[HTML][HTML] In vivo spatiotemporal control of voltage-gated ion channels by using photoactivatable peptidic toxins

…, S Nicolas, D Chu, C Caumes, R Béroud… - Nature …, 2022 - nature.com
Photoactivatable drugs targeting ligand-gated ion channels open up new opportunities for
light-guided therapeutic interventions. Photoactivable toxins targeting ion channels have the …

[HTML][HTML] Chemical Synthesis, Proper Folding, Nav Channel Selectivity Profile and Analgesic Properties of the Spider Peptide Phlotoxin 1

…, S Diochot, E Cuypers, S De Waard, R Béroud… - Toxins, 2019 - mdpi.com
Phlotoxin-1 (PhlTx1) is a peptide previously identified in tarantula venom (Phlogius species)
that belongs to the inhibitory cysteine-knot (ICK) toxin family. Like many ICK-based spider …

From identification to functional characterization of cyriotoxin‐1a, an antinociceptive toxin from the spider Cyriopagopus schioedtei

…, L Bialy, S Hourcade, R Béroud… - British journal of …, 2019 - Wiley Online Library
Background and Purpose The Na V 1.7 channel is highly expressed in dorsal root ganglia
of the sensory nervous system and plays a central role in the pain signalling process. We …

2-Hydroxy-4-methoxybenzyl as a Thiol-Protecting Group for Directed-Disulfide Bond Formation

C Zoukimian, R Béroud, D Boturyn - Organic Letters, 2022 - ACS Publications
The chemical synthesis of disulfide-rich peptides such as toxins can be accomplished by using
numerous orthogonal cysteine-protecting groups. Herein we report the use of the Hmb off/…

[HTML][HTML] Structure-function relationship of new peptides activating human Nav1. 1

…, M Mantegazza, J Tytgat, C Cohen, R Béroud… - Biomedicine & …, 2023 - Elsevier
Na v 1.1 is an important pharmacological target as this voltage-gated sodium channel is
involved in neurological and cardiac syndromes. Channel activators are actively sought to try to …

Fluorescent‐ and tagged‐protoxin II peptides: potent markers of the Nav1.7 channel pain target

…, M Mantegazza, R Boukaiba, R Béroud… - British Journal of …, 2021 - Wiley Online Library
Background and Purpose Protoxin II (ProTx II) is a high affinity gating modifier that is thought
to selectively block the Na v 1.7 voltage‐dependent Na + channel, a major therapeutic …

[HTML][HTML] MT9, a natural peptide from black mamba venom antagonizes the muscarinic type 2 receptor and reverses the M2R-agonist-induced relaxation in rat and …

…, G Blanchet, C Gauthier-Erfanian, R Beroud… - Biomedicine & …, 2022 - Elsevier
All five muscarinic receptors have important physiological roles. The endothelial M2 and M3
subtypes regulate arterial tone through direct coupling to Gq or Gi/o proteins. Yet, we lack …

From a Cone Snail Toxin to a Competitive MC4R Antagonist

…, P Kessler, L Konnert, R Beroud… - Journal of Medicinal …, 2022 - ACS Publications
The melanocortin 4 receptor (MC4R) plays a role in energy homeostasis and represents a
target for treating energy balance disorders. For decades, synthetic ligands have been …

Synthesis by native chemical ligation and characterization of the scorpion toxin AmmTx3

…, KA Ouares, S Nicolas, M Canepari, R Béroud… - Bioorganic & Medicinal …, 2019 - Elsevier
The scorpion toxin AmmTx3 is a specific blocker of K v 4 channels. It was shown to have
interesting potential for neurological disorders. In this study, we report the first chemical …

Heterodimeric insecticidal peptide provides new insights into the molecular and functional diversity of ant venoms

…, M Triquigneaux, L Jaquillard, R Beroud… - ACS Pharmacology & …, 2020 - ACS Publications
Ants use venom for predation, defense, and communication; however, the molecular diversity,
function, and potential applications of ant venom remains understudied compared to other …