Article
Target engagement analysis and link to pharmacodynamic endpoint for a novel class of CNS-penetrant and efficacious p38α MAPK inhibitors.
Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology - 1 Sept 2014
Bachstetter Adam D, Watterson D Martin, Van Eldik Linda J
Abstract excerpt
The protein kinase, p38α MAPK, is a key intracellular transducer of stressor-induced neuroinflammatory responses and, as such, is of high interest as a potential therapeutic target. We recently reported the synthesis and evaluation of first-in-class CNS-penetrant and highly specific p38 MAPK inhibitors that avoid target crossover issues seen in popular small molecule p38 MAPK inhibitors used in hundreds of...
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