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Polypharmacology: challenges and opportunities in drug discovery.

Abstract：

: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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Anighoro A,Bajorath J,Rastelli G

doi

10.1021/jm5006463

subject

Has Abstract

pub_date

2014-10-09 00:00:00

pages

7874-87

issue

19

eissn

0022-2623

issn

1520-4804

journal_volume

57

pub_type

杂志文章,评审

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