Results 151 to 160 of about 297,833 (301)

Engineering yeast model for study of the metabolism of cytochrome P450-3A4

, 2005
A stable engineering yeast model with high expression of human NADPH-P450 reductase (hCPR) was established in the present study. A new plasmid used to insert hCPR in the chromosome of S.cerevisiae was constructed.
程婕, 龚毅, 杨凌
core  

Repurposing Drugs for Malaria through a Human Dose Prediction: A Case Study with Berzosertib

Clinical Pharmacology &Therapeutics, EarlyView.
Repurposing drugs whose clinical safety has been established offers a valuable approach to reduce the cost and time associated with the development of new drugs for malaria. Here, we investigate the potential to repurpose the anticancer kinase inhibitor berzosertib for the treatment of malaria, by assessing whether a predicted efficacious human dose ...
Devasha Redhi, Mwila Mulubwa, Mmakwena M. Mmonwa, Mathew Njoroge, Liezl Krugmann, Kelly Chibale   +5 more
wiley   +1 more source

Characterization of Lysosomal Hydrolases and Transporters and Their Age‐Dependent Variability: Relevance to Drug Metabolism and Transport of Small Molecule and Biologic Drugs

Clinical Pharmacology &Therapeutics, EarlyView.
Lysosomes play a key role in the accumulation, catabolism, and transport of endogenous and exogenous metabolites and proteins and are involved in drug metabolism and prodrug activation. However, the protein abundance and interindividual variability of lysosomal drug‐metabolizing enzymes and transporters (DMETs) remain underexplored.
Darshak Gadara, Dilip Kumar Singh, Sandhya Subash, Guihua Yue, Deepak Ahire, Chris Bohl, Maciej Czerwinski, Stephanie Helmstetter, Scott Heyward, Robert S. Jones, Cyrus Khojasteh, Ryota Kikuchi, Priyanka Kulkarni, Bin Ma, Bernard Murray, Chris Seib, Bill Smith, David M. Stresser, Mitchell E. Taub, Ting Wang, Bhagwat Prasad   +20 more
wiley   +1 more source

Cytochrome P450-based toxicity research of Pyrrolizidine alkaloids

, 2007
Pyrrolizidine alkaloids were considered as the essential components in the toxicity of some composite plants. The previous study suggested that cytochrome P450 (CYPs)–mediated bioactivation and succedent formation of DNA adducts triggered toxicity of ...
张江伟, 何芋岐, 刘勇, 杨凌, 杨丽, 王峥涛   +5 more
core  

Virtual Twin Approach Using Physiologically Based Pharmacokinetic Modeling to Support Precision Dosing of Valproic Acid in Geriatric Patients

Clinical Pharmacology &Therapeutics, EarlyView.
Personalized dosing is particularly important for drugs with narrow therapeutic indices in geriatric patients, who exhibit substantial physiological variability and limited pharmacokinetic (PK) evidence to guide individualized dose selection. Valproic acid (VPA) is an effective treatment option for bipolar disorder in older adults, yet dosing largely ...
Yoo Jin Jang, Dong‐Gyu Heo, Eunjin Hong   +2 more
wiley   +1 more source

Endothelial cytochrome P450 -derived cholesterol limits angiogenesis. [PDF]

Redox Biol
Malacarne PF, Lopez M, Chatterjee S, Herrle N, Weiss L, Günther S, Osborne T, Glaubitz C, Schmid T, Kurrle N, Schnütgen F, Lütjohann D, Brandes RP, Rezende F.   +13 more
europepmc   +1 more source

Identification of a Functional CYP2C8 Variant Allele that Alters Splicing, Reduces Protein Expression, and Increases Drug Exposure

Clinical Pharmacology &Therapeutics, EarlyView.
This study investigated genetic determinants of the pharmacokinetics of the CYP2C8 index drugs repaglinide and gemfibrozil, and their interaction in healthy participants. Sequencing data from a study with montelukast revealed a novel functional CYP2C8 allele (rs2071426, CYP2C8*19), predicted to create an intronic splice donor site.
Anssi J. H. Mykkänen, Päivi Hirvensalo, Kathrin Klein, Dorota Kaminska, Markus Grube, Tuija Tapaninen, Johanna I. Kiiski, Mikko Neuvonen, Ville T. Männistö, Jussi Pihlajamäki, Mladen Tzvetkov, Matthias Schwab, Aleksi Tornio, Janne T. Backman, Mikko Niemi   +14 more
wiley   +1 more source

Clinical Characterization of Enzyme and Transporter Precipitants to Evaluate Drug–Drug Interactions for Orforglipron, a Small Molecule Glucagon‐Like Peptide‐1 Receptor Agonist

Clinical Pharmacology &Therapeutics, EarlyView.
Orforglipron is an orally administered, small‐molecule glucagon‐like peptide‐1 receptor agonist in clinical development for the treatment of type 2 diabetes and obesity. Orforglipron is a substrate of CYP3A4, organic anion transporting polypeptides (OATPs) 1B/1B3, and P‐glycoprotein (P‐gp); however, precipitants commonly used to define these mechanisms
Bridget L. Morse, David E. Coutant, Xiaosu Ma, Sohini Raha, Keerthan Aithal, Clare Nicoll, Luc R. A. Rougée, Shobha Bhattachar   +7 more
wiley   +1 more source

ATTNSOM: learning cross-isoform attention for cytochrome P450 site-of-metabolism prediction. [PDF]

Bioinformatics
Kim H, Lee E, Chung S, Park J, Baek S, Kang J.   +5 more
europepmc   +1 more source

Influence of paraoxonase-1 Q192R and cytochrome P450 2C19 polymorphisms on clopidogrel response

, 2012
Rolf P Kreutz1,2, Perry Nystrom2, Yvonne Kreutz2, Jia Miao2, Zeruesenay Desta2, Jeffrey A Breall1, Lang Li2, ChienWei Chiang2, Richard Kovacs1, David A Flockhart2, Yan Jin21Krannert Institute of Cardiology, 2Division of Clinical Pharmacology, Indiana ...
Breall JA, Desta Z, Flockhart DA, Nystrom P, Chiang C, Kreutz RP, Kreutz Y, Kovacs R, Jin Y, Li L, Miao J   +10 more
core