Scorpion Peptides and Ion Channels: An Insightful Review of Mechanisms and Drug Development

Mendes, Laís Campelo; Viana, Gabriela Magnólia Melo; Nencioni, Ana Leonor Abrahão; Pimenta, Daniel C.; Beraldo-Neto, Emidio

doi:10.3390/toxins15040238

Cited by 11 publications

(7 citation statements)

References 141 publications

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“…These toxins contain residue of lysine in position 34 (K 34 ) in their sequences, which could be the principal interaction mode with the potassium channel [ 26 ]. The CnErg1 toxin blocks the Kv11.1 and 11.3 channels in a closed state in humans and rats [ 27 ], while the CmERG1 toxin only blocks the Kv11.1 channel [ 28 ]. The CpoKTxGam05_01 sequence was identified in the proteome, where two unique peptides were identified ( Supplementary Table S2 ).…”

Section: Resultsmentioning

confidence: 99%

Unveiling the Protein Components of the Secretory-Venom Gland and Venom of the Scorpion Centruroides possanii (Buthidae) through Omic Technologies

García-Villalvazo

Jiménez-Vargas

Lino-López³

et al. 2023

Toxins

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Centruroides possanii is a recently discovered species of “striped scorpion” found in Mexico. Certain species of Centruroides are known to be toxic to mammals, leading to numerous cases of human intoxications in the country. Venom components are thought to possess therapeutic potential and/or biotechnological applications. Hence, obtaining and analyzing the secretory gland transcriptome and venom proteome of C. possanii is relevant, and that is what is described in this communication. Since this is a newly described species, first, its LD50 to mice was determined and estimated to be 659 ng/g mouse weight. Using RNA extracted from this species and preparing their corresponding cDNA fragments, a transcriptome analysis was obtained on a Genome Analyzer (Illumina) using the 76-base pair-end sequencing protocol. Via high-throughput sequencing, 19,158,736 reads were obtained and ensembled in 835,204 sequences. Of them, 28,399 transcripts were annotated with Pfam. A total of 244 complete transcripts were identified in the transcriptome of C. possanii. Of these, 109 sequences showed identity to toxins that act on ion channels, 47 enzymes, 17 protease inhibitors (PINs), 11 defense peptides (HDPs), and 60 in other components. In addition, a sample of the soluble venom obtained from this scorpion was analyzed using an Orbitrap Velos apparatus, which allowed for identification by liquid chromatography followed by mass spectrometry (LC-MS/MS) of 70 peptides and proteins: 23 toxins, 27 enzymes, 6 PINs, 3 HDPs, and 11 other components. Until now, this work has the highest number of scorpion venom components identified through omics technologies. The main novel findings described here were analyzed in comparison with the known data from the literature, and this process permitted some new insights in this field.

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Section: Resultsmentioning

confidence: 99%

Unveiling the Protein Components of the Secretory-Venom Gland and Venom of the Scorpion Centruroides possanii (Buthidae) through Omic Technologies

García-Villalvazo

Jiménez-Vargas

Lino-López³

et al. 2023

Toxins

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“…In addition to neurotoxins, promising sources in the treatment of channelopathies, 13 scorpion venoms contain a wide range of other molecules with interesting therapeutic properties, making them a valuable source of bioactive molecules that can serve as the basis for developing new drugs for the treatment of various diseases. 14 The literature reports the anticancer potential, and against pathogen infections, such as antimicrobial, antifungal, antiviral, antimalarial, antitrypanosoma and antileishmanial effects.…”

Section: Discussionmentioning

confidence: 99%

In vitro activity of Tityus metuendus and Brotheas amazonicus scorpion venoms against Plasmodium falciparum FRC3

Procópio,

Pereira,

Martins

et al. 2024

IJMMTD

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Scorpion venoms contain different classes of molecules with possible pharmacological activities, making them sources of bioactive molecules for the development of new drugs against infections caused by pathogens, such as malaria, a disease caused by protozoa of the genus Plasmodium. Malaria faces challenges in its control due to pathogen resistance to available antimalarials. In this study, we evaluated the venom activity of the Amazonian scorpions and against FRC3, the analysis was performed by flow cytometry. At the analyzed concentrations, we found that the crude venom of had an average inhibition of 87% at the concentration of 100 µg/mL, above that obtained with the drug (quinine), which had mean inhibition of 84% against FCR3. Regarding the venom of , lower activity was observed in comparison with the inhibition potential of the venom and the standard drug, venom showed low toxicity against the human fibroblast MRC5. Because peptides and toxins from scorpion venom are related to biological functions, they can be used in the design of new therapeutic agents, with venom being a possible source of molecules for the development of antimalarial drugs.

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“…There is a vast and growing canon of animal and plant venom peptide toxins used as pharmacological tools and as potential therapeutics targeting ion channels (for reviews see: Cardoso, 2020 ; Dueñas-Cuellar et al, 2020 ; Groome, 2023 ; Luo et al, 2022 ; Mendes et al, 2023 ; Nogueira Souza et al, 2023 ; Osipov and Utkin, 2023 ; Talukdar et al, 2023 ; Wulff et al, 2019 ). Soricin, one such toxin from the Northern short-tailed shrew ( Blarina brevicauda ), shortened to the C-terminal 13mer peptide (SOR-C13), was shown to be a potent TRPV6 blocker (IC 50 = 14 nM).…”

Section: Clinical Research Example 2—trpv6 In Calcium Homeostasis Gen...mentioning

confidence: 99%

News and views on ion channels in cancer: is cancer a channelopathy?

Bell,

Leanza,

Gentile

et al. 2023

Front. Pharmacol.

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Ion channels are key signaling proteins found throughout the body; they are critical in many, wide-ranging physiological processes, from gene expression, sensory perception and processing to the cardiac action potential. When ion channel activity goes awry, for example, via mutation, damage or disrupted homeostasis, the outcome can result in causation, development and/or maintenance of disease. Ion channel dependent diseases have been dubbed channelopathies. Recent studies on the role of ion channels in cancer biology suggest that cancer is one such channelopathy. Many ion channels have now been implicated in the cellular processes that are affected in a multitude of cancers. In the last two decades, the field of ion channel and cancer research has been growing exponentially: a combination of developments in molecular biology, genetics, electrophysiology and automation have driven an explosion in our capabilities to interrogate ion channel pathways; how, why and where they go wrong and therapeutic interventions to correct their pathophysiology in cancer. A review of this vast and rapidly developing field would require a titanic tome to merely dimple the surface of research that has ballooned recently. In lieu of that huge undertaking—for the benefit of both authors and readers - this review discusses select examples of primary, applied and clinical research, aiming to shine a light on some of the more innovative and novel findings that this exciting field is excavating.

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Scorpion Peptides and Ion Channels: An Insightful Review of Mechanisms and Drug Development

Cited by 11 publications

References 141 publications

Unveiling the Protein Components of the Secretory-Venom Gland and Venom of the Scorpion Centruroides possanii (Buthidae) through Omic Technologies

Unveiling the Protein Components of the Secretory-Venom Gland and Venom of the Scorpion Centruroides possanii (Buthidae) through Omic Technologies

In vitro activity of Tityus metuendus and Brotheas amazonicus scorpion venoms against Plasmodium falciparum FRC3

News and views on ion channels in cancer: is cancer a channelopathy?

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