Multistage screening reveals chameleon ligands of the human farnesyl pyrophosphate synthase: Implications to drug discovery for neurodegenerative diseases

Journal of Medicinal Chemistry

Volumn 57, Issue 13, 2014, Pages 5764-5776

  De Schutter, Joris W ^a   Park, Jaeok ^a   Leung, Chun Yuen ^a   Gormley, Patrick ^b   Lin, Yih Shyan ^a   Hu, Zheping ^a   Berghuis, Albert M ^a   Poirier, Judes ^b   Tsantrizos, Youla S ^a  

^a MCGILL UNIVERSITY   (Canada)

^b DOUGLAS MENTAL HEALTH UNIVERSITY INSTITUTE   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

BISPHOSPHONIC ACID DERIVATIVE; ENZYME; ENZYME INHIBITOR; FARNESYL PYROPHOSPHATE SYNTHASE; FARNESYL PYROPHOSPHATE SYNTHASE INHIBITOR; LACTATE DEHYDROGENASE; LIGAND; MAGNESIUM ION; MESSENGER RNA; TAU PROTEIN; UNCLASSIFIED DRUG; [2 [6 (4 TOLYL)[2,3 D]PYRIMIDIN 4 YL]ETHYL]PHOSPHONIC ACID; [2 [[6 (4 TOLYL)[2,3 D]PYRIMIDIN 4 YL]AMINO]ETHYL]PHOSPHONIC ACID; [[[6 (3 CHLORO 4 METHYLPHENYL)THIENOL[2,3 D]PYRIMIDIN 4 YL]AMINO]METHYL]PHOSPHONIC ACID; [[[6 (4 TOLYL)THIENOL[2,3 D]PYRIMIDIN 4 YL]AMINO]METHYL]PHOSPHONIC ACID;

ALLOSTERISM; ALZHEIMER DISEASE; ARTICLE; DEGENERATIVE DISEASE; DIFFERENTIAL SCANNING CALORIMETRY; DRUG DEVELOPMENT; DRUG SCREENING; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN TISSUE; IC 50; ISOTHERMAL TITRATION CALORIMETRY; PROTEIN PHOSPHORYLATION; SINGLE NUCLEOTIDE POLYMORPHISM;

ALLOSTERIC SITE; ALZHEIMER DISEASE; CATALYTIC DOMAIN; CRYSTALLOGRAPHY, X-RAY; DIPHOSPHONATES; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; GERANYLTRANSTRANSFERASE; HUMANS; LIGANDS; NEURODEGENERATIVE DISEASES; ORGANOPHOSPHONATES; PHOSPHORYLATION; POLYMORPHISM, SINGLE NUCLEOTIDE; PYRIMIDINES; TAU PROTEINS;

EID: 84904339081     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500629e     Document Type: Article

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