Rational Design of Autotaxin Inhibitors by Structural Evolution of Endogenous Modulators.
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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