Results 91 to 100 of about 56,066 (278)

A new pathway for phosphatidylserine synthesis in rat liver microsomes [PDF]

, 1988
It has been shown that the phosphate moiety of glycerophosphate is incorporated into phosphatidylserine of rat liver microsomes, but not of mitochondria. The reaction is dependent on CMP.
Baraǹska, Jolanta, Jolanta Baraǹska
core   +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

Beyond-Rule-of-Five Compounds Are Not Different: In Vitro–In Vivo Extrapolation of Female CD-1 Mouse Clearance Based on Merck Healthcare KGaA Compound Set

Pharmaceuticals
Background: Extrapolation of intrinsic clearance from in vitro systems such as liver microsomes or hepatocytes is an established approach to predict clearance in preclinical species and in humans.
Christine K. Maurer, Zhizhou Fang, Heide M. Duevel, Stephanie Harlfinger, Carl Petersson   +4 more
doaj   +1 more source

UGT1A6 and UGT1A9 involving in the metabolism of daphnetin by human liver microsomes

, 2009
Daphnetin (7, 8-dihydroxycoumarin), one of coumarin derivatives, is the major bioactive constituent from Daphne odora (Thymelaeaceae). Previous studies indicated that daphnetin has the anti-coagulant activity like other coumarin analogs, and other ...
梁思成, 葛广波, Yang L, 杨凌, 刘慧鑫   +4 more
core  

Do Brain Extracellular Fluid Concentrations Predict PET‐Inferred Receptor Occupancy in Human CNS? A Mechanistic Model‐Based Analysis of Dopamine D2 Receptor Ligands

Clinical Pharmacology &Therapeutics, EarlyView.
A mechanistic CNS PBPK model framework was applied to eight antipsychotic D2 receptor ligands, comparing brain extracellular fluid (brainECF) and brain cell membrane (brainM) as biophase for predicting human receptor occupancy compared against PET neuroimaging data. BrainM concentrations showed improved agreement with PET‐derived receptor occupancy for
Divakar Budda, J.G. Coen van Hasselt, Elizabeth C.M. de Lange   +2 more
wiley   +1 more source

Influence of butylcaptax and Dropp on the phospholipid composition and lipid peroxidation (LPO) in the liver mitochondria and microsomes of pregnant rats and their embryos [PDF]

Caspian Journal of Environmental Sciences
This study investigates the effects of the defoliants butylcaptax and Dropp on the phospholipid composition and lipid peroxidation (LPO) in the liver mitochondria and microsomes of pregnant rats and their embryos.
Dilfuza Tuychiyeva, Parida Mirkhamidova, Gulnara Shakhmurova, Rano Alimova, Gafurzhon Mukhamedov, Xusniddin Karimov, Nurxon Moydinova, Mavjuda Rakhmatullayeva, Maxliyo Sattorova, Salomat Almardanova   +9 more
doaj   +1 more source

Metabolism of tyrosine kinase inhibitor cabozantinib by rat liver microsomes [PDF]

, 2019
Cabozantinib is an anticancer drug that was approved for treatment of progressive thyroid cancer by FDA and EMA organizations. Cabozantinib is a tyrosine kinase inhibitor. It blocks signal pathway receptors that are important for growth of tumors.
Jurečka, Tomáš
core  

Physiologically Based Pharmacokinetic Modeling to Assess Transporter‐Mediated Drug–Drug Interactions in Support of Labeling Recommendations for Zavegepant Nasal Spray

Clinical Pharmacology &Therapeutics, EarlyView.
Zavegepant nasal spray, a calcitonin gene‐related peptide receptor antagonist indicated for acute treatment of migraine with or without aura in adults, is a substrate for organic anion transporting polypeptide 1B3 (OATP1B3), Na+/taurocholate cotransporting polypeptide (NTCP), P‐glycoprotein (P‐gp), and cytochrome P450 3A4 (CYP3A4).
Alice Ke, Ernesto Callegari, Manthena V.S. Varma, Mayur K Ladumor, Chieko Muto, Richard J. Bertz, Hannah M. Jones, Vaishali Sahasrabudhe, Jing Liu   +8 more
wiley   +1 more source

Activation of HMG-CoA reductase by microsomal phosphatase

Journal of Lipid Research, 1983
HMG-CoA reductase activity can be modulated by a reversible phosphorylation-dephosphorylation with the phosphorylated form of the enzyme being inactive and the dephosphorylated form, active. Phosphatases from diverse sources, including cytosol, have been
K R Feingold, M H Wiley, A H Moser, S R Lear, M D Siperstein   +4 more
doaj   +1 more source

From Prediction to Decision Making: PBPK and QSP as Regulatory‐Grade NAMs

Clinical Pharmacology &Therapeutics, EarlyView.
New approach methodologies (NAMs) encompass a diverse and rapidly evolving set of experimental and computational tools designed to generate human‐relevant mechanistic data for use in drug development and regulatory decision making. Experimental NAMs provide insights into drug disposition, pharmacological activity, and disease biology that are difficult
Karen Rowland Yeo, Piet H. van der Graaf
wiley   +1 more source