Small Molecule Targeting NaV17 via Inhibition of the CRMP2-Ubc9 Interaction Reduces Pain in Chronic Constriction Injury (CCI) Rats

Authors

Jiahe Li
Harrison J Stratton
Sabina A Lorca
Peter M Grace
Rajesh Khanna

Publication Date

12-1-2022

Journal

Channels

Abstract

The voltage-gated sodium channel isoform NaV1.7 is a critical player in the transmission of nociceptive information. This channel has been heavily implicated in human genetic pain disorders and is a validated pain target. However, targeting this channel directly has failed, and an indirect approach - disruption of interactions with accessory protein partners - has emerged as a viable alternative strategy. We recently reported that a small-molecule inhibitor of CRMP2 SUMOylation, compound

Keywords

Animals, Constriction, Ganglia, Spinal, Hyperalgesia, Mice, NAV1.7 Voltage-Gated Sodium Channel, Nerve Tissue Proteins, Neuralgia, Rats

Comments

PMID: 34983286