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
Inhibitors of the Structural and Nonstructural Proteins of Alphaviruses.
Sign Up to like & getrecommendations! Published in 2024 at "ACS infectious diseases"
DOI: 10.1021/acsinfecdis.4c00254
Abstract: The Alphavirus genus includes viruses that cause encephalitis due to neuroinvasion and viruses that cause arthritis due to acute and chronic inflammation. There is no approved therapeutic for alphavirus infections, but significant efforts are ongoing,… read more here.
Keywords: structural nonstructural; inhibitors structural; proteins alphaviruses; nonstructural proteins ... 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