Results 21 to 30 of about 50,120 (254)

In vitro metabolism, reaction phenotyping, enzyme kinetics, CYP inhibition and induction potential of ataluren

Pharmacology Research & Perspectives, 2020
Ataluren promotes ribosomal readthrough of premature termination codons in mRNA which result from nonsense mutations. In vitro studies were performed to characterize the metabolism and enzyme kinetics of ataluren and its interaction potential with CYP ...
Ronald Kong, Jiyuan Ma, Seongwoo Hwang, Young‐Choon Moon, Ellen M. Welch, Marla Weetall, Joseph M. Colacino, Neil Almstead, John Babiak, Elizabeth Goodwin   +9 more
doaj   +1 more source

Study on In Vitro Metabolism and In Vivo Pharmacokinetics of Beauvericin

Toxins, 2022
Beauvericin (BEA) is a well-known mycotoxin produced by many fungi, including Beaveria bassiana. The purpose of this study was to evaluate the in vitro distribution and metabolism characteristics as well as the in vivo pharmacokinetic (PK) profile of BEA.
Yu Yuan, Guangpeng Meng, Yuanbo Li, Chunjie Wu   +3 more
doaj   +1 more source

Studies on the inhibitory effect of isavuconazole on flumatinib metabolism in vitro and in vivo

Frontiers in Pharmacology, 2023
As the validated agent for the treatment of chronic myelogenous leukemia (CML), flumatinib is a novel oral tyrosine kinase inhibitor (TKI) with higher potency and selectivity for BCR-ABL1 kinase compared to imatinib.
Ya-nan Liu, Ya-nan Liu, Xinhao Xu, Xinhao Xu, Jingjing Nie, Jingjing Nie, Yingying Hu, Xuegu Xu, Ren-ai Xu, Xiaoxiang Du   +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

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

Characterization of iodothyronine sulfatase activities in human and rat liver and placenta [PDF]

, 2002
In conditions associated with high serum iodothyronine sulfate concentrations, e.g. during fetal development, desulfation of these conjugates may be important in the regulation of thyroid hormone homeostasis. However, little is known
Coughtrie, M.W., Dijk, C.H. (Caren) van, Kaptein, E. (Ellen), Kester, M.H.A. (Monique), Roest, T.J. (Thirza), Tibboel, D. (Dick), Visser, T.J. (Theo)   +6 more
core   +3 more sources

Nontargeted Metabolomics by High-Resolution Mass Spectrometry to Study the In Vitro Metabolism of a Dual Inverse Agonist of Estrogen-Related Receptors β and γ, DN203368

Pharmaceutics, 2021
DN203368 ((E)-3-[1-(4-[4-isopropylpiperazine-1-yl]phenyl) 3-methyl-2-phenylbut-1-en-1-yl] phenol) is a 4-hydroxy tamoxifen analog that is a dual inverse agonist of estrogen-related receptor β/γ (ERRβ/γ).
Sin-Eun Kim, Seung-Bae Ji, Euihyeon Kim, Minseon Jeong, Jina Kim, Gyung-Min Lee, Hyung-Ju Seo, Subin Bae, Yeojin Jeong, Sangkyu Lee, Sunghwan Kim, Taeho Lee, Sung Jin Cho, Kwang-Hyeon Liu   +13 more
doaj   +1 more source

3-hydroxy-3-methylglutaryl coenzyme A reductase in human liver microsomes: active and inactive forms and cross-reactivity with antibody against rat liver enzyme.

Journal of Lipid Research, 1984
3-Hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the enzyme catalyzing the rate-limiting step in cholesterol biosynthesis, exists in one active (dephosphorylated) and one inactive (phosphorylated) form in liver microsomes obtained from several ...
B Angelin, K Einarsson, L Liljeqvist, K Nilsell, RA Heller   +4 more
doaj   +1 more source

Characterization of the human omega-oxidation pathway for omega-hydroxy-very-long-chain fatty acids [PDF]

, 2008
Very-long-chain fatty acids (VLCFAs) have long been known to be degraded exclusively in peroxisomes via beta-oxidation. A defect in peroxisomal beta-oxidation results in elevated levels of VLCFAs and is associated with the most frequent inherited ...
Dacremont, Georges, Kemp, Stephan, Ofman, Rob, Sanders, Robert-Jan, Wanders, Ronald J. A.   +4 more
core   +2 more sources

Identification and interspecies characterization of UDP-glucuronosyltransferase isoforms catalyzing acacetin glucuronidation using recombinant UGT enzymes and microsomes

Journal of Traditional Chinese Medical Sciences, 2019
Objective: To explore the glucuronic acid metabolism of acacetin in human liver and intestinal microsomes to better characterize human uridine 5′-diphospho (UDP)-glucuronosyltransferase (UGT) isoforms. In addition, interspecies comparisons were performed
Kangle Shi, Shan Li, Qinggang Meng
doaj   +1 more source