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Marine Drugs
Volume 20
Issue 12
10.3390/md20120773
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Review

Conus regius-Derived Conotoxins: Novel Therapeutic Opportunities from a Marine Organism

by
Francesco Margiotta
1,
Laura Micheli
1,
Clara Ciampi
1,
Carla Ghelardini
1,
J. Michael McIntosh
2,3,4 and
Lorenzo Di Cesare Mannelli
1,*
1
Department of Neuroscience, Psychology, Drug Research and Child Health—NEUROFARBA, Pharmacology and Toxicology Section, University of Florence, 50139 Florence, Italy
2
George E. Wohlen Veterans Affairs Medical Center, Salt Lake City, UT 84148, USA
3
Department of Psychiatry, University of Utah, Salt Lake City, UT 84108, USA
4
School of Biological Sciences University of Utah, Salt Lake City, UT 84112, USA
*
Author to whom correspondence should be addressed.
Mar. Drugs 2022, 20(12), 773; https://doi.org/10.3390/md20120773
Submission received: 7 November 2022 / Revised: 3 December 2022 / Accepted: 6 December 2022 / Published: 10 December 2022
(This article belongs to the Special Issue Conotoxin and Conotoxin Analogues: A Pharmacy Cabinet under the Sea)
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Abstract

Conus regius is a marine venomous mollusk of the Conus genus that captures its prey by injecting a rich cocktail of bioactive disulfide bond rich peptides called conotoxins. These peptides selectively target a broad range of ion channels, membrane receptors, transporters, and enzymes, making them valuable pharmacological tools and potential drug leads. C. regius-derived conotoxins are particularly attractive due to their marked potency and selectivity against specific nicotinic acetylcholine receptor subtypes, whose signalling is involved in pain, cognitive disorders, drug addiction, and cancer. However, the species-specific differences in sensitivity and the low stability and bioavailability of these conotoxins limit their clinical development as novel therapeutic agents for these disorders. Here, we give an overview of the main pharmacological features of the C. regius-derived conotoxins described so far, focusing on the molecular mechanisms underlying their potential therapeutic effects. Additionally, we describe adoptable chemical engineering solutions to improve their pharmacological properties for future potential clinical translation.
Keywords: alpha-conotoxins; nAChRs; alpha9alpha10 nAChRs; RgIA; RgIA analogues; RegIIA; RgIB; M-conotoxins; pain; neuropathic pain alpha-conotoxins; nAChRs; alpha9alpha10 nAChRs; RgIA; RgIA analogues; RegIIA; RgIB; M-conotoxins; pain; neuropathic pain

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MDPI and ACS Style

Margiotta, F.; Micheli, L.; Ciampi, C.; Ghelardini, C.; McIntosh, J.M.; Di Cesare Mannelli, L. Conus regius-Derived Conotoxins: Novel Therapeutic Opportunities from a Marine Organism. Mar. Drugs 2022, 20, 773. https://doi.org/10.3390/md20120773

AMA Style

Margiotta F, Micheli L, Ciampi C, Ghelardini C, McIntosh JM, Di Cesare Mannelli L. Conus regius-Derived Conotoxins: Novel Therapeutic Opportunities from a Marine Organism. Marine Drugs. 2022; 20(12):773. https://doi.org/10.3390/md20120773

Chicago/Turabian Style

Margiotta, Francesco, Laura Micheli, Clara Ciampi, Carla Ghelardini, J. Michael McIntosh, and Lorenzo Di Cesare Mannelli. 2022. "Conus regius-Derived Conotoxins: Novel Therapeutic Opportunities from a Marine Organism" Marine Drugs 20, no. 12: 773. https://doi.org/10.3390/md20120773

APA Style

Margiotta, F., Micheli, L., Ciampi, C., Ghelardini, C., McIntosh, J. M., & Di Cesare Mannelli, L. (2022). Conus regius-Derived Conotoxins: Novel Therapeutic Opportunities from a Marine Organism. Marine Drugs, 20(12), 773. https://doi.org/10.3390/md20120773

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