Selective 7-Azaindole Modulators Targeting Fyn and GSK-3β for Dual-Target Neuromodulation
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.
Authors
- Steven H. Liang (ORCID: https://orcid.org/0000-0003-1413-6315)
- Haofeng Shi (ORCID: https://orcid.org/0000-0002-9187-0751)
- Yinlong Li
Institutions
- Georgia Institute of Technology (US)
- Emory University (US)
- The Wallace H. Coulter Department of Biomedical Engineering (US)
Publication Details
- Journal
- ACS Medicinal Chemistry Letters
- Published
- 2025-12-24
- DOI
- https://doi.org/10.1021/acsmedchemlett.5c00728
- Primary Topic
- Wnt/β-catenin signaling in development and cancer
- Type
- article
- Field-Weighted Citation Impact
- 0.00