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Authors: Freitas, Ana C. N.
Peigneur, Steve
Macedo, Flávio H. P.
Menezes-Filho, José E.
Millns, Paul
Medeiros, Liciane Fernandes
Arruda, Maria A.
Cruz, Jader
Holliday, Nicholas D.
Tytgat, Jan
Hathway, Gareth
Lima, Maria E. de
Title: The Peptide PnPP-19, a Spider Toxin Derivative, Activates µ-Opioid Receptors and Modulates Calcium Channels
Keywords: Phoneutria nigriventer;Opioid receptor;Spider toxin;Antinociception
Issue Date: 2018
Publisher: Multidisciplinary Digital Publishing Institute
Citation: FREITAS, A. C. N. et al. The Peptide PnPP-19, a Spider Toxin Derivative, Activates µ-Opioid Receptors and Modulates Calcium Channels. Toxins, v. 10, n. 1, jan. 2018. Disponível em: Acesso em: 03 ago. 2021.
Abstract: The synthetic peptide PnPP-19 comprehends 19 amino acid residues and it represents part of the primary structure of the toxin δ-CNTX-Pn1c (PnTx2-6), isolated from the venom of the spider Phoneutria nigriventer. Behavioural tests suggest that PnPP-19 induces antinociception by activation of CB1, µ and δ opioid receptors. Since the peripheral and central antinociception induced by PnPP-19 involves opioid activation, the aim of this work was to identify whether this synthetic peptide could directly activate opioid receptors and investigate the subtype selectivity for µ-, δ- and/or κ-opioid receptors. Furthermore, we also studied the modulation of calcium influx driven by PnPP-19 in dorsal root ganglion neurons, and analyzed whether this modulation was opioid-mediated. PnPP-19 selectively activates µ-opioid receptors inducing indirectly inhibition of calcium channels and hereby impairing calcium influx in dorsal root ganglion (DRG) neurons. Interestingly, notwithstanding the activation of opioid receptors, PnPP-19 does not induce β-arrestin2 recruitment. PnPP-19 is the first spider toxin derivative that, among opioid receptors, selectively activates µ-opioid receptors. The lack of β-arrestin2 recruitment highlights its potential for the design of new improved opioid agonists.
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