Document Detail

PARP inhibitors in cancer therapy: an update.
MedLine Citation:
PMID:  23379721     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: Inhibitors of the poly(ADP-ribose) polymerases (PARPs) family of proteins are currently being evaluated as potential anticancer medicines at both preclinical and clinical levels. They have the peculiarity to increase the efficacy of DNA-damaging agents and to selectively target tumor cells with specific DNA repair defects. This later development of these drugs should make it possible, in principle, to selectively target neoplastic vs healthy cells, thus realizing the Ehrlich's magic bullet concept of a personalized and tailored cure of diseases.
AREAS COVERED: This review is designed to provide the readers with a brief summary and an update on PARP inhibitors in the oncology field, by covering the recent patent literature (2010 - 2012: and Questel Intellectual Property Portal [QPat] database search).
EXPERT OPINION: Presently, along with a number of preclinical candidates, there are eight PARP inhibitors in the clinic as either single agents or in combination with various chemotherapy and radiotherapy regimens. The tremendous efforts underneath those results testify the high interest on the target. The investigation and understanding of the cross-reactivity among members of the PARPs family as well as a deeper knowledge of their biological functions may lead to a more profound characterization of the PARP inhibitor's profile. This, in turn, will cast additional light on this exciting approach in treating cancer.
Gianluca Papeo; Elena Casale; Alessia Montagnoli; Alessandra Cirla
Publication Detail:
Type:  Journal Article; Review     Date:  2013-02-05
Journal Detail:
Title:  Expert opinion on therapeutic patents     Volume:  23     ISSN:  1744-7674     ISO Abbreviation:  Expert Opin Ther Pat     Publication Date:  2013 Apr 
Date Detail:
Created Date:  2013-03-14     Completed Date:  2013-09-03     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:  503-14     Citation Subset:  IM    
Nerviano Medical Sciences, Department of Medicinal Chemistry, Nerviano (MI), Italy.
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MeSH Terms
Antineoplastic Agents / chemistry,  pharmacology*,  therapeutic use
Drug Design
Drug and Narcotic Control
Enzyme Inhibitors / chemistry,  pharmacology*,  therapeutic use
Molecular Structure
Molecular Targeted Therapy*
Neoplasms / drug therapy*,  enzymology,  pathology
Patents as Topic
Poly(ADP-ribose) Polymerases / antagonists & inhibitors*,  metabolism
Signal Transduction / drug effects
Structure-Activity Relationship
Reg. No./Substance:
0/Antineoplastic Agents; 0/Enzyme Inhibitors; EC Polymerases

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