Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease

Journal of Medicinal Chemistry

Volumn 55, Issue 3, 2012, Pages 1021-1046

  Prime, Michael E ^a   Andersen, Ole A ^a   Barker, John J ^a   Brooks, Mark A ^a   Cheng, Robert K Y ^a   Toogood Johnson, Ian ^a   Courtney, Stephen M ^a   Brookfield, Frederick A ^a   Yarnold, Christopher J ^a   Marston, Richard W ^a   Johnson, Peter D ^a   Johnsen, Siw F ^a   Palfrey, Jordan J ^a   Vaidya, Darshan ^a   Erfan, Sayeh ^a   Ichihara, Osamu ^a   Felicetti, Brunella ^a   Palan, Shilpa ^a   Pedret Dunn, Anna ^a   Schaertl, Sabine ^b   Sternberger, Ina ^b   Ebneth, Andreas ^b   Scheel, Andreas ^b   Winkler, Dirk ^b   Toledo Sherman, Leticia ^c   Beconi, Maria ^c   MacDonald, Douglas ^c   Muñoz Sanjuan, Ignacio ^c   Dominguez, Celia ^c   Wityak, John ^c   more..

^a EVOTEC UK LTD   (United Kingdom)

^b EVOTEC AG   (Germany)

^c CHDI MANAGEMENT CHDI FOUNDATION   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACRYLAMIDE DERIVATIVE; ACYLTRANSFERASE INHIBITOR; N (4 BROMOPHENYL)ACRYLAMIDE; PHENYLACRYLAMIDE; PROTEIN GLUTAMINE GAMMA GLUTAMYLTRANSFERASE 2; TRANSGLUTAMINASE 2 INHIBITOR; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; ARTICLE; CELL ASSAY; CELL LYSATE; CELL SURVIVAL; CHEMICAL REACTION; CONTROLLED STUDY; COVALENT BOND; DRUG DESIGN; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; ENZYME INHIBITION; GENE DELETION; HUMAN; HUMAN CELL; HUNTINGTON CHOREA; IC 50; IN VITRO STUDY; MOLECULAR BIOLOGY; NERVE CELL NECROSIS; PHENOTYPE; STRUCTURE ACTIVITY RELATION;

ACRYLAMIDES; ANIMALS; CACO-2 CELLS; CELL MEMBRANE PERMEABILITY; GTP-BINDING PROTEINS; HEK293 CELLS; HUMANS; HUNTINGTON DISEASE; MALE; MICE; MICROSOMES, LIVER; MODELS, MOLECULAR; PIPERAZINES; PYRIDINES; PYRIMIDINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES; TRANSGLUTAMINASES;

EID: 84856877208     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm201310y     Document Type: Article

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