Document Detail


Objective assessment of cancer genes for drug discovery.
MedLine Citation:
PMID:  23274470     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
Selecting the best targets is a key challenge for drug discovery, and achieving this effectively, efficiently and systematically is particularly important for prioritizing candidates from the sizeable lists of potential therapeutic targets that are now emerging from large-scale multi-omics initiatives, such as those in oncology. Here, we describe an objective, systematic, multifaceted computational assessment of biological and chemical space that can be applied to any human gene set to prioritize targets for therapeutic exploration. We use this approach to evaluate an exemplar set of 479 cancer-associated genes, reveal the tension between biological relevance and chemical tractability, and describe major gaps in available knowledge that could be addressed to aid objective decision-making. We also propose drug repurposing opportunities and identify potentially druggable cancer-associated proteins that have been poorly explored with regard to the discovery of small-molecule modulators, despite their biological relevance.
Authors:
Mishal N Patel; Mark D Halling-Brown; Joseph E Tym; Paul Workman; Bissan Al-Lazikani
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Nature reviews. Drug discovery     Volume:  12     ISSN:  1474-1784     ISO Abbreviation:  Nat Rev Drug Discov     Publication Date:  2012 Dec 
Date Detail:
Created Date:  2012-12-31     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101124171     Medline TA:  Nat Rev Drug Discov     Country:  England    
Other Details:
Languages:  eng     Pagination:  35-50     Citation Subset:  IM    
Affiliation:
Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, UK.
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