Document Detail

Systematic exploration of dual-acting modulators from a combined medicinal chemistry and biology perspective.
MedLine Citation:
PMID:  23281966     Owner:  NLM     Status:  Publisher    
The traditional drug discovery strategy of pursuing "one compound - one target" has had difficulties delivering novel therapies for complex diseases currently lacking adequate treatments. An alternative and complementary approach is the design of multi-targeted modulators simultaneously addressing multiple pathological mechanisms or overcoming pathway robustness. In this study, we propose a methodology to increase the probability of success for developing dual-acting modulators by systematically and rationally evaluating all dual-acting modulator opportunities within a specific disease area. This approach employs a combination of a five-step medicinal chemistry evaluation and a two-step biological analysis to help select the optimal target combination. It provides a novel methodology suitable for widespread application across disease areas. To exemplify the power of this approach, we focus on an analysis of the gastrointestinal (GI) disease area to identify opportunities supported by current literature data.
Aurelie Bornot; Udo Bauer; Alastair Brown; Mike Firth; Caroline Hellawell; Ola Engkvist
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-1-3
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2013 Jan 
Date Detail:
Created Date:  2013-1-3     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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