[HTML][HTML] K252a and CEP1347 are neuroprotective compounds that inhibit mixed-lineage kinase-3 and induce activation of Akt and ERK

PP Roux, G Dorval, M Boudreau… - Journal of Biological …, 2002 - ASBMB
K252a is best known as a Trk inhibitor, but is also a neuroprotective compound. CEP1347, a
K252a derivative, retains neuroprotective properties, but does not inhibit TrkA. CEP1347 has
recently been shown to directly inhibit MAPKKKs, including MLK3, but the effect of K252a on
MAPKKKs remains unknown. K252a and CEP1347 not only prevent death, but also facilitate
neurite outgrowth and maintenance, somal hypertrophy, and neurotransmitter synthesis. The
biochemical basis for these trophic effects remains unknown. We have compared the effects …