We report the synthesis and biochemical evaluation of new competitive inhibitors of the cytosolic (NADH-dependent) glycerophosphate dehydrogenase. The best tested compound, phosphono-propionohydroxamic acid, with a Ki of 6 microM, might be of interest as an anti-obesity drug.
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http://dx.doi.org/10.1016/j.bmcl.2006.10.030 | DOI Listing |
J Bacteriol
January 2025
Laboratoire de Communication Bactérienne et Stratégies Anti-infectieuses (CBSA UR4312, formerly LMSM EA4312), Univ Rouen Normandie, Université Caen Normandie, Normandie Univ, Rouen, France.
Unlabelled: MFE01 is an environmental bacterium characterized by an hyperactive type 6 secretion system (T6SS) and a strong emission of volatile organic compounds (VOCs). In a previous study, a transposition mutant, 3H5, exhibited an inactive T6SS and altered VOC emission. In 3H5, the interruption of gene by the transposon was insufficient to explain these phenotypes.
View Article and Find Full Text PDFBioTech (Basel)
December 2024
The BCPH Unit of Molecular Physiology, Department of Chemistry, Biology and Marine Science, Faculty of Science, University of the Ryukyus, Nishihara 903-0213, Okinawa, Japan.
Functionally important amino acid sequences in proteins are often located at multiple sites. Three-dimensional structural analysis and site-directed mutagenesis may be performed to allocate functional sites for understanding structure‒function relationships and for developing novel inhibitory drugs. However, such methods are too demanding to comprehensively cover potential functional sites throughout a protein chain.
View Article and Find Full Text PDFChemMedChem
January 2025
Syracuse University, Chemistry, 111 College Pl, 132441200, Syracuse, UNITED STATES OF AMERICA.
The SH2-containing inositol phosphatase (SHIP) has become an actively researched therapeutic target for a number of disorders, including Alzheimer's Disease, Graft-vs-Host disease, obesity and cancer. Analogs of the aminosteroid SHIP inhibitor 3a-aminocholestane (3AC) have been synthesized and tested. Analogs with improved water solubility have been identified.
View Article and Find Full Text PDFUltrason Sonochem
January 2025
College of Food Science, Heilongjiang Bayi Agricultural University, Daqing 163319, PR China; National Coarse Cereals Engineering Research Center, Daqing 163319, PR China; Key Laboratory of Agro-Products Processing and Quality Safety of Heilongjiang Province, Daqing 163319, PR China. Electronic address:
In this study, we adopted the synergistic modification technology of hydrodynamic cavitation and snail enzyme, to improve the yield and activity of soluble dietary fibers (SDFs) of rice husk. The physicochemical properties, structural changes, and inhibition of α-glucosidase and α-amylase of SDFs were examined in vitro. This synergistic treatment significantly increased the yield of SDFs to 18.
View Article and Find Full Text PDFJ Enzyme Inhib Med Chem
December 2025
Department of Biology Education, Teachers College and Institute for Phylogenomics and Evolution, Kyungpook National University, Daegu, Republic of Korea.
This study investigated the potential of the indirubin-3'-oxime (I3O) compound to mitigate temperature-induced male infertility in . Elevated temperatures significantly reduced egg-hatching rates, but I3O supplementation improved these rates, suggesting it can partially restore fertility under heat stress. Additionally, I3O was found to inhibit soluble epoxide hydrolase (sEH), an enzyme involved in the metabolism of epoxyeicosatrienoic acids, which are vital for reproductive health.
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