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Venomous animals occupy one of the most successful evolutionary niches and occur on nearly every continent. They deliver venoms via biting and stinging apparatuses with the aim to rapidly incapacitate prey and deter predators. This has led to the evolution of venom components that act at a number of biological targets – including ion channels, G-protein coupled receptors, transporters and enzymes – with exquisite selectivity and potency, making venom-derived components attractive pharmacological tool compounds and drug leads. In recent years, plate-based pharmacological screening approaches have been introduced to accelerate venom-derived drug discovery. A range of assays are amenable to this purpose, including high-throughput electrophysiology, fluorescence-based functional and binding assays. However, despite these technological advances, the traditional activity-guided fractionation approach is time-consuming and resource-intensive. The combination of screening techniques suitable for miniaturization with sequence-based discovery approaches – supported by advanced proteomics, mass spectrometry, chromatography as well as synthesis and expression techniques – promises to further improve venom peptide discovery.Here, we discuss practical aspects of establishing a pipeline for venom peptide drug discovery with a particular emphasis on pharmacology and pharmacological screening approaches.This article is part of the Special Issue entitled ‘Venom-derived Peptides as Pharmacological Tools.’Venom peptides are a rich source of bioactives with therapeutic potential.Pharmacological screening is a validated venom peptide drug discovery approach.Assay-guided fractionation is particularly powerful combined with transcriptomics and proteomics.