| Systematic exploration of dual-acting modulators from a combined medicinal chemistry and biology perspective. | |
| | |
MedLine Citation:
|
PMID: 23281966 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
|
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. |
| | |
Authors:
|
Aurelie Bornot; Udo Bauer; Alastair Brown; Mike Firth; Caroline Hellawell; Ola Engkvist |
Related Documents
:
|
21257506 - Disease due to salmonella diagnosed in cattle and pigs in scotland. 23594086 - Stories of chronic kidney disease: listening for the unsayable. 23055696 - Current and novel drug therapies for idiopathic pulmonary fibrosis. 21428176 - Do cardio-vascular and periodontal diseases have a close, causal relationship? 15768036 - 19f and 1h mri detection of amyloid beta plaques in vivo. 23083986 - Histopathology of celiac disease. |
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: - |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
|
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Thyroid hormone replacement therapy attenuates the decline of renal function in chronic kidney disea...
Next Document: Solid-contact ion-selective electrodes with novel highly selective thioamide derivatives of p-tert-b...