Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors

Journal of Medicinal Chemistry

Volumn 56, Issue 5, 2013, Pages 2110-2124

  Liu, Feng ^a,c   Li, Fengling ^b   Ma, Anqi ^a   Dobrovetsky, Elena ^b   Dong, Aiping ^b   Gao, Cen ^a   Korboukh, Ilia ^a   Liu, Jing ^a   Smil, David ^b   Brown, Peter J ^b   Frye, Stephen V ^a   Arrowsmith, Cheryl H ^b   Schapira, Matthieu ^b   Vedadi, Masoud ^b   Jin, Jian ^a  

^a University of North Carolina   (United States)

^b UNIVERSITY OF TORONTO   (Canada)

^c SOOCHOW UNIVERSITY   (China)

Author keywords

[No Author keywords available]

Indexed keywords

1 (BENZO[D][1,2,3]THIADIAZOL 6 YL) 3 (2 OXO 2 PHENYLETHYL) UREA; METHYLTRANSFERASE; METHYLTRANSFERASE INHIBITOR; PRMT3 PROTEIN; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG DESIGN; DRUG POTENCY; DRUG SYNTHESIS; IC 50; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ALLOSTERIC SITE; ENZYME INHIBITORS; HUMANS; INHIBITORY CONCENTRATION 50; PROTEIN-ARGININE N-METHYLTRANSFERASES; RIBOSOMAL PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP; THIADIAZOLES; X-RAY DIFFRACTION;

EID: 84875177663     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm3018332     Document Type: Article

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