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Angewandte Chemie - International Edition

Volumn 54, Issue 17, 2015, Pages 5166-5170

A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3)

(29) Kaniskan, H Ümit a Szewczyk, Magdalena M b Yu, Zhengtian c Eram, Mohammad S b Yang, Xiaobao a Schmidt, Keith a Luo, Xiao c Dai, Miao c He, Feng c Zang, Irene c Lin, Ying c Kennedy, Steven b Li, Fengling b Dobrovetsky, Elena b Dong, Aiping b Smil, David b Min, Sun Joon a,f Landon, Melissa b Lin Jones, Jennifer d Huang, Xi Ping e more..

a MOUNT SINAI SCHOOL OF MEDICINE (United States)

b UNIVERSITY OF TORONTO (Canada)

c Novartis Institutes for Biomedical Research (China)

d DiscoveRx Corporation (United States)

e UNIVERSITY OF NORTH CAROLINA SCHOOL OF MEDICINE (United States)

f Korea Institute of Science and Technology (South Korea)

g PRINCESS MARGARET HOSPITAL (Canada)

Author keywords

allosteric inhibition; chemical probes; enzyme inhibitors; histone methylation; X ray diffraction

Indexed keywords

ALKYLATION; AMINO ACIDS; ANIMALS; ARGININE; CELLS; CYTOLOGY; DISEASES; ENZYME INHIBITION; MOBILE SECURITY; PROBES; PROTEINS; STRUCTURAL OPTIMIZATION; X RAY DIFFRACTION;

ALLOSTERIC INHIBITION; ALLOSTERIC INHIBITOR; CHEMICAL PROBES; ENZYME INHIBITORS; HISTONE METHYLATION; MECHANISM OF ACTION; METHYLTRANSFERASE ACTIVITY; PROTEIN-ARGININE METHYLTRANSFERASE;

CRYSTAL STRUCTURE;

ENZYME INHIBITOR; HISTONE; ISOQUINOLINE DERIVATIVE; PRMT3 PROTEIN, HUMAN; PROTEIN ARGININE METHYLTRANSFERASE; PROTEIN BINDING; SGC707;

ALLOSTERISM; ANTAGONISTS AND INHIBITORS; BINDING SITE; CALORIMETRY; CHEMISTRY; GENETICS; HEK293 CELL LINE; HUMAN; METABOLISM; METHYLATION; MOLECULAR DYNAMICS; MUTAGENESIS; PROTEIN TERTIARY STRUCTURE; SURFACE PLASMON RESONANCE; TUMOR CELL LINE;

ALLOSTERIC REGULATION; BINDING SITES; CALORIMETRY; CELL LINE, TUMOR; ENZYME INHIBITORS; HEK293 CELLS; HISTONES; HUMANS; ISOQUINOLINES; METHYLATION; MOLECULAR DYNAMICS SIMULATION; MUTAGENESIS; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; PROTEIN-ARGININE N-METHYLTRANSFERASES; SURFACE PLASMON RESONANCE;

EID: 84927720612 PISSN: 14337851 EISSN: 15213773 Source Type: Journal
DOI: 10.1002/anie.201412154 Document Type: Article

Times cited : (94)

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