Targeting T-type/CaV3.2 Channels for Chronic Pain

Overview

Journal Transl Res

Publisher Elsevier

Specialty Pathology

Date 2021 Jan 10

PMID 33422652

Citations 35

Authors

Song Cai

Kimberly Gomez

Aubin Moutal

Rajesh Khanna

Affiliations

Soon will be listed here.

Abstract

T-type calcium channels regulate neuronal excitability and are important contributors of pain processing. CaV3.2 channels are the major isoform expressed in nonpeptidergic and peptidergic nociceptive neurons and are emerging as promising targets for pain treatment. Numerous studies have shown that CaV3.2 expression and/or activity are significantly increased in spinal dorsal horn and in dorsal root ganglia neurons in different inflammatory and neuropathic pain models. Pharmacological campaigns to inhibit the functional expression of CaV3.2 for treatment of pain have focused on the development of direct channel blockers, but none have produced lead candidates. Targeting the proteins that regulate the trafficking or transcription, and the ones that modify the channels via post-translational modifications are alternative means to regulate expression and function of CaV3.2 channels and hence to develop new drugs to control pain. Here we synthesize data supporting a role for CaV3.2 in numerous pain modalities and then discuss emerging opportunities for the indirect targeting of CaV3.2 channels.

Citing Articles

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A non-conducting role of the Ca1.4 Ca channel drives homeostatic plasticity at the cone photoreceptor synapse.

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SUMOylation and DeSUMOylation: Tug of War of Pain Signaling.

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