Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 1, 2014, Pages 204-208

  Ernst, Justin T ^a   Liu, Michael ^a   Zuccola, Harmon ^a   Neubert, Timothy ^a   Beaumont, Kevin ^a   Turnbull, Amy ^a   Kallel, Adam ^a   Vought, Bryan ^a   Stamos, Dean ^a  

^a VERTEX PHARMACEUTICALS   (United States)

Author keywords

GRP94; HSP90 inhibitors; Huntingtin; Huntington's disease; Isoform selectivity; Structure based drug design; TRAP1

Indexed keywords

ALVESPIMYCIN; BIIB 021; GLUCOSE REGULATED PROTEIN 94; HEAT SHOCK PROTEIN; HEAT SHOCK PROTEIN 75; HEAT SHOCK PROTEIN 90; HEAT SHOCK PROTEIN 90 ALPHA; HEAT SHOCK PROTEIN 90 BETA; HEAT SHOCK PROTEIN 90 INHIBITOR; LUMINESPIB; SNX 2112; UNCLASSIFIED DRUG; 2 AMINO 6 CHLORO 9 [(4 METHOXY 3,5 DIMETHYL 2 PYRIDINYL)METHYL]PURINE; BEP800; CENTRAL NERVOUS SYSTEM AGENTS; HSP 90ABETA PROTEIN; HSP 90ALPHA PROTEIN; HUNTINGTIN; ISOPROTEIN; MITOCHONDRIAL PROTEIN; MUTANT PROTEIN; SNX0723; SNX2112; TRAP1 PROTEIN;

ALPHA HELIX; ARTICLE; BINDING ASSAY; CONFORMATIONAL TRANSITION; CRYSTAL STRUCTURE; DEGENERATIVE DISEASE; DRUG DESIGN; DRUG PROTEIN BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG TARGETING; ENDOPLASMIC RETICULUM; FLUORESCENCE POLARIZATION; HYDROGEN BOND; MITOCHONDRION; PROTEIN CONFORMATION; CORRELATIONAL STUDY; DRUG CONFORMATION; DRUG MECHANISM; DRUG SYNTHESIS; EMBRYO; GENE SILENCING; HUMAN; HUMAN CELL; IN VITRO STUDY; STRUCTURE ACTIVITY RELATION;

GRP94; HSP90 INHIBITORS; HUNTINGTIN; HUNTINGTON'S DISEASE; ISOFORM SELECTIVITY; STRUCTURE-BASED DRUG DESIGN; TRAP1;

CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HSP90 HEAT-SHOCK PROTEINS; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NEURODEGENERATIVE DISEASES; PROTEIN ISOFORMS;

EID: 84891484732     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.11.036     Document Type: Article

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