Affiliation: H. Lundbeck A/S
- Inhibition of microglial inflammation by the MLK inhibitor CEP-1347Søren Lund
Disease Biology, H Lundbeck A S, Ottiliavej 9, 2500 Valby, Denmark
J Neurochem 92:1439-51. 2005..These data imply MLKs as important, yet unrecognized, modulators of microglial inflammation, and demonstrate a novel anti-inflammatory potential of CEP-1347...
- Mixed lineage kinase activity of indolocarbazole analoguesChikara Murakata
Kyowa Hakko Kogyo Co, Ltd, Tokyo, Japan
Bioorg Med Chem Lett 12:147-50. 2002..Addition of 3,9-bis-alkylthiomethyl groups to K-252a results in potent and selective MLK inhibitors. The in vitro and in vivo survival promoting activity of bis-isopropylthiomethyl-K-252a (16, CEP-11004/KT-8138) is reported...
- Inhibition of mixed lineage kinase 3 attenuates MPP+-induced neurotoxicity in SH-SY5Y cellsJoanne R Mathiasen
Neurobiology, Cephalon, Inc, 145 Brandywine Parkway, West Chester, PA 19380, USA
Brain Res 1003:86-97. 2004..These studies show that inhibition of the MLK 3/JNK pathway attenuates MPP(+)-mediated SH-SY5Y cell death in culture and supports the mechanism of action of CEP-1347 as an MLK family inhibitor...
- CEP-11004, an inhibitor of the SAPK/JNK pathway, reduces TNF-alpha release from lipopolysaccharide-treated cells and miceJohn R Ciallella
Cephalon, Inc, 145 Brandywine Parkway, West Chester, PA 19380, USA
Eur J Pharmacol 515:179-87. 2005..These results suggest that MLK blockade may be useful in inhibiting pro-inflammatory cytokine production in a wide range of diseases...
- Targeting the JNK pathway for therapeutic benefit in CNS diseaseDonna Bozyczko-Coyne
Cephalon Inc, West Chester, PA 19380, USA
Curr Drug Targets CNS Neurol Disord 1:31-49. 2002..Also included is the progress on development of inhibitors targeting the JNK pathway for therapeutic benefit...
- Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine modelsRobert L Hudkins
Discovery Research, Cephalon, Incorporated, 145 Brandywine Parkway, West Chester, Pennsylvania 19380, USA
J Med Chem 51:5680-9. 2008..The MLK1 structure-activity relationships were supported by the first-reported X-ray crystal structure of MLK1 bound with 16...