Results 91 to 100 of about 2,738,308 (324)

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

Towards the Development of an In vivo Chemical Probe for Cyclin G Associated Kinase (GAK)

Molecules, 2019
SGC-GAK-1 (1) is a potent, selective, cell-active chemical probe for cyclin G-associated kinase (GAK). However, 1 was rapidly metabolized in mouse liver microsomes by cytochrome P450-mediated oxidation, displaying rapid clearance in liver microsomes and ...
Christopher R. M. Asquith, James M. Bennett, Lianyong Su, Tuomo Laitinen, Jonathan M. Elkins, Julie E. Pickett, Carrow I. Wells, Zengbiao Li, Timothy M. Willson, William J. Zuercher   +9 more
doaj   +1 more source

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

Lipid composition and turnover of rough and smooth microsomal membranes in rat liver

Journal of Lipid Research, 1968
Subfractions of rat liver microsomes (rough, smooth I, and smooth II), isolated in a cation-containing sucrose gradient system, were analyzed. After removal of adsorbed and luminal protein, these subfractions had the same phospholipid/protein ratio ...
Hans Glaumann, Gustav Dallner
doaj   +1 more source

Resolution of the cytochrome P-450-containing omega-hydroxylation system of liver microsomes into three components.

Journal of Biological Chemistry, 1969
The enzyme system in liver microsomes which catalyzes the ω-hydroxylation of fatty acids in the presence of molecular oxygen and a reduced pyridine nucleotide has been solubilized and resolved into fractions containing cytochrome P-450, a cytochrome P ...
Anthony Y. H. Lu, Karen W. Junk, M. J. Coon   +2 more
semanticscholar   +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

Studies on acyl-coenzyme A: cholesterol acyltransferase activity in human liver microsomes.

Journal of Lipid Research, 1989
The aim of the present study was to characterize the acyl-coenzyme A: cholesterol acyltransferase (ACAT) activity in human liver microsomes. Liver biopsies were obtained from patients undergoing elective cholecystectomy under highly standardized ...
K Einarsson, L Benthin, S Ewerth, G Hellers, D Ståhlberg, B Angelin   +5 more
doaj   +1 more source

Role of hemoprotein P-450 in fatty acid omega-hydroxylation in a soluble enzyme system from liver microsomes.

Journal of Biological Chemistry, 1968
An enzyme system which catalyzes the ω-hydroxylation of fatty acids in the presence of reduced triphosphopyridine nucleotide and molecular oxygen has been obtained in a soluble form from rabbit liver microsomes.
Anthony Y. H. Lu, M. J. Coon
semanticscholar   +1 more source

Progress report on new epilepsy treatments: A summary of the Eighteenth Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XVIII). II. Treatments in more advanced clinical development

Epilepsia, EarlyView.
Abstract This article summarizes data for 13 investigational treatments for which at least preliminary seizure outcome data in patients with epilepsy were reported at the Eighteenth Eilat Conference on New Antiepileptic Drugs and Devices held in Madrid, Spain, on May 3–6, 2026.
Meir Bialer, Cecilie Johannessen Landmark, Matthias J. Koepp, Emilio Perucca, Piero Perucca, Torbjörn Tomson, H. Steve White, Elaine Wirrell   +7 more
wiley   +1 more source

EROD and MROD as Markers of Cytochrome P450 1A Activities in Hepatic Microsomes from Entire and Castrated Male Pigs

Sensors, 2009
In the present study, we characterized the kinetic parameters of 7-ethoxy-resorufin O-deethylation (EROD) and 7-methoxyresorufin O-demethylation (MROD) in hepatic microsomes from entire and castrated male pigs.
Vladimir Zlabek, Galia Zamaratskaia
doaj   +1 more source