Results 41 to 50 of about 1,677,689 (317)

Direct Oxidation and Covalent Binding of Isoniazid to Rodent Liver and Human Hepatic Microsomes: Humans Are More Like Mice than Rats

Chemical Research in Toxicology, 2012
Isoniazid (INH) is associated with serious liver injury and autoimmunity. Classic studies in rats indicated that a reactive metabolite of acetylhydrazine is responsible for the covalent binding and toxicity of INH.
Imir G. Metushi, T. Nakagawa, J. Uetrecht   +2 more
semanticscholar   +1 more source

The ATM Kinase Inhibitor AZD0156 Is a Potent Inhibitor of Plasmodium Phosphatidylinositol 4‐Kinase (PI4Kβ) and Is an Attractive Candidate for Medicinal Chemistry Optimization Against Malaria

Angewandte Chemie, EarlyView.
AZD0156, an ATM kinase inhibitor in clinical development, shows promising multistage antiplasmodial activity by targeting Plasmodium falciparum phosphatidylinositol 4‐kinase (PfPI4Kβ). With an improved specificity profile relative to other PfPI4Kβ inhibitors and moderate efficacy in a P.
John G. Woodland, Dina Coertzen, Kathryn J. Wicht, Virginia Franco Hidalgo, Charisse Flerida A. Pasaje, Luiz C. Godoy, Tarrick Qahash, Mmakwena M. Mmonwa, Godwin A. Dziwornu, Lynn Wambua, Sarah Harries, Constance M. Korkor, Mathew Njoroge, Liezl Krugmann, Dale Taylor, Meta Leshabane, Henrico Langeveld, Tayla Rabie, Janette Reader, Mariëtte van der Watt, Nelius Venter, Erica Erlank, Ayesha S. Aswat, Lizette L. Koekemoer, Tomas Yeo, Jin H. Jeon, David A. Fidock, Francisco Javier Gamo, Sergio Wittlin, Jacquin C. Niles, Manuel Llinas, Lauren B. Coulson, Lyn‐Marié Birkholtz, Kelly Chibale   +33 more
wiley   +2 more sources

Morphine Metabolism in Human Skin Microsomes [PDF]

, 2012
For patients with severe skin wounds, topically applied morphine is an option to induce efficient analgesia due to the presence of opioid receptors in the skin.
Heilmann, S., Küchler, Sarah, Schäfer-Korting, Monika   +2 more
core   +2 more sources

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

3‐Oxabicyclo[3.1.1]heptane as an Isostere of meta‐Benzene

Angewandte Chemie, EarlyView.
3‐Oxabicyclo[3.1.1]heptanes were designed as saturated isosteres of meta‐benzene. Crystallographic analysis revealed that these structures and meta‐benzene have identical geometric properties. Replacement of the central benzene ring in the anticancer drug Sonidegib with 3‐oxabicyclo[3.1.1]heptane provided a patent‐free analogue with a nanomolar potency,
Dmitry Dibchak, Pavel K. Mykhailiuk
wiley   +2 more sources

Physiology-based IVIVE predictions of tramadol from in vitro metabolism data [PDF]

, 2014
To predict the tramadol in vivo pharmacokinetics in adults by using in vitro metabolism data and an in vitro-in vivo extrapolation (IVIVE)-linked physiologically-based pharmacokinetic (PBPK) modeling and simulation approach (SimcypA (R)).
Allegaert, Karel, Annaert, Pieter, Boussery, Koen, Colin, Pieter, Cuyckens, Filip, Mannens, Geert, Snoeys, Jan, T'jollyn, Huybrecht, Van Bocxlaer, Jan, Van Peer, Achiel, Vermeulen, An   +10 more
core   +1 more source

NAFLD‐related hepatocellular carcinoma: The growing challenge

Hepatology, EarlyView., 2022
Risk and protective factors for NAFLD‐related hepatocellular carcinoma Abstract Hepatocellular carcinoma (HCC) is a common cause of cancer‐related mortality and morbidity worldwide. With the obesity pandemic, NAFLD‐related HCC is contributing to the burden of disease exponentially.
Pir Ahmad Shah, Rashmee Patil, Stephen A. Harrison   +2 more
wiley   +1 more source

Effect of blood plasma lipoproteins on hydroxylation of benzo[a]pyrene in liver microsomes of rats

Атеросклероз, 2020
This work presents the characteristics of the catalytic activity of hydroxylation of benzo[a] pyrene (B[a]P) in rat liver microsomes using plasma lipoproteins (LP) (VLDL, LDL, HDL) as transport forms of B[a]P.
L. M. Polyakov, R. A. Knyazev, N. V. Trifonova, M. V. Kotova, E. I. Solovyova, A. V. Ryabchenko   +5 more
doaj   +1 more source

Qualification of Human Liver Microsomes for Antibacterial Activity Screening of Drug Metabolites

Applied Microbiology, 2023
Microsomes are commonly used to perform in vitro drug metabolism, predominantly to form phase I drug metabolites. Pooled microsomes from multiple donors can contain microorganisms from underlying microbial diseases.
Navid Jubaer
doaj   +1 more source

Liver segmentation and metastases detection in MR images using convolutional neural networks [PDF]

J. Med. Imag. 6(4), 044003 (2019), 2019
Primary tumors have a high likelihood of developing metastases in the liver and early detection of these metastases is crucial for patient outcome. We propose a method based on convolutional neural networks (CNN) to detect liver metastases. First, the liver was automatically segmented using the six phases of abdominal dynamic contrast enhanced (DCE) MR
arxiv   +1 more source