6beta-hydroxylation (CYP3A4/5 marker activity). testosterone 6beta 88-106 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 122-128 23514827-6 2013 The activity of CYP3A4 was assessed using testosterone 6beta-hydroxylation with recombinant CYP3A4. testosterone 6beta 42-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 16-22 17827338-6 2007 There was a high correlation between the rates of formation of M2/M3, M15, and M41, which was determined using 10 human liver microsomal samples and testosterone 6beta-hydroxylation catalyzed by CYP3A4/5 (r > or = 0.91). testosterone 6beta 149-167 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 195-201 21964476-6 2011 CYP3A4 activity was confirmed by measuring testosterone 6beta-hydroxylation. testosterone 6beta 43-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 21273732-6 2011 This includes midazolam 1"-hydroxylation and testosterone 6beta-hydroxylation, which are catalyzed by cynomolgus monkey cytochrome P450 (CYP) 3A4/5, orthologs of human CYP3A4/5, which are important drug-metabolizing enzymes. testosterone 6beta 45-63 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 168-174 20955791-3 2011 P-gp and CYP3A4 activities were assayed by [(3)H]digoxin and rhodamine 123 cellular retention and testosterone 6beta-hydroxylation, respectively. testosterone 6beta 98-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 9-15 20964620-0 2010 Activation of CYP3A-mediated testosterone 6beta-hydroxylation by tanshinone IIA and midazolam 1-hydroxylation by cryptotanshinone in human liver microsomes. testosterone 6beta 29-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-19 20964620-6 2010 In addition, tanshinone IIA activated CYP3A-mediated testosterone 6beta-hydroxylation, whereas cryptotanshinone and tanshinone I did not. testosterone 6beta 53-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-43 19817686-5 2009 Reconstitution of catalytic activity of cytochrome P450 3A4 in the reaction of testosterone 6beta-hydroxylation in the presence of Hmwb(5)-EGFP indicates that cytochrome b(5) in the fusion protein is able to stimulate the hydroxylation reaction. testosterone 6beta 79-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-59 22382318-4 2012 Ethyl acetate extracts of the tomato juices moderately reduced residual activity of CYP3A4 testosterone 6beta-hydroxylation activity by 19.3-26.2% with 0-min preincubation. testosterone 6beta 91-109 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-90 16702113-3 2006 Both CYP3A5 and CYP3A4 showed sigmoid and substrate inhibition patterns for testosterone 6beta-hydroxylation and terfenadine t-butylhydroxylation (TFDOH), respectively. testosterone 6beta 76-94 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 16-22 16416302-4 2006 CYP3A activity was determined from the measurement of testosterone 6beta-hydroxylation with human liver microsomes (HLM) and recombinant CYP3A4 as the enzyme sources. testosterone 6beta 54-72 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 16344723-10 2006 CYP3A4*1B showed a moderate effect on CYP3A4 mRNA and protein expression, as well as on CYP3A activity assessed as Vmax of testosterone 6beta-hydroxylation in a liver bank. testosterone 6beta 123-141 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 27699667-0 2006 Thin-Layer Chromatography Analysis of Human CYP3A-Catalyzed Testosterone 6beta-Hydroxylation. testosterone 6beta 60-78 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-49 27699667-6 2006 This method is applicable to enzymatic studies for the determination of CYP3A-dependent testosterone 6beta- hydroxylation activity in both human and animal liver microsomes. testosterone 6beta 88-106 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-77 16719384-0 2006 Thin-layer chromatography analysis of human CYP3A-catalyzed testosterone 6beta-hydroxylation. testosterone 6beta 60-78 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-49 16719384-6 2006 This method is applicable to enzymatic studies for the determination of CYP3A-dependent testosterone 6beta-hydroxylation activity in both human and animal liver microsomes. testosterone 6beta 88-106 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-77 16344723-10 2006 CYP3A4*1B showed a moderate effect on CYP3A4 mRNA and protein expression, as well as on CYP3A activity assessed as Vmax of testosterone 6beta-hydroxylation in a liver bank. testosterone 6beta 123-141 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 12756208-4 2003 CYP3A activity was measured by analysis of the rate of testosterone 6beta-hydroxylation. testosterone 6beta 55-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 15763633-2 2005 Zn2+ specifically inhibited the testosterone 6beta-hydroxylation activity of CYP3A4 with an IC50 value of 27 microM. testosterone 6beta 32-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 77-83 15608130-10 2005 This assay thus represents a high-throughput version of the classical testosterone 6beta-hydroxylation assay, which is the most widely used method to assess the potential for CYP3A4/5 inhibition of new chemical entities. testosterone 6beta 70-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 175-181 15175893-4 2004 The CYP3A4 activity of intact hepatocytes was measured as the rate of testosterone 6beta-hydroxylation. testosterone 6beta 70-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-10 14690448-6 2003 Cytochrome b(5) (b(5)) and apolipoprotein b(5) further enhanced the testosterone 6beta-hydroxylation activities of CYP3A4 in all tested phospholipids vesicles with various compositions. testosterone 6beta 68-86 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-121 15772082-0 2005 Cytochrome P450 3A4-catalyzed testosterone 6beta-hydroxylation stereochemistry, kinetic deuterium isotope effects, and rate-limiting steps. testosterone 6beta 30-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-19 15792627-6 2005 Western blots and testosterone 6beta-hydroxylation indicated that CYP3A was increased 50% by 4-NP, but was not affected by SJW. testosterone 6beta 18-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-71