Results 61 to 70 of about 24,113 (256)

A Facile Protocol for C(sp2)–C(sp3) Bond Formation Reactions Toward Functionalized E3 Ligase Ligands

ChemMedChem, EarlyView.
A robust C(sp2)–C(sp3) decarboxylative coupling strategy enables access to new CRBN ligands and degraders with improved physicochemical properties. This synthetic approach is expanding the chemical space beyond C(sp2)–N linkages, fine‐tuning proteolysis‐targeting chimera activities and unlocking previously inaccessible degrader chemotypes.
Anita Maksutova, Thomas M. Geiger, Lorenzo Cianni, Dominika E. Pieńkowska, Jan Gerhartz, Lina Read, Aleša Bricelj, Alexander Herrmann, Maurice Leon Nelles, Yuen Lam Dora Ng, Marcus D. Hartmann, Jan Krönke, Izidor Sosič, Radosław P. Nowak, Michael Gütschow, Christian Steinebach   +15 more
wiley   +1 more source

Effects of glycyrrhizin on the pharmacokinetics of asiatic acid in rats and its potential mechanism

Pharmaceutical Biology, 2018
Context: Asiatic acid has been reported to possess a wide range of pharmacological activities. Objective: This study investigates the effects of glycyrrhizin on the pharmacokinetics of asiatic acid in rats and its potential mechanism.
Ling Guo, Ying Cui, Kaijun Hao
doaj   +1 more source

Antimutagenic effect of essential oil of sage (Salvia officinalis L.) and its fractions against UV-induced mutations in bacterial and yeast cells [PDF]

Archives of Biological Sciences, 2005
The inhibition of spontaneous and UV-induced mutations by essential oil (EO) of sage (Salvia officinalis L.) and its fractions F1-F5 containing different proportions of mono- and sesquiterpenes was studied with the Salmonella/microsome, E.
Knežević-Vukčević Jelena B., Vuković-Gačić Branka S., Stević Tatjana, Stanojević Jasna, Nikolić Biljana, Simić Draga   +5 more
doaj   +1 more source

Changes of microsomal membrane compositions modulate microsomal enzyme activity [PDF]

Pediatric Research, 1979
We have shown previously, that the activity of cerebrosulfotransferase (CST) a microsomal enzyme involved in myelin synthesis is modulated in vitro by the cholesterol-phospholipid ratio (C/P) in microsomal membranes. To further investigate this mechanism, we studied two different models: 1.) Removal of cholesterol by phospholipid micelles and 2 ...
N Herschkowitz, H P Siegrist, H Jutzi, U Wiesmann   +3 more
openaire   +1 more source

Clinical Study to Evaluate Drug Interactions of Cannabidiol with Citalopram and Morphine in Healthy Adults

Clinical Pharmacology &Therapeutics, EarlyView.
Cannabidiol (CBD) is one of the most abundant bioactive cannabinoids. Research has demonstrated CBD’s ability to inhibit metabolic enzymes like cytochrome P450 (CYP) and UDP‐glucuronosyltransferase (UGT), potentially leading to drug interactions. However, clinical knowledge gaps remain, particularly with regard to drugs that are more commonly taken by ...
Pablo Salcedo, Donna A. Volpe, Anik Chaturbedi, Aanchal Shah, Ashok Krishna, Paula L Hyland, Giri Vegesna, Cheng‐Hui Hsiao, Ryan De Palma, Melanie Fein, Rodney Rouse, Jeffry Florian   +11 more
wiley   +1 more source

Comparative chemical and biological hydrolytic stability of homologous esters and isosteres

Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Esters are one of the major functional groups present in the structures of prodrugs and bioactive compounds. Their presence is often associated with hydrolytic lability.
Hygor M. R. de Souza, Jéssica S. Guedes, Rosana H. C. N. Freitas, Luis G. V. Gelves, Harold H. Fokoue, Carlos Mauricio R. Sant’Anna, Eliezer J. Barreiro, Lidia M. Lima   +7 more
doaj   +1 more source

Interpretation of in vitro concentration‐response data for risk assessment and regulatory decision‐making: Report from the 2022 IWGT quantitative analysis expert working group meeting

Environmental and Molecular Mutagenesis, EarlyView.
Abstract Quantitative risk assessments of chemicals are routinely performed using in vivo data from rodents; however, there is growing recognition that non‐animal approaches can be human‐relevant alternatives. There is an urgent need to build confidence in non‐animal alternatives given the international support to reduce the use of animals in toxicity ...
Marc A. Beal, Guangchao Chen, Kerry L. Dearfield, Min Gi, Bhaskar Gollapudi, Robert H. Heflich, Katsuyoshi Horibata, Alexandra S. Long, David P. Lovell, Barbara L. Parsons, Stefan Pfuhler, John Wills, Andreas Zeller, George Johnson, Paul A. White   +14 more
wiley   +1 more source

Induction of humoral and cellular immune responses against the HIV-1 envelope protein using γ-retroviral virus-like particles

Virology Journal, 2011
This study evaluates the immunogenicity of the HIV envelope protein (env) in mice presented either attached to γ-retroviral virus-like-particles (VLPs), associated with cell-derived microsomes or as solubilized recombinant protein (gp160).
Purcell Damian FJ, Center Robert J, Pedersen Finn S, Bahrami Shervin, Melchjorsen Jesper, Wheatley Adam, Kirkegaard Tea, Ostergaard Lars, Duch Mogens, Tolstrup Martin   +9 more
doaj   +1 more source

Computer‐Aided Functional Oligosaccharide Screening and the Regulatory Role in Lipid Metabolism

Food Bioengineering, EarlyView.
ABSTRACT This study investigated the lipid‐lowering effects and intervention mechanisms of structurally diverse functional oligosaccharides on non‐alcoholic fatty liver disease (NAFLD). By integrating computational tools such as molecular docking and molecular dynamics simulations (MDS), a comprehensive “in silico‐in vitro‐in vivo” tri‐dimensional ...
Rui Jing, Shanshan Deng, Mengyao Zhao, Liming Zhao   +3 more
wiley   +1 more source

2-fenilbenzotriazóis (PBTA): uma nova classe de contaminantes ambientais 2-phenylbenzotriazoles (PBTAs): a new class of environmental contaminants

Química Nova, 2008
This work is a literature review of PBTAs, the phenylbenzotriazoles generated from the reduction and chlorination of azo dyes. The PBTAs and the non- chlorinated PBTAs were isolated for the first time from river blue rayon organic extracts that showed ...
Fábio Kummrow, Gisela de Aragão Umbuzeiro   +1 more
doaj   +1 more source