PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 29759885-1 2018 Cytochrome P450 2J2 (CYP2J2) is involved in the metabolism of drugs, including albendazole, astemizole, ebastine, and endogenous substrates. Astemizole 92-102 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 0-19 33335233-7 2020 Molecular docking of a series of compounds including amiodarone, astemizole, danazol, ebastine, ketoconazole, terfenadine, terfenadone, and arachidonic acid to CYP2J2 confirmed the role of those residues in determining substrate binding and specificity of CYP2J2. Astemizole 65-75 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 160-166 33335233-7 2020 Molecular docking of a series of compounds including amiodarone, astemizole, danazol, ebastine, ketoconazole, terfenadine, terfenadone, and arachidonic acid to CYP2J2 confirmed the role of those residues in determining substrate binding and specificity of CYP2J2. Astemizole 65-75 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 256-262 33312341-8 2020 Interestingly, 6,8-diprenylorobol inhibited CYP2J2-mediated astemizole O-demethylation and ebastine hydroxylase activities with K i values of 9.46 and 2.61 muM, respectively. Astemizole 60-70 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 44-50 29759885-2 2018 In a previous study, we used recombinant CYP2J2 and determined whether danazol, hydroxyebastine, telmisartan, and terfenadone inhibited CYP2J2 by using four representative CYP2J2 substrates, namely albendazole, astemizole, ebastine, and terfenadine. Astemizole 211-221 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 136-142 29759885-2 2018 In a previous study, we used recombinant CYP2J2 and determined whether danazol, hydroxyebastine, telmisartan, and terfenadone inhibited CYP2J2 by using four representative CYP2J2 substrates, namely albendazole, astemizole, ebastine, and terfenadine. Astemizole 211-221 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 136-142 29759885-4 2018 Among the four CYP2J2 inhibitors tested, terfenadone was strongest inhibitor of CYP2J2-mediated metabolism of albendazole, astemizole, and terfenadine with IC50 values of 0.31, 0.15, and 2.11 muM, respectively, in human liver microsomes (HLMs). Astemizole 123-133 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 15-21 29759885-4 2018 Among the four CYP2J2 inhibitors tested, terfenadone was strongest inhibitor of CYP2J2-mediated metabolism of albendazole, astemizole, and terfenadine with IC50 values of 0.31, 0.15, and 2.11 muM, respectively, in human liver microsomes (HLMs). Astemizole 123-133 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 80-86 29759885-6 2018 Danazol, weakly inhibited CYP2J2-mediated metabolism of albendazole and astemizole with IC50 values of 13.8 and 18.3 muM, respectively in HLMs, whereas it strongly inhibited the CYP2J2-mediated ebastine hydroxylase activity in HLMs and HIMs (IC50 = 1.93-1.95 muM). Astemizole 72-82 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 26-32 29759885-1 2018 Cytochrome P450 2J2 (CYP2J2) is involved in the metabolism of drugs, including albendazole, astemizole, ebastine, and endogenous substrates. Astemizole 92-102 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 21-27 29433675-9 2018 RESULTS: In all candidates, plumbagin showed the strongest inhibitory effect on the CYP2J2-mediated astemizole O-demethylation activity. Astemizole 100-110 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 84-90 29655687-5 2018 METHODS: Two representative CYP2J2-specific probe substrates, astemizole and ebastine, were incubated in HLMs with BCA. Astemizole 62-72 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 28-34 29655687-8 2018 RESULTS: BCA inhibited CYP2J2-mediated astemizole O-demethylation and ebastine hydroxylase activities in a concentration dependent manner with Ki values of 2.3 and 3.7 microM, respectively. Astemizole 39-49 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 23-29 28958841-3 2017 Previously, we demonstrated that dronedarone, amiodarone and their main metabolites, namely N-desbutyldronedarone (NDBD) and N-desethylamiodarone (NDEA), potently inhibit human cardiac CYP2J2-mediated astemizole metabolism in vitro. Astemizole 201-211 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 185-191 28237650-4 2017 Additionally, CYP2J2 metabolizes a number of xenobiotics such as astemizole and terfenadine and is potently inhibited by danazol and telmisartan. Astemizole 65-75 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 14-20 26899760-0 2016 Marmoset cytochrome P450 2J2 mainly expressed in small intestines and livers effectively metabolizes human P450 2J2 probe substrates, astemizole and terfenadine. Astemizole 134-144 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 9-28 28461575-3 2017 LKY-047 was demonstrated to be a strong competitive inhibitor of CYP2J2-mediated astemizole O-demethylase and terfenadine hydroxylase activity, with Ki values of 0.96 and 2.61 muM, respectively. Astemizole 81-91 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 65-71 28160853-5 2017 METHOD: Astemizole, a representative CYP2J2 probe substrate, was incubated in HLMs in the presence or absence of acetylshikonin. Astemizole 8-18 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 37-43 28160853-9 2017 RESULTS: Acetylshikonin inhibited CYP2J2-mediated astemizole O-demethylation activity (Ki = 2.1microM) in a noncompetitive manner. Astemizole 50-60 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 34-40 28160853-10 2017 The noncompetitive inhibitory effect of acetylshikonin on CYP2J2 enzyme was also demonstrated using this 3D structure, which showed different binding location of astemizole and acetylshikonin in CYP2J2 model. Astemizole 162-172 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 58-64 28160853-10 2017 The noncompetitive inhibitory effect of acetylshikonin on CYP2J2 enzyme was also demonstrated using this 3D structure, which showed different binding location of astemizole and acetylshikonin in CYP2J2 model. Astemizole 162-172 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 195-201 29911373-3 2017 Additionally, CYP2J2 plays an indispensable role in the intestinal metabolism of various drugs, such as astemizole, terfenadine and ebastine. Astemizole 104-114 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 14-20 26209360-4 2015 Of these, tanshinone IIA dose-dependently and non-competitively inhibited CYP2J2-mediated astemizole O-demethylation activity. Astemizole 90-100 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 74-80 26048912-1 2015 Cytochrome P450 2J2 (CYP2J2) is an enzyme responsible for the metabolism of endogenous substrates including arachidonic acid, as well as therapeutic drugs such as albendazole, astemizole, ebastine, and terfenadine. Astemizole 176-186 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 0-19 26048912-1 2015 Cytochrome P450 2J2 (CYP2J2) is an enzyme responsible for the metabolism of endogenous substrates including arachidonic acid, as well as therapeutic drugs such as albendazole, astemizole, ebastine, and terfenadine. Astemizole 176-186 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 21-27 26048912-4 2015 Of these four CYP2J2 inhibitors, danazol strongly inhibited CYP2J2-mediated albendazole, astemizole, ebastine, and terfenadine metabolism in a substrate-independent manner, with IC50 values of 0.05, 0.07, 0.18, and 0.34 muM, respectively. Astemizole 89-99 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 60-66 26048912-5 2015 Danazol noncompetitively inhibited CYP2J2-mediated astemizole O-demethylation activities with a Ki value of 0.06 muM. Astemizole 51-61 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 35-41 26048912-6 2015 Terfenadone strongly inhibited CYP2J2-mediated albendazole, astemizole, and terfenadine metabolism (IC50 < 0.21 muM), whereas it showed weak inhibition against CYP2J2-catalyzed ebastine hydroxylase activity (IC50 = 6.04 muM). Astemizole 60-70 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 31-37 19923256-1 2010 Several antihistamine drugs including terfenadine, ebastine, and astemizole have been identified as substrates for CYP2J2. Astemizole 65-75 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 115-121 24788058-2 2014 To identify a CYP2J2 inhibitor, 50 natural products obtained from plants were screened using astemizole as a CYP2J2 probe substrate in human liver microsomes. Astemizole 93-103 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 14-20 19923256-7 2010 Extracted ion chromatograms of metabolites observed for albendazole, amiodarone, astemizole, thioridazine, mesoridazine, and danazol showed marked differences in the regioselectivity of CYP2J2 and CYP3A4. Astemizole 81-91 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 186-192 24788058-2 2014 To identify a CYP2J2 inhibitor, 50 natural products obtained from plants were screened using astemizole as a CYP2J2 probe substrate in human liver microsomes. Astemizole 93-103 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 109-115 24788058-3 2014 Of these, decursin noncompetitively inhibited CYP2J2-mediated astemizole O-demethylation and terfenadine hydroxylation activities with Ki values of 8.34 and 15.8muM, respectively. Astemizole 62-72 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 46-52 24021950-10 2013 CYP2J2 activity in the cell line was inhibited by danazol, astemizole, and ketoconazole in submicromolar range, but also by xenobiotics known to cause cardiac adverse effects. Astemizole 59-69 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 0-6 22328583-1 2012 CYP2J2, an arachidonic acid epoxygenase, is recognized for its role in the first-pass metabolism of astemizole and ebastine. Astemizole 100-110 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 0-6 22328583-6 2012 To identify a specific CYP2J2 inhibitor, 138 drugs were screened using terfenadine and astemizole as probe substrates with recombinant CYP2J2. Astemizole 87-97 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 23-29 22328583-11 2012 Thus, danazol, amiodarone, and astemizole will facilitate the ability to determine the metabolic role of CYP2J2 in hepatic and extrahepatic tissues. Astemizole 31-41 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 105-111 20926621-11 2011 Formation of M20 by human liver microsomes was inhibited 89% by ketoconazole, 75% by astemizole (a CYP2J2 inhibitor), and 43% by CYP3A4 monoclonal antibody. Astemizole 85-95 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 99-105 12386130-0 2002 Involvement of CYP2J2 on the intestinal first-pass metabolism of antihistamine drug, astemizole. Astemizole 85-95 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 15-21 12851038-11 2003 All the chemicals inhibited astemizole O-demethylation in recombinant CYP2J2 microsomes. Astemizole 28-38 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 70-76 12851038-12 2003 The results suggest that CYP2J2 is involved in astemizole O-demethylation in both the human small intestine and liver; however, the contribution in the liver is lower than in the small intestine. Astemizole 47-57 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 25-31 12386130-7 2002 A clear activity of astemizole O-demethylation was detected in recombinant CYP2J2 with K(m) = 0.65 microM and V(max) = 1129 pmol/nmol P450/min. Astemizole 20-30 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 75-81 12386130-9 2002 Expression levels of the immunoreactive protein with the CYP2J2 antibody in the small intestine were well correlated with the activities of the astemizole O-demethylation (r = 0.901, n = 5, p < 0.05). Astemizole 144-154 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 57-63 12386130-10 2002 The CYP2J2 substrates, arachidonic acid and ebastine, strongly inhibited the microsomal astemizole O-demethylation in the human small intestines and recombinant CYP2J2. Astemizole 88-98 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 4-10 12386130-10 2002 The CYP2J2 substrates, arachidonic acid and ebastine, strongly inhibited the microsomal astemizole O-demethylation in the human small intestines and recombinant CYP2J2. Astemizole 88-98 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 161-167 12386130-11 2002 These results indicate the involvement of CYP2J2 in the presystemic elimination of astemizole in the human small intestine. Astemizole 83-93 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 42-48