Results 21 to 30 of about 27,101 (273)

Regioselective Hydroxylation of Phloretin, a Bioactive Compound from Apples, by Human Cytochrome P450 Enzymes

Pharmaceuticals, 2020
Phloretin, the major polyphenol compound in apples and apple products, is interesting because it shows beneficial effects on human health. It is mainly found as a form of glucoside, phlorizin. However, the metabolic pathway of phloretin in humans has not
Ngoc Anh Nguyen, Ngoc Tan Cao, Thi Huong Ha Nguyen, Thien-Kim Le, Gun Su Cha, Soo-Keun Choi, Jae-Gu Pan, Soo-Jin Yeom, Hyung-Sik Kang, Chul-Ho Yun   +9 more
doaj   +1 more source

Stereoselective glucuronidation of formoterol by human liver microsomes [PDF]

British Journal of Clinical Pharmacology, 2000
Aims Formoterol is a β2‐adrenoceptor agonist marketed as a racemic mixture of the active (R; R)‐ and inactive (S; S)‐enantiomers (rac‐formoterol). The drug produces prolonged bronchodilation by inhalation but there is significant interpatient variability in duration of effect.
M, Zhang, J P, Fawcett, J M, Kennedy, J P, Shaw   +3 more
openaire   +2 more sources

Analysis of in vitro and in vivo metabolism of zidovudine and gemfibrozil in trans‐chromosomic mouse line expressing human UGT2 enzymes

Pharmacology Research & Perspectives, 2022
UDP‐glucuronosyltransferases (UGTs) catalyze the conjugation of various substrates with sugars. Since the UGT2 family forms a large cluster spanning 1.5 Mb, transgenic mouse lines carrying the entire human UGT2 family have not been constructed because of
Kaoru Kobayashi, Tsuneo Deguchi, Satoshi Abe, Naoyo Kajitani, Kanako Kazuki, Shoko Takehara, Kazuomi Nakamura, Atsushi Kurihara, Mitsuo Oshimura, Yasuhiro Kazuki   +9 more
doaj   +1 more source

Intestinal peroxisome proliferator‐activated receptor α‐fatty acid‐binding protein 1 axis modulates nonalcoholic steatohepatitis

Hepatology, EarlyView., 2022
Abstract Background and Aims Peroxisome proliferator‐activated receptor α (PPARα) regulates fatty acid transport and catabolism in liver. However, the role of intestinal PPARα in lipid homeostasis is largely unknown. Here, intestinal PPARα was examined for its modulation of obesity and NASH. Approach and Results Intestinal PPARα was activated and fatty
Tingting Yan, Yuhong Luo, Nana Yan, Keisuke Hamada, Nan Zhao, Yangliu Xia, Ping Wang, Changdong Zhao, Dan Qi, Shoumei Yang, Lulu Sun, Jie Cai, Qiong Wang, Changtao Jiang, Oksana Gavrilova, Kristopher W. Krausz, Daxesh P. Patel, Xiaoting Yu, Xuan Wu, Haiping Hao, Weiwei Liu, Aijuan Qu, Frank J. Gonzalez   +22 more
wiley   +1 more source

In vitro metabolic characterization of the SARS-CoV-2 papain-like protease inhibitors GRL0617 and HY-17542

Frontiers in Pharmacology, 2023
The SARS-CoV-2 pandemic requires a new therapeutic target for viral infection, and papain-like protease (Plpro) has been suggested as a druggable target.
Hyunki Cho, Hyunki Cho, Young Jun Kim, Jung-Woo Chae, Markus R. Meyer, Sang Kyum Kim, Chang Seon Ryu   +6 more
doaj   +1 more source

Loss of hepatic SMLR1 causes hepatosteatosis and protects against atherosclerosis due to decreased hepatic VLDL secretion

Hepatology, EarlyView., 2022
The role of SMLR1 in lipid metabolism (high fat + cholesterol diet in mice) Abstract Background and Aims The assembly and secretion of VLDL from the liver, a pathway that affects hepatic and plasma lipids, remains incompletely understood. We set out to identify players in the VLDL biogenesis pathway by identifying genes that are co‐expressed with the ...
Willemien van Zwol, Antoine Rimbert, Justina C. Wolters, Marieke Smit, Vincent W. Bloks, Niels J. Kloosterhuis, Nicolette C. A. Huijkman, Mirjam H. Koster, Umesh Tharehalli, Simon M. de Neck, Colin Bournez, Marceline M. Fuh, Jeroen Kuipers, Sujith Rajan, Alain de Bruin, Henry N. Ginsberg, Gerard J. P. van Westen, M. Mahmood Hussain, Ludger Scheja, Joerg Heeren, Philip Zimmerman, Bart van de Sluis, Jan Albert Kuivenhoven   +22 more
wiley   +1 more source

Dual effects of ketoconazole cis-enantiomers on CYP3A4 in human hepatocytes and HepG2 Cells. [PDF]

PLoS ONE, 2014
Antifungal drug ketoconazole causes severe drug-drug interactions by influencing gene expression and catalytic activity of major drug-metabolizing enzyme cytochrome P450 CYP3A4.
Aneta Novotná, Kristýna Krasulová, Iveta Bartoňková, Martina Korhoňová, Petr Bachleda, Pavel Anzenbacher, Zdeněk Dvořák   +6 more
doaj   +1 more source

Interspecies Variation in NCMN-O-Demethylation in Liver Microsomes from Various Species

Molecules, 2019
NCMN (N-(3-carboxy propyl)-4-methoxy-1,8-naphthalimide), a newly developed ratiometric two-photon fluorescent probe for human Cytochrome P450 1A (CYP1A), shows the best combination of specificity and reactivity for real-time detection of the enzymatic ...
Ziru Dai, Guibo Sun, Jiada Yang, Jie Hou, Ping Zhou, Weijie Xie, Guangbo Ge, Xiaobo Sun, Ling Yang   +8 more
doaj   +1 more source

Debrisoquine metabolism and CYP2D expression in marmoset liver microsomes

, 2011
The objective of this study was to define CYP2D enzymes in marmoset (Callithrix jacchus) liver microsomes, both at the activity level using debrisoquine as the model substrate and at the protein level using antibodies raised to human CYP2D6.
Costas Ioannides, Cybulski, ZR, S. W. Annie Bligh, Hall, M, Hall, M., Ioannides, C., Ioannides, C, Cooke, B.R., Brian R. Cooke, Michael Hall, Z. Richard Cybulski, Cooke, BR, Cybulski, Z.R., Bligh, SW, Bligh, S.W.A.   +14 more
core   +2 more sources

In Vitro Phase I Metabolism of CRV431, a Novel Oral Drug Candidate for Chronic Hepatitis B

Pharmaceutics, 2017
The cytochrome P450-mediated Phase I in vitro metabolism of CRV431 was studied using selective chemical inhibition and recombinant human enzymes. Additionally, the metabolic profile of CRV431 in human, rat, and monkey liver microsomes was investigated ...
Daniel J. Trepanier, Daren R. Ure, Robert T. Foster   +2 more
doaj   +1 more source