期刊
BIOCHEMICAL PHARMACOLOGY
卷 181, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bcp.2020.114129
关键词
Venom peptide drug discovery; Pharmacological probes; Neuropeptides; Selectivity; G protein-coupled receptor (GPCR)
资金
- European Research Council under the European Union [714366]
- Australian Research Council [DE150100784, DP190101667]
- European Research Council (ERC) [714366] Funding Source: European Research Council (ERC)
- Australian Research Council [DE150100784] Funding Source: Australian Research Council
Neuropeptides are signalling molecules mainly secreted from neurons that act as neurotransmitters or peptide hormones to affect physiological processes and modulate behaviours. In humans, neuropeptides are implicated in numerous diseases and understanding their role in physiological processes and pathologies is important for therapeutic development. Teasing apart the (patho)physiology of neuropeptides remains difficult due to ligand and receptor promiscuity and the complexity of the signalling pathways. The current approach relies on a pharmacological toolbox of agonists and antagonists displaying high selectivity for independent receptor sub-types, with the caveat that only few selective ligands have been discovered or developed. Animal venoms represent an underexplored source for novel receptor subtype-selective ligands that could aid in dissecting human neuropeptide signalling systems. Multiple endogenous-like neuropeptides as well as peptides acting on neuropeptide receptors are present in venoms. In this review, we summarise current knowledge on neuropeptides and discuss venoms as a source for ligands targeting neuropeptide signalling systems.
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