Drug Discovery on Natural Products: From Ion Channels to nAChRs, from Nature to Libraries, from Analytics to Assays

Reka A. Otvos, Kristina B.M. Still, Govert W. Somsen, August B. Smit, Jeroen Kool*

*Corresponding author for this work

Research output: Contribution to JournalReview articleAcademicpeer-review

Abstract

Natural extracts are complex mixtures that may be rich in useful bioactive compounds and therefore are attractive sources for new leads in drug discovery. This review describes drug discovery from natural products and in explaining this process puts the focus on ion-channel drug discovery. In particular, the identification of bioactives from natural products targeting nicotinic acetylcholine receptors (nAChRs) and serotonin type 3 receptors (5-HT 3 Rs) is discussed. The review is divided into three parts: “Targets,” “Sources,” and “Approaches.” The “Targets” part will discuss the importance of ion-channel drug targets in general, and the α7-nAChR and 5-HT 3 Rs in particular. The “Sources” part will discuss the relevance for drug discovery of finding bioactive compounds from various natural sources such as venoms and plant extracts. The “Approaches” part will give an overview of classical and new analytical approaches that are used for the identification of new bioactive compounds with the focus on targeting ion channels. In addition, a selected overview is given of traditional venom-based drug discovery approaches and of diverse hyphenated analytical systems used for screening complex bioactive mixtures including venoms.

Original languageEnglish
Pages (from-to)362-385
Number of pages24
JournalSLAS Discovery
Volume24
Issue number3
DOIs
Publication statusPublished - 1 Mar 2019

Keywords

  • 5-hydroxytryptamine receptors (5-HT Rs)
  • bioactive mixture profiling
  • nicotinic acetylcholine receptors (nAChRs)
  • venoms and natural extracts drug discovery

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