Document Detail


Modulation of epigenetic targets for anticancer therapy: clinicopathological relevance, structural data and drug discovery perspectives.
MedLine Citation:
PMID:  23016851     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Research on cancer epigenetics has flourished in the last decade. Nevertheless growing evidence point on the importance to understand the mechanisms by which epigenetic changes regulate the genesis and progression of cancer growth. Several epigenetic targets have been discovered and are currently under validation for new anticancer therapies. Drug discovery approaches aiming to target these epigenetic enzymes with small-molecules inhibitors have produced the first pre-clinical and clinical outcomes and many other compounds are now entering the pipeline as new candidate epidrugs. The most studied targets can be ascribed to histone deacetylases and DNA methyltransferases, although several other classes of enzymes are able to operate post-translational modifications to histone tails are also likely to represent new frontiers for therapeutic interventions. By acknowledging that the field of cancer epigenetics is evolving with an impressive rate of new findings, with this review we aim to provide a current overview of pre-clinical applications of smallmolecules for cancer pathologies, combining them with the current knowledge of epigenetic targets in terms of available structural data and drug design perspectives.
Authors:
Federico Andreoli; Arménio Jorge Moura Barbosa; Marco Daniele Parenti; Alberto Del Rio
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review    
Journal Detail:
Title:  Current pharmaceutical design     Volume:  19     ISSN:  1873-4286     ISO Abbreviation:  Curr. Pharm. Des.     Publication Date:  2013  
Date Detail:
Created Date:  2013-01-23     Completed Date:  2013-07-08     Revised Date:  2013-07-11    
Medline Journal Info:
Nlm Unique ID:  9602487     Medline TA:  Curr Pharm Des     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  578-613     Citation Subset:  IM    
Affiliation:
Department of Experimental Pathology, Alma Mater Studiorum - University of Bologna, Via S.Giacomo 14, 40126 Bologna, Italy.
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MeSH Terms
Descriptor/Qualifier:
Animals
Antineoplastic Agents / pharmacology*
Disease Progression
Drug Design
Drug Discovery / methods
Epigenesis, Genetic*
Humans
Molecular Targeted Therapy
Neoplasms / drug therapy*,  genetics,  pathology
Chemical
Reg. No./Substance:
0/Antineoplastic Agents
Comments/Corrections

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