Results 61 to 70 of about 11,599 (234)

Tetrazine Ligation in Living Systems: Beyond Fast Kinetics to Effective Bioorthogonality

Chemistry – A European Journal, EarlyView.
Rapid reaction kinetics (k2) alone do not ensure successful tetrazine ligation in living systems. This review introduces ‘effective orthogonality’—focusing on chemical survival, availability, and encounter—as a practical framework. We highlight how bottlenecks shift from cellular sinks to in vivo delivery limits, offering design strategies for reliable
Junhyeong Yim, Junyoung Park, Youngjun Lee, Jongmin Park   +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

ER Adaptor SCAP Translocates and Recruits IRF3 to Perinuclear Microsome Induced by Cytosolic Microbial DNAs. [PDF]

PLoS Pathogens, 2016
Stimulator of interferon genes (STING, also known as MITA, ERIS or MPYS) induces the activation of TBK1 kinase and IRF3 transcription factor, upon sensing of microbial DNAs. How IRF3 is recruited onto the STING signalosome remains unknown. We report here
Wei Chen, Senlin Li, Huansha Yu, Xing Liu, Lulu Huang, Qiang Wang, Heng Liu, Ye Cui, Yijun Tang, Peng Zhang, Chen Wang   +10 more
doaj   +1 more source

Advances in Human Mass Balance Studies: An IQ Consortium Perspective on Current Practices and Emerging Trends

Clinical Pharmacology &Therapeutics, EarlyView.
Human radiolabeled mass balance studies are crucial for comprehensively characterizing the absorption, distribution, metabolism, and excretion (ADME) of investigational drugs, providing essential data for drug development, regulatory evaluation, and product labeling.
Jason Boer, Ellen Cannady, Filip Cuyckens, Ulrike Glaenzel, Camille Granvil, Felix Huth, Alexander D. James, Wenying Li, Céline Veau, Graeme Young, Qin Yue, Gregory S. Walker, Upendra A. Argikar, Jonathan N. Bauman, Cathy Cantalloube, Yu‐Luan Chen, Ping Kang, Patricia Moliner, Mette L. Pedersen, Isabel Piel, Simone Schadt, Hanno Schieferstein, Julia Suchomel, Shuai Wang, S. Cyrus Khojasteh   +24 more
wiley   +1 more source

Effects of psoralen on the pharmacokinetics of anastrozole in rats

Pharmaceutical Biology, 2018
Context: Psoralen and anastrozole are always used together for breast cancer patients in Chinese clinics. Objective: This study investigates the effects of psoralen on the pharmacokinetics of anastrozole in rats and its potential mechanism. Materials and
Yuzhu Zhang, Jingjing Wu, Yue Zhou, Yulian Yin, Hongfeng Chen   +4 more
doaj   +1 more source

PharmVar GeneFocus: CYP1A2—Clinical Impact, Genetic Variation, and Updated Nomenclature

Clinical Pharmacology &Therapeutics, EarlyView.
The Pharmacogene Variation Consortium (PharmVar) provides nomenclature for the highly polymorphic human CYP1A2 gene. CYP1A2 plays a crucial role in the biotransformation of several commonly used drugs, including antipsychotics, antidepressants, anxiolytics, and methylxanthines.
Katalin Monostory, Gonzalo Villapalos Garcia, Dora Koller, Solomon Adams, Chad A. Bousman, Evangelia Eirini Tsermpini, Michelle Whirl‐Carrillo, Amy J. Turner, Volker M. Lauschke, Mohamed Nagy, Erin C. Boone, Teri E. Klein, Pablo Zubiaur, Andrea Gaedigk   +13 more
wiley   +1 more source

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

Pharmaceutical Biology, 2019
Context: Paeoniflorin is reported to possess numerous pharmacological activities. Paeoniflorin and glycyrrhizin are always used together for the treatment of disease in China clinics; however, the drug–drug interaction between glycyrrhizin and ...
Hongjuan Sun, Jingfeng Wang, Juan Lv
doaj   +1 more source

Total Synthesis and Metabolic Stability of Hispidulin and Its d-Labelled Derivative

Molecules, 2017
Hispidulin is a naturally occurring flavone known to have various Central nervous system (CNS) activities. Proposed synthetic approaches to synthesizing hispidulin have proven unsatisfactory due to their low feasibility and poor overall yields.
Liang-Chieh Chen, Kai-Cheng Hsu, Lih-Chu Chiou, Hui-Ju Tseng, Wei-Jan Huang   +4 more
doaj   +1 more source

Microsomal epoxide hydrolase polymorphisms

Molecular Medicine Reports, 2010
Microsomal epoxide hydrolase plays a dual role in the activation and detoxification of carcinogenic compounds. Two polymorphic sites have been described in exons 3 and 4 of the microsomal epoxide hydrolase gene that change tyrosine residue 113 to histidine (Tyr113His) and histidine 139 to arginine (His139Arg), respectively.
Pinarbasi, Hatice, Silig, Yavuz, Pinarbasi, Ergun   +2 more
openaire   +5 more sources

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