# Selective 7‑Azaindole Modulators Targeting Fyn and GSK-3β for Dual-Target Neuromodulation

## TL;DR

Researchers developed a new compound that targets two brain-related enzymes, Fyn and GSK-3β, to potentially treat neurodegenerative diseases.

## Contribution

A novel dual-target compound with nanomolar selectivity for Fyn and GSK-3β is proposed for neuroregenerative therapy.

## Key findings

- A lead compound was identified with nanomolar potency against Fyn and GSK-3β.
- The compound shows neuroprotective and modulatory properties in preclinical models.
- Structure–activity relationship optimization guided the development of multitarget inhibitors.

## Abstract

Fyn proto-oncogene
kinase (Fyn) and glycogen synthase kinase-3β
(GSK-3β) belong to distinct branches of the protein kinase (PK)
superfamily. Fyn is a member of the Src family of tyrosine kinases,
whereas GSK-3β is classified within the CMGC group of serine/threonine
kinases. Both play critical roles in neurodegenerative processes,
and their dysregulation has been implicated in disease progression.
The development of Fyn and GSK-3β inhibitors has attracted increasing
research attention. The design of multitarget inhibitors represents
a promising, though underexplored, therapeutic strategy. A recent
study reported a series of dual selective nanomolar inhibitors based
on structure–activity relationship (SAR) optimization. In-depth
profiling of the lead compound’s neuroprotective and modulatory
properties establishes a foundation for the development of next-generation
neuroregenerative therapeutics.