A substrate-free activity-based protein profiling screen for the discovery of selective PREPL inhibitors

Journal of the American Chemical Society

Volumn 133, Issue 30, 2011, Pages 11665-11674

  Lone, Anna Mari ^a   Bachovchin, Daniel A ^b   Westwood, David B ^a   Speers, Anna E ^b   Spicer, Timothy P ^c   Fernandez Vega, Virneliz ^c   Chase, Peter ^c   Hodder, Peter S ^c   Rosen, Hugh ^b   Cravatt, Benjamin F ^b   Saghatelian, Alan ^a  

^a HARVARD UNIVERSITY   (United States)

^b SCRIPPS RESEARCH INSTITUTE   (United States)

^c SCRIPPS RESEARCH INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVITY-BASED; CENTRAL NERVOUS SYSTEMS; COGNITIVE DEFICITS; FLUORESCENCE POLARIZATION; GENETIC STUDIES; IN-VIVO; PHYSIOLOGICAL SUBSTRATE; PROLYL ENDOPEPTIDASE; PROTEIN PROFILING; SERINE HYDROLASES; SMALL-MOLECULE INHIBITORS; SUBSTRATE-FREE;

AMINO ACIDS; ASSAYS; BIOCHEMISTRY; ENZYMES; GENES; MAMMALS; PHYSIOLOGY; PYRIDINE;

SUBSTRATES;

1 ISOBUTYL 3 OXO 3,5,6,7 TETRAHYDRO 2H CYCLOPENTA[C]PYRIDINE 4 CARBONITRILE; CYANIDE; ISOBUTYL 3 OXO 2,3,5,6,7,8 HEXAHYDROISOQUINOLINE 4 CARBONITRILE; PROLYL ENDOPEPTIDASE; PROLYL ENDOPEPTIDASE INHIBITOR; PROLYL ENDOPEPTIDASE LIKE; PROLYL ENDOPEPTIDASE LIKE INHIBITOR; PYRIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRAIN; ENZYME ACTIVITY; ENZYME ANALYSIS; ENZYME ASSAY; ENZYME INHIBITION; ENZYME PURIFICATION; FLUORESCENCE POLARIZATION; FLUORESCENCE POLARIZATION ACTIVITY BASED PROTEIN PROFILING; MOUSE; NONHUMAN; PROTEIN EXPRESSION;

ANIMALS; CELL LINE, TUMOR; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; ENZYME INHIBITORS; FLUORESCENCE POLARIZATION; GENE EXPRESSION PROFILING; HIGH-THROUGHPUT SCREENING ASSAYS; MICE; MICE, INBRED C57BL; MOLECULAR STRUCTURE; SERINE ENDOPEPTIDASES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79960851570     PISSN: 00027863     EISSN: 15205126     Source Type: Journal    
DOI: 10.1021/ja2036095     Document Type: Article

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