High-throughput screening for small-molecule inhibitors of LARG-stimulated RhoA nucleotide binding via a novel fluorescence polarization assay

Journal of Biomolecular Screening

Volumn 14, Issue 2, 2009, Pages 161-172

  Evelyn, Chris R ^a   Ferng, Timothy ^a   Rojas, Rafael J ^b   Larsen, Martha J ^a   Sondek, John ^b   Neubig, Richard R ^a,c  

^a UNIVERSITY OF MICHIGAN HEALTH SYSTEM   (United States)

^b UNIVERSITY OF NORTH CAROLINA SCHOOL OF MEDICINE   (United States)

^c 1301 MSRB III ^*  (United States)

Author keywords

Drug discovery; Fluorescence polarization; High throughput screening; LARG; RhoA; RhoGEF

Indexed keywords

2 [(3 METHYLPHENYL)AMINO] N' [(2,4,6 TRIBROMO 3 HYDROXYPHENYL)METHYLIDENE]ACETOHYDRAZIDE; 3 (2H 1,3 BENZODIOXOL 5 YL) 2 IMINO 5 [[5 (2 NITROPHENYL)FURAN 2 YL]METHYLIDENE] 1,3 THIAZOLIDIN 4 ONE; 4 [5 [(4,6 DIOXO 2 SULFANYLIDENE ,3 DIAZINAN 5 YLIDENE)METHYL]FURAN 2 YL] N (1,3 THIAZOL 2 YL)BENZENE 1 SULFONAMIDE; 4 AMINO 2 (5 AMINO 1,3 BENZOTHIAZOL 2 YL)PHENOL; 7 (3 NITROPHENYL) 8 AZATRICYCLO[7.4.0.0 [2,6]]TRIDECA 1 (13),3,9,11 TETRAENE 10 CARBOXYLIC ACID; 7 HYDROXY 3 [2 (4 PHENYLPHENYL) 1,3 THIAZOL 4 YL] 2H CHROMEN 2 ONE; CCG 11952; CCG 12529; CCG 13528; CCG 14113; CCG 14631; CCG 14899; CCG 5275; CCG 5650; CCG 5849; CCG 7167; CCG 8218; CCG 9340; GUANINE NUCLEOTIDE EXCHANGE FACTOR; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); LEUKEMIA ASSOCIATED RHO GUANINE NUCLEOTIDE EXCHANGE FACTOR; PROTEIN INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SCREENING; DRUG SELECTIVITY; FLUORESCENCE POLARIZATION; HIGH THROUGHPUT SCREENING; IC 50; INTERMETHOD COMPARISON; PRIORITY JOURNAL;

ALGORITHMS; DRUG EVALUATION, PRECLINICAL; FLUORESCENCE POLARIZATION; GROWTH INHIBITORS; GUANINE NUCLEOTIDE EXCHANGE FACTORS; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HUMANS; MODELS, BIOLOGICAL; PROTEIN BINDING; RHOA GTP-BINDING PROTEIN; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 61849108234     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057108328761     Document Type: Article

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