Target engagement analysis and link to pharmacodynamic endpoint for a novel class of CNS-penetrant and efficacious p38α MAPK inhibitors

Journal of Neuroimmune Pharmacology

Volumn 9, Issue 4, 2014, Pages 454-460

  Bachstetter, Adam D ^a   Watterson, D Martin ^b   Van Eldik, Linda J ^a  

^a UNIVERSITY OF KENTUCKY   (United States)

^b NORTHWESTERN UNIVERSITY   (United States)

Author keywords

Cytokine; Drug discovery; Microglia; Mitogen activated protein kinase; Neurodegeneration; Signal transduction

Indexed keywords

CXCL1 CHEMOKINE; INTERLEUKIN 10; INTERLEUKIN 1BETA; INTERLEUKIN 6; MITOGEN ACTIVATED PROTEIN KINASE 14; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE P38ALPHA INHIBITOR; MW 181; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG; CYTOKINE; LIPOPOLYSACCHARIDE; N,N-DIMETHYL-6-(NAPHTHALEN-1-YL)-5-(PYRIDIN-4-YL)PYRIDAZIN-3-AMINE; PROTEIN KINASE INHIBITOR; PYRIDAZINE DERIVATIVE; PYRIDINE DERIVATIVE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; BRAIN LEVEL; CONTROLLED STUDY; CYTOKINE PRODUCTION; DOSE RESPONSE; DRUG EFFICACY; DRUG PENETRATION; DRUG SCREENING; DRUG SPECIFICITY; DRUG SYNTHESIS; DRUG TARGETING; FEMALE; GLIA; IN VIVO STUDY; MALE; MICROGLIAL CELL CULTURE; MOUSE; NERVOUS SYSTEM INFLAMMATION; NONHUMAN; PHARMACODYNAMICS; PHOSPHORYLATION; PRIORITY JOURNAL; REVIEW; WILD TYPE; ANIMAL; ANTAGONISTS AND INHIBITORS; BRAIN; CELL CULTURE; DRUG EFFECTS; DRUG RESISTANCE; GENETICS; METABOLISM; MUTATION; UPREGULATION;

ANIMALS; BRAIN; CELLS, CULTURED; CYTOKINES; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG RESISTANCE; FEMALE; LIPOPOLYSACCHARIDES; MALE; MICE; MITOGEN-ACTIVATED PROTEIN KINASE 14; MUTATION; NEUROGLIA; PROTEIN KINASE INHIBITORS; PYRIDAZINES; PYRIDINES; UP-REGULATION;

EID: 84906344231     PISSN: 15571890     EISSN: 15571904     Source Type: Journal    
DOI: 10.1007/s11481-014-9543-3     Document Type: Review

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