Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design

Journal of Medicinal Chemistry

Volumn 48, Issue 13, 2005, Pages 4212-4215

  Dymock, Brian W ^a   Barril, Xavier ^a   Brough, Paul A ^a   Cansfield, Julie E ^a   Massey, Andrew ^a   McDonald, Edward ^b   Hubbard, Roderick E ^a   Surgenor, Allan ^a   Roughley, Stephen D ^a   Webb, Paul ^a   Workman, Paul ^b   Wright, Lisa ^a   Drysdale, Martin J ^a  

^a Vernalis PLC   (United Kingdom)

^b INSTITUTE OF CANCER RESEARCH   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIBIOTIC AGENT; CCT 018159; CHAPERONE; HEAT SHOCK PROTEIN 70; HEAT SHOCK PROTEIN 90; PROTEIN INHIBITOR; RADICICOL; RAF PROTEIN; UNCLASSIFIED DRUG; VER 49009;

AMINO TERMINAL SEQUENCE; ARTICLE; CELL PROLIFERATION; COLON TUMOR; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG ACTIVITY; DRUG BINDING; DRUG DESIGN; DRUG POTENCY; DRUG STRUCTURE; FLUORESCENCE POLARIZATION IMMUNOASSAY; HUMAN; HUMAN CELL; PHARMACODYNAMICS; PROTEIN DOMAIN; X RAY ANALYSIS;

ADENOSINE TRIPHOSPHATE; AMIDES; AMINES; BINDING SITES; DRUG DESIGN; GLYCINE; HSP90 HEAT-SHOCK PROTEINS; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN CONFORMATION; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 21244505104     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm050355z     Document Type: Article

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29. Atomic coordinates have been deposited with the Protein Data Bank at Rutgers University (http://rcsb.rutgers.edu/pdb/index.html). PDBid codes for 1 and 11 are 2BT0 and 2BSM, respectively.