Systems approaches to polypharmacology and drug discovery

Aislyn D.W. Boran, Ravi Iyengar

Research output: Contribution to journalReview articlepeer-review

263 Scopus citations


Systems biology uses experimental and computational approaches to characterize large sample populations systematically, process large datasets, examine and analyze regulatory networks, and model reactions to determine how components are joined to form functional systems. Systems biology technologies, data and knowledge are particularly useful in understanding disease processes and drug actions. An important area of integration between systems biology and drug discovery is the concept of polypharmacology: the treatment of diseases by modulating more than one target. Polypharmacology for complex diseases is likely to involve multiple drugs acting on distinct targets that are part of a network regulating physiological responses. This review discusses the current state of the systems-level understanding of diseases and both the therapeutic and adverse mechanisms of drug actions. Drug-target networks can be used to identify multiple targets and to determine suitable combinations of drug targets or drugs. Thus, the discovery of new drug therapies for complex diseases may be greatly aided by systems biology.

Original languageEnglish
Pages (from-to)297-309
Number of pages13
JournalCurrent Opinion in Drug Discovery and Development
Issue number3
StatePublished - May 2010


  • Drug discovery
  • drug resistance
  • polypharmacology
  • regulatory network
  • systems biology
  • targeted therapy


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