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The Role of Toxins in the Pursuit for Novel Analgesics

The Institute for Drug Research (IDR), School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 9112001, Israel
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Toxins 2019, 11(2), 131;
Received: 24 January 2019 / Revised: 17 February 2019 / Accepted: 20 February 2019 / Published: 23 February 2019
(This article belongs to the Special Issue From Toxins to Drugs)
PDF [2097 KB, uploaded 23 February 2019]


Chronic pain is a major medical issue which reduces the quality of life of millions and inflicts a significant burden on health authorities worldwide. Currently, management of chronic pain includes first-line pharmacological therapies that are inadequately effective, as in just a portion of patients pain relief is obtained. Furthermore, most analgesics in use produce severe or intolerable adverse effects that impose dose restrictions and reduce compliance. As the majority of analgesic agents act on the central nervous system (CNS), it is possible that blocking pain at its source by targeting nociceptors would prove more efficient with minimal CNS-related side effects. The development of such analgesics requires the identification of appropriate molecular targets and thorough understanding of their structural and functional features. To this end, plant and animal toxins can be employed as they affect ion channels with high potency and selectivity. Moreover, elucidation of the toxin-bound ion channel structure could generate pharmacophores for rational drug design while favorable safety and analgesic profiles could highlight toxins as leads or even as valuable therapeutic compounds themselves. Here, we discuss the use of plant and animal toxins in the characterization of peripherally expressed ion channels which are implicated in pain. View Full-Text
Keywords: TRPV1; TRPA1; ASIC; NaV channels; chronic pain; analgesics; toxins; pharmacophore. TRPV1; TRPA1; ASIC; NaV channels; chronic pain; analgesics; toxins; pharmacophore.

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Maatuf, Y.; Geron, M.; Priel, A. The Role of Toxins in the Pursuit for Novel Analgesics. Toxins 2019, 11, 131.

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