Rational Design of Autotaxin Inhibitors by Structural Evolution of Endogenous Modulators.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.6b01743
Abstract: Autotaxin produces the bioactive lipid lysophosphatidic acid (LPA) and is a drug target of considerable interest for numerous pathologies. We report the expedient, structure-guided evolution of weak physiological allosteric inhibitors (bile salts) into potent competitive… read more here.
Keywords: evolution; inhibitors structural; autotaxin; rational design ... See more keywords
Protein Prenyltransferases and Their Inhibitors: Structural and Functional Characterization
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DOI: 10.3390/ijms23105424
Abstract: Protein prenylation is a post-translational modification controlling the localization, activity, and protein–protein interactions of small GTPases, including the Ras superfamily. This covalent attachment of either a farnesyl (15 carbon) or a geranylgeranyl (20 carbon) isoprenoid… read more here.
Keywords: prenyltransferases inhibitors; structural functional; inhibitors structural; ggtase ... See more keywords
Anti-Tuberculosis Mur Inhibitors: Structural Insights and the Way Ahead for Development of Novel Agents
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DOI: 10.3390/ph16030377
Abstract: Mur enzymes serve as critical molecular devices for the synthesis of UDP-MurNAc-pentapeptide, the main building block of bacterial peptidoglycan polymer. These enzymes have been extensively studied for bacterial pathogens such as Escherichia coli and Staphylococcus… read more here.
Keywords: tuberculosis; anti tuberculosis; tuberculosis mur; inhibitors structural ... See more keywords