Histone deacetylase inhibitors: Discovery and development as anticancer agents Journal Article


Authors: Marks, P. A.; Dokmanovic, M.
Article Title: Histone deacetylase inhibitors: Discovery and development as anticancer agents
Abstract: Histone deacetylase (HDAC) inhibitors are a new class of targeted anticancer agents. Several HDAC inhibitors are in clinical trials and have shown significant activity against a spectrum of both haematological and solid tumours at doses that are well tolerated by patients. HDACs and histone acetyltransferases can, by reversible acetylation, modify the structure and function of histones and proteins in transcription factor complexes, which are involved in the regulation of gene expression, as well as many non-histone proteins that are involved in regulating cell proliferation and cell death. HDAC inhibitors are a structurally diverse group of molecules; these agents selectively alter the expression of genes. HDAC inhibitors can induce cancer cell death, whereas normal cells are relatively resistant to HDAC inhibitor-induced cell death. © 2005 Ashley Publications.
Keywords: unclassified drug; fludarabine; histone deacetylase inhibitor; clinical trial; drug activity; drug tolerability; fatigue; review; angiogenesis inhibitor; diarrhea; drug potentiation; nonhuman; solid tumor; antineoplastic agents; antineoplastic agent; protein function; cell proliferation; nonhistone protein; animals; cell death; cell cycle; imatinib; unindexed drug; apoptosis; bortezomib; nausea; thrombocytopenia; vomiting; protein; transcription factor; drug structure; benzyloxycarbonylvalylalanylaspartyl fluoromethyl ketone; drug design; drug selectivity; drug delivery systems; gene expression regulation; hematologic malignancy; regulatory mechanism; enzyme inhibitors; histone; sulfonamide; cancer cell; vorinostat; histone deacetylase inhibitors; flavopiridol; drug bioavailability; heart arrhythmia; protein structure; anthracycline; histone deacetylases; valproic acid; histone deacetylase; protein modification; arylbutyric acid derivative; n (2 aminophenyl) 4 (3 pyridinylmethoxycarbonylaminomethyl)benzamide; 4 n acetyldinaline; trichostatin a; acetylation; depsipeptide; benzamide derivative; suberoylanilide hydroxamic acid; hydroxamic acid derivative; thioredoxin; histone acetyltransferase; histone acetyltransferases; fr 901228; oxamflatin; apicidin; bl 1521; carboxyxinnamic acid bishydroxamide
Journal Title: Expert Opinion on Investigational Drugs
Volume: 14
Issue: 12
ISSN: 1354-3784
Publisher: Taylor & Francis Group  
Date Published: 2005-12-01
Start Page: 1497
End Page: 1511
Language: English
DOI: 10.1517/13543784.14.12.1497
PUBMED: 16307490
PROVIDER: scopus
DOI/URL:
Notes: --- - "Cited By (since 1996): 141" - "Export Date: 24 October 2012" - "CODEN: EOIDE" - "Source: Scopus"
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