Unnamed inner-ear GPCR subtype on ciliated cells

This target is a G protein-coupled receptor (GPCR) located on the ciliated cells, specifically the hair cells, of the inner ear's organ of Corti. It is currently an undisclosed or unnamed target being developed by Perha Pharmaceuticals for the prevention of hearing loss. The receptor is targeted by a family of molecules known as Triskellines, which are potent and highly selective antagonists derived from the cyclin-dependent kinase (CDK) inhibitor roscovitine. Activation of this GPCR is implicated in the signaling pathways that lead to hair cell damage and death following exposure to ototoxic agents, such as cisplatin and aminoglycoside antibiotics, or acoustic trauma. By antagonizing this receptor, Triskellines provide significant otoprotection in animal models, preserving the structural and functional integrity of the sensory ciliated cells. The target represents a novel therapeutic approach to addressing avoidable causes of deafness and associated risks of cognitive decline.

Other names

Undisclosed GPCR target of TriskellinesPerha Pharmaceuticals GPCR targetOtoprotective GPCR

GPCR antagonism