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
Benzoxaboroles—Novel Autotaxin Inhibitors
Sign Up to like & getrecommendations! Published in 2019 at "Molecules"
DOI: 10.3390/molecules24193419
Abstract: Autotaxin (ATX) is an extracellular enzyme that hydrolyses lysophosphatidylcholine (LPC) to lysophosphatidic acid (LPA), which has a role in the mediation of inflammation, fibrosis and cancer. ATX is a drug target that has been the… read more here.
Keywords: autotaxin inhibitors; novel autotaxin; benzoxaboroles novel;