Azo-bonded prodrugs of 5-aminosalicylic acid (mesalazine)—sulfasalazine, balsalazide, and olsalazine, which are used in the treatment of ulcerative colitis, rely on colonic bacteria to cleave the azo bond and liberate the active drug in the large intestine. The aim of this study was to use an in vitro colonic simulator to determine the rates of metabolism of these three prodrugs in the presence...

DNA gyrase and topoisomerase IV control bacterial DNA topology by breaking DNA, passing duplex DNA through the break, and then resealing the break. This process is subject to reversible corruption by fluoroquinolones, antibacterials that form drug-enzyme-DNA complexes in which the DNA is broken. The complexes, called cleaved complexes due to the presence of DNA breaks, have been crystallized an...

The role of -glutamyltranspeptidase (GGT) in transferring glutamate from endogenous glutathione (GSH) to the benzylamine moiety of a compound, such as 1-[3-(aminomethyl)phenyl]-N-[3fluoro-2 -(methylsulfonyl)-[1,1 -biphenyl]-4-yl]-3-(trifluoromethyl)1H-pyrazole-5-carboxamide (DPC 423), is described. Studies were performed with structurally related analogs of DPC 423 to demonstrate that this type...

Open AccessCCS ChemistryRESEARCH ARTICLE1 Feb 2021Macrocyclic Nonapeptides Incorporating Uncharacterized Amino Acids with Inhibitory Effects on Th17 Differentiation Kai-Long Ji, Yao-Yue Fan, Hio-Ha Kuok, Qun-Fang Liu, Ting Li and Jian-Min Yue Ji State Key Laboratory of Drug Research, Shanghai Institute Materia Medica, Chinese Academy Sciences, 201203 Google Scholar More articles by this author ...

Nanoscale reversed-phase liquid chromatography (LC) combined with electrospray ionization-tandem mass spectrometry (ESI-MS/ MS) has been used as a method for the direct identification of multiple cytochrome P450 (P450) isoforms found in male and female rat liver. In this targeted proteomic approach, rat liver microsomes were subjected to sodium dodecyl sulfate-polyacrylamide gel electrophoresis...

Nanoscale reversed-phase liquid chromatography (LC) combined with electrospray ionization-tandem mass spectrometry (ESI-MS/ MS) has been used as a method for the direct identification of multiple cytochrome P450 (P450) isoforms found in male and female rat liver. In this targeted proteomic approach, rat liver microsomes were subjected to sodium dodecyl sulfate-polyacrylamide gel electrophoresis...

25 Most functional metagenomic studies have been limited by the poor expression of many genes 26 derived from metagenomic DNA in Escherichia coli, which has been the predominant surrogate 27 host to date. To expand the range of expressed genes, we developed tools for construction and 28 functional screening of metagenomic libraries in Streptomyces lividans. We expanded on 29 previously publishe...

Nanoscale reversed-phase liquid chromatography (LC) combined with electrospray ionization-tandem mass spectrometry (ESI-MS/ MS) has been used as a method for the direct identification of multiple cytochrome P450 (P450) isoforms found in male and female rat liver. In this targeted proteomic approach, rat liver microsomes were subjected to sodium dodecyl sulfate-polyacrylamide gel electrophoresis...

Cardiolipin (CL) is a phospholipid predominantly found in the mitochondrial inner membrane and associated structurally with individual complexes of the electron transport chain (ETC). Since the ETC is the major mitochondrial reactive oxygen species (ROS) generating site, the proximity to the ETC and bisallylic methylenes of the polyunsaturated fatty acid chains of CL make it a likely target of ...