J T Durkin

Summary

Affiliation: Cephalon Inc
Country: USA

Publications

  1. ncbi Rank-order of potencies for inhibition of the secretion of abeta40 and abeta42 suggests that both are generated by a single gamma-secretase
    J T Durkin
    Cephalon, Inc, West Chester, Pennsylvania 19380, USA
    J Biol Chem 274:20499-504. 1999
  2. ncbi Phosphoregulation of mixed-lineage kinase 1 activity by multiple phosphorylation in the activation loop
    John T Durkin
    Cephalon, Inc, 145 Brandywine Parkway, West Chester, Pennsylvania 19380, USA
    Biochemistry 43:16348-55. 2004
  3. ncbi Amino-terminal isoforms of the human glycine transporter GlyT1 exhibit similar pharmacology
    John T Durkin
    Worldwide Discovery Research, Cephalon Inc, 145 Brandywine Parkway, West Chester, PA 19380, USA
    Brain Res 1374:1-7. 2011
  4. ncbi 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 models
    Robert L Hudkins
    Discovery Research, Cephalon, Incorporated, 145 Brandywine Parkway, West Chester, Pennsylvania 19380, USA
    J Med Chem 51:5680-9. 2008
  5. ncbi Glycine transporter (GlyT1) inhibitors with reduced residence time increase prepulse inhibition without inducing hyperlocomotion in DBA/2 mice
    Karla Kopec
    Cephalon, Inc, West Chester, PA 19380, USA
    Biochem Pharmacol 80:1407-17. 2010
  6. ncbi Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase family
    A C Maroney
    Cephalon Inc, 145 Brandywine Pkwy, West Chester, Pennsylvania 19380, USA
    J Biol Chem 276:25302-8. 2001
  7. ncbi ALK mutants in the kinase domain exhibit altered kinase activity and differential sensitivity to small molecule ALK inhibitors
    Lihui Lu
    Worldwide Discovery Research, Cephalon Inc, West Chester, Pennsylvania 19380, USA
    Biochemistry 48:3600-9. 2009

Collaborators

Detail Information

Publications7

  1. ncbi Rank-order of potencies for inhibition of the secretion of abeta40 and abeta42 suggests that both are generated by a single gamma-secretase
    J 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...
  2. ncbi Phosphoregulation of mixed-lineage kinase 1 activity by multiple phosphorylation in the activation loop
    John 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...
  3. ncbi Amino-terminal isoforms of the human glycine transporter GlyT1 exhibit similar pharmacology
    John 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...
  4. ncbi 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 models
    Robert 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...
  5. ncbi Glycine transporter (GlyT1) inhibitors with reduced residence time increase prepulse inhibition without inducing hyperlocomotion in DBA/2 mice
    Karla 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...
  6. ncbi Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase family
    A 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...
  7. ncbi ALK mutants in the kinase domain exhibit altered kinase activity and differential sensitivity to small molecule ALK inhibitors
    Lihui 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...