Combined rational design and a high throughput screening platform for identifying chemical inhibitors of a ras-activating enzyme

Journal of Biological Chemistry

Volumn 290, Issue 20, 2015, Pages 12879-12898

  Evelyn, Chris R ^a   Biesiada, Jacek ^a   Duan, Xin ^a   Tang, Hong ^a,b   Shang, Xun ^a   Papoian, Ruben ^b,c   Seibel, William L ^a,b   Nelson, Sandra ^b   Meller, Jaroslaw ^a,c   Zheng, Yi ^a  

^a CINCINNATI CHILDREN S HOSPITAL RESEARCH FOUNDATION   (United States)

^b UNIVERSITY OF CINCINNATI   (United States)

^c UNIVERSITY OF CINCINNATI COLLEGE OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CELL SIGNALING; CHEMICAL ACTIVATION; ENZYMES; FLUORESCENT SCREENS; GENE EXPRESSION; ION EXCHANGE; LOADING; MOBILE SECURITY; MOLECULES; NUCLEOTIDES; POSITIVE IONS; THROUGHPUT;

CANCER PATHOGENESIS; ENSEMBLE STRUCTURES; GUANINE NUCLEOTIDE EXCHANGE FACTORS; GUANINE NUCLEOTIDES; HIGH THROUGHPUT SCREENING; MULTIPLE CELLULAR PROCESS; SMALL MOLECULE INHIBITOR; STRUCTURE ACTIVITY RELATIONSHIPS;

CATALYST ACTIVITY;

ENZYME; ENZYME INHIBITOR; FLUORESCEIN; GUANOSINE DIPHOSPHATE; GUANOSINE TRIPHOSPHATE; RAS GUANINE NUCLEOTIDE EXCHANGE FACTOR ENZYME; RAS PROTEIN; SOS1; UC 104460; UC 376097; UC 773587; UC 857993; UC 992652; UNCLASSIFIED DRUG; GUANINE NUCLEOTIDE EXCHANGE FACTOR; GUANOSINE TRIPHOSPHATASE ACTIVATING PROTEIN; HRAS PROTEIN, HUMAN; PROTEIN P21;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CATALYSIS; CONTROLLED STUDY; DISSOCIATION; DRUG DESIGN; DRUG IDENTIFICATION; ENZYME BINDING; ENZYME INHIBITION; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; MOLECULAR LIBRARY; MOUSE; MUTAGENESIS; NONHUMAN; PREDICTION; PRIORITY JOURNAL; PROTEIN INTERACTION; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DOSE RESPONSE; DRUG DELIVERY SYSTEM; DRUG SCREENING; GENETICS; METABOLISM; PROCEDURES;

DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DELIVERY SYSTEMS; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; HUMANS; PROTO-ONCOGENE PROTEINS P21(RAS); RAS GTPASE-ACTIVATING PROTEINS; RAS GUANINE NUCLEOTIDE EXCHANGE FACTORS;

EID: 84929340871     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M114.634493     Document Type: Article

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