Purine-scaffold Hsp90 inhibitors Journal Article


Authors: Taldone, T.; Chiosis, G.
Article Title: Purine-scaffold Hsp90 inhibitors
Abstract: Hsp90 is a molecular chaperone with important roles in regulating the function of several proteins with potential pathogenic activity. Because many of these proteins are involved in cancer and neurodegenerative promoting pathways, Hsp90 has emerged as an attractive therapeutic target in these diseases. Molecules that bind to the N-terminal nucleotide pocket of Hsp90 inhibit its activity, and consequently, disrupt client protein function. A number of these inhibitors from several chemical classes are now known, and some are already in clinical trials. This review focuses on the purine class of Hsp90 inhibitors, their discovery through rational design, and on efforts aimed towards their optimization and development into clinically viable drugs for the treatment of cancer. Their potential towards neurodegenerative diseases will also be touched upon. © 2009 Bentham Science Publishers Ltd.
Keywords: unclassified drug; review; liver cell carcinoma; nonhuman; drug targeting; antineoplastic agent; protein function; animals; breast cancer; antineoplastic activity; drug design; structure activity relation; structure-activity relationship; cancer therapy; lung small cell cancer; b cell lymphoma; drug research; amino terminal sequence; 17 demethoxy 17 (2 dimethylaminoethylamino)geldanamycin; heat shock protein 90 inhibitor; tanespimycin; heat shock protein 90; single drug dose; hsp90 heat-shock proteins; stomach cancer; purines; purine derivative; alzheimer disease; degenerative disease; neurodegeneration; purine; 5 (2,4 dihydroxy 5 isopropylphenyl) 4 (4 morpholinomethylphenyl) 3 isoxazolecarboxylic acid ethylamide; 8 benzothiazolothiopurine; 8 benzylpurine methylene; 8 pyridinothiazolothiopurine; 8 sulfanyladenine; 8 sulfanylpurine sulfur; purine 3; purine h 71; snx 2112; tanespimycin hydroquinone; frontotemporal dementia
Journal Title: Current Topics in Medicinal Chemistry
Volume: 9
Issue: 15
ISSN: 1568-0266
Publisher: Bentham Science Publishers  
Date Published: 2009-01-01
Start Page: 1436
End Page: 1446
Language: English
DOI: 10.2174/156802609789895737
PUBMED: 19860732
PROVIDER: scopus
PMCID: PMC4699796
DOI/URL:
Notes: --- - "Cited By (since 1996): 4" - "Export Date: 30 November 2010" - "CODEN: CTMCC" - "Source: Scopus"
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MSK Authors
  1. Gabriela Chiosis
    216 Chiosis
  2. Tony Taldone
    74 Taldone
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