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[Establishment and evaluation of haloalkane dehalogenase tagged -adrenergic receptor chromatography].
Se Pu
October 2024
Joint Laboratory for Research on Active Components and Pharmacological Mechanism of Tibetan MateriaMedica of Tibetan Medical Research Center of Tibet, Xizang Minzu University, Xianyang 712082, China.
Receptor chromatography is an efficient analytical technique that combines the high separation ability of chromatography with the high specificity of receptors for drug recognition. In addition, this technique offers the advantages of active recognition, online separation, and convenient multidimensional target tracking. This strategy allows target active ingredients in complex systems, such as traditional Chinese medicines, to be efficiently screened and accurately identified.
View Article and Find Full Text PDFMolecular docking and in vitro evaluations reveal the role of human cytochrome P450 3A4 in the cross-coupling metabolism of phenolic xenobiotics.
Environ Res
March 2023
Laboratory for Earth Surface Processes, College of Urban and Environmental Sciences, Peking University, Beijing 100871, China. Electronic address:
Metabolism generally transforms xenobiotics into more polar and hydrophilic products, facilitating their elimination from the body. Recently, a new metabolic pathway that transforms phenolic xenobiotics into more lipophilic and bioactive dimer products was discovered. To elucidate the role of cytochrome P450 (CYP) enzymes in mediating this cross-coupling metabolism, we used high-throughput screening to identify the metabolites generated from the coupling of 20 xenobiotics with four endogenous metabolites in liver microsomes.
View Article and Find Full Text PDFThe neurotoxic mechanism of Jack Bean Urease in insects involves the interplay between octopaminergic and dopaminergic pathways.
Pestic Biochem Physiol
January 2023
Laboratório de Neurobiologia e Toxinologia (LANETOX), Universidade Federal do Pampa, Campus São Gabriel, São Gabriel, RS, Brazil; Programa de Pós-Graduação em Ciências Biológicas: Bioquímica Toxicológica (PPGBTox), Universidade Federal de Santa Maria (UFSM), Santa Maria, RS, Brazil; Departamento Multidisciplinar, Escola Paulista de Política, Economia e Negócios (EPPEN), Universidade Federal de São Paulo (UNIFESP), Rua Angélica, 100, Jardim das Flores, 06110295, Osasco, SP, Brazil. Electronic address:
In the last decades, the entomotoxicity of JBU and its derived peptides became an object of study, due mainly to the ubiquitous interaction of these compounds with different species of insects and their potential as natural insecticides. In this work, we investigated the neurotoxic effects of JBU in Nauphoeta cinerea cockroaches by dissecting pharmacologically the monoaminergic pathways involved. Selective pharmacological modulators for monoaminergic pathways in in vivo and ex vivo experimental models were employed.
View Article and Find Full Text PDFMolecular Interactions of Zyesami with the SARS-CoV-2 nsp10/nsp16 Protein Complex.
Comb Chem High Throughput Screen
March 2023
Department of Medical Laboratory Sciences, College of Applied Medical Sciences in Al-Quwayiyah, Shaqra University, Saudi Arabia.
Background: SARS-CoV-2 emerged in late 2019 and caused COVID-19. Patients treated with Zyesami were found to have a 3-fold decrease in respiratory failure and improved clinical outcomes. It was reported that Zyesami inhibits RNA replication of SARS-CoV-2, including several non-structural proteins essential in viral RNA replication.
View Article and Find Full Text PDFSite-selective covalently immobilized alpha 1A adrenergic receptor for thermodynamic and extra-thermodynamic study of four ligands binding to the receptor by chromatographic methods.
J Chromatogr A
February 2022
College of Life Sciences, Northwest University, Xi'an 710069, China. Electronic address:
Immobilized G protein-coupled receptor is a versatile tool to study ligand-receptor interactions. In this work, we synthesized the immobilized alpha 1A adrenergic receptor (α-AR), a GPCR subtype mediating smooth muscle contraction, through a site-selective covalent method that relies on the reaction between haloalkane dehalogenase tagged α-AR and macroporous silica gel coated with 6-chlorohexanoic acid. To investigate thermodynamic and extra-thermodynamic parameters for ligand binding, we utilized the covalently immobilized receptor as stationary phase to perform frontal analysis and injection-amount dependent analysis as well as compared with the random immobilization method.
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