Document Detail

Tankyrase-targeted therapeutics: expanding opportunities in the PARP family.
MedLine Citation:
PMID:  23197039     Owner:  NLM     Status:  In-Data-Review    
The poly(ADP-ribose) polymerase (PARP) protein superfamily has wide-ranging roles in cellular processes such as DNA repair and WNT signalling. Efforts to pharmacologically target PARP enzymes have largely focused on PARP1 and the closely related PARP2, but recent work highlighting the role of another family member, tankyrase 1 (TANK1; also known as PARP5A and ARTD5), in the control of WNT signalling has fuelled interest in the development of additional inhibitors to target this enzyme class. Tankyrase function is also implicated in other processes such as the regulation of telomere length, lung fibrogenesis and myelination, suggesting that tankyrase inhibitors could have broad clinical utility. Here, we discuss the biology of tankyrases and the discovery of tankyrase-specific inhibitors. We also consider the challenges that lie ahead for the clinical development of PARP family inhibitors in general.
Jenna L Riffell; Christopher J Lord; Alan Ashworth
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Nature reviews. Drug discovery     Volume:  11     ISSN:  1474-1784     ISO Abbreviation:  Nat Rev Drug Discov     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-11-30     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101124171     Medline TA:  Nat Rev Drug Discov     Country:  England    
Other Details:
Languages:  eng     Pagination:  923-36     Citation Subset:  IM    
The Breakthrough Breast Cancer Research Centre, Institute of Cancer Research, Fulham Road, London SW3 6JB, UK.
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