4.5 Review

Rational application of drug promiscuity in medicinal chemistry

Journal

FUTURE MEDICINAL CHEMISTRY
Volume 10, Issue 15, Pages 1835-1851

Publisher

FUTURE SCI LTD
DOI: 10.4155/fmc-2018-0018

Keywords

drug repurposing; druggability; multi-target drug; polypharmacology; promiscuity

Funding

  1. Natural Science Research Foundation of Huaian, Jiangsu China [HAB201711, HAB201712, HAG201613]
  2. State Key Program Foundation of Jiangsu Food & Pharmaceutical Science College [JSSPZD2017101]

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'Drug promiscuity' refers to a drug that can act on multiple molecular targets, exhibiting similar or different pharmacological effects. Drugs may interact with unwanted targets, leading to off-target effects (one of the main reasons for side effects). Thus, intervention to prevent off-target effects in the early stages of drug discovery could reduce the risk of failure. The conversion between target and off-target effects is important for drug repurposing. Drug repurposing strategies could reduce research and development costs. This review details the research progress in the rational application of drug promiscuity for the discovery of multi-target drugs, drug repurposing and improving druggability in medicinal chemistry over the last 5 years.

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