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J Med Chem. 2014 Oct 9;57(19):7874-87. doi: 10.1021/jm5006463. Epub 2014 Jun 25.

Polypharmacology: challenges and opportunities in drug discovery.

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Life Sciences Department, University of Modena and Reggio Emilia , Via Campi 183, 41125 Modena, Italy.


At present, the legendary magic bullet, i.e., a drug with high potency and selectivity toward a specific biological target, shares the spotlight with an emerging and alternative polypharmacology approach. Polypharmacology suggests that more effective drugs can be developed by specifically modulating multiple targets. It is generally thought that complex diseases such as cancer and central nervous system diseases may require complex therapeutic approaches. In this respect, a drug that "hits" multiple sensitive nodes belonging to a network of interacting targets offers the potential for higher efficacy and may limit drawbacks generally arising from the use of a single-target drug or a combination of multiple drugs. In this review, we will compare advantages and disadvantages of multitarget versus combination therapies, discuss potential drug promiscuity arising from off-target effects, comment on drug repurposing, and introduce approaches to the computational design of multitarget drugs.

[Indexed for MEDLINE]

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