J T Durkin
Affiliation: Cephalon Inc
- Rank-order of potencies for inhibition of the secretion of abeta40 and abeta42 suggests that both are generated by a single gamma-secretaseJ T Durkin
Cephalon, Inc, West Chester, Pennsylvania 19380, USA
J Biol Chem 274:20499-504. 1999..These results favor the hypothesis that Abeta variants ending at residue 40 or 42 are generated by a single gamma-secretase...
- Phosphoregulation of mixed-lineage kinase 1 activity by multiple phosphorylation in the activation loopJohn T Durkin
Cephalon, Inc, 145 Brandywine Parkway, West Chester, Pennsylvania 19380, USA
Biochemistry 43:16348-55. 2004..This mechanism is broadly similar to that previously reported for MLK3 [Leung, I. W., and Lassam, N. (2001) J. Biol. Chem. 276, 1961-1967], but the key residue differs...
- Amino-terminal isoforms of the human glycine transporter GlyT1 exhibit similar pharmacologyJohn T Durkin
Worldwide Discovery Research, Cephalon Inc, 145 Brandywine Parkway, West Chester, PA 19380, USA
Brain Res 1374:1-7. 2011..Antipsychotics previously shown to be weak inhibitors of GlyT1 likewise had similar potency against all three isoforms. The cell lines validated here are tools for discovering inhibitors that might distinguish among GlyT1 isoforms...
- 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...
- Glycine transporter (GlyT1) inhibitors with reduced residence time increase prepulse inhibition without inducing hyperlocomotion in DBA/2 miceKarla Kopec
Cephalon, Inc, West Chester, PA 19380, USA
Biochem Pharmacol 80:1407-17. 2010..Thus, GlyT1 inhibitors with short residence times demonstrated efficacy without mechanism-based adverse effects...
- Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase familyA C Maroney
Cephalon Inc, 145 Brandywine Pkwy, West Chester, Pennsylvania 19380, USA
J Biol Chem 276:25302-8. 2001..These results identify MLKs as targets of CEP-1347 in the JNK signaling cascade and demonstrate that CEP-1347 can block MLK-induced cell death...
- ALK mutants in the kinase domain exhibit altered kinase activity and differential sensitivity to small molecule ALK inhibitorsLihui Lu
Worldwide Discovery Research, Cephalon Inc, West Chester, Pennsylvania 19380, USA
Biochemistry 48:3600-9. 2009..Further characterization of these mutants may help to identify and develop potent ALK inhibitors active against both WT and resistant mutants of ALK...