Document Detail

DNA methyltransferase inhibitors in cancer: a chemical and therapeutic patent overview and selected clinical studies.
MedLine Citation:
PMID:  23033952     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: DNA methylation is an epigenetic modification that modulates gene expression without altering the DNA base sequence. It plays a crucial role in cancer by silencing tumor suppressor genes (TSG). The DNA methyltransferases (DNMT) are the enzymes that catalyze DNA methylation and they are interesting therapeutical targets since DNA methylation is reversible such that an aberrant hypermethylation of DNA can be reverted by inhibition of DNMTs. Today, two drugs are on the market for the treatment of myelodysplastic syndrome, azacitidine and decitabine.
AREAS COVERED: Here, we present a review of the patents describing the chemistry and biological activities of novel DNMT inhibitors and discuss select clinical studies.
EXPERT OPINION: DNMT inhibitors have shown efficacy in clinics. However, highly efficient and specific DNMT inhibitors have not yet been identified. Improving methods will certainly lead to the prediction of novel directly binding inhibitors in the future.
Jacques Fahy; Albert Jeltsch; Paola B Arimondo
Publication Detail:
Type:  Journal Article; Review     Date:  2012-10-03
Journal Detail:
Title:  Expert opinion on therapeutic patents     Volume:  22     ISSN:  1744-7674     ISO Abbreviation:  Expert Opin Ther Pat     Publication Date:  2012 Dec 
Date Detail:
Created Date:  2012-11-20     Completed Date:  2013-05-10     Revised Date:  2013-11-06    
Medline Journal Info:
Nlm Unique ID:  9516419     Medline TA:  Expert Opin Ther Pat     Country:  England    
Other Details:
Languages:  eng     Pagination:  1427-42     Citation Subset:  IM    
USR 3388 Epigenetic Targeting of Cancer, CNRS-Pierre Fabre, CRDPF, BP 13562, 3 avenue Hubert Curien, 31 035 Toulouse CEDEX 01, France.
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MeSH Terms
Antineoplastic Agents / chemistry,  pharmacology*,  therapeutic use
Cell Line
DNA Methylation / drug effects
DNA Modification Methylases / antagonists & inhibitors*,  genetics,  metabolism
Drug Design*
Enzyme Inhibitors / chemistry,  pharmacology*,  therapeutic use
Epigenesis, Genetic / drug effects
Gene Expression Regulation, Neoplastic / drug effects
High-Throughput Screening Assays
Molecular Structure
Patents as Topic*
Protein Conformation
Structure-Activity Relationship
Reg. No./Substance:
0/Antineoplastic Agents; 0/Enzyme Inhibitors; EC 2.1.1.-/DNA Modification Methylases

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