Probing Allosteric Kinase Modulators as Next Game-Changers in Fighting Neurodegeneration

Kinases represent one of the main targets of interest in recent years, completely revolutionizing small molecule anticancer therapy. Particularly, several medicinal chemistry strategies (e.g., covalent and allosteric inhibitors) allowed overcoming of the challenging selectivity issue, thus enabling the massive clinical translation of kinase inhibitors. However, the same success has not been detected yet for tackling neurodegenerative diseases, despite plenty of experimental evidence regarding kinases' pivotal roles in onset and development of neurodegenerative processes. In this perspective we highlight the therapeutic potential of allosteric kinase modulators in this respect, by showcasing the developmental processes and neuroprotective properties of CNS-directed allosteric kinases modulators developed so far. Moreover, we present additional kinases whose modulation is related to neuroprotection and featured by validated allosteric modulators not yet exploited in this context. This, along with a critical discussion on main drawbacks and future directions, may foster the development of allosteric kinase modulators in neurodegenerative diseases.

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Publication Details

Journal
Journal of Medicinal Chemistry
Published
2026-04-27
DOI
https://doi.org/10.1021/acs.jmedchem.5c03783
Primary Topic
Melanoma and MAPK Pathways
Type
article
Field-Weighted Citation Impact
0.00

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article

Probing Allosteric Kinase Modulators as Next Game-Changers in Fighting Neurodegeneration

Michela Rosini, Anna Minarini, Filippo Basagni, Elena Roggiolani
Journal of Medicinal Chemistry
Melanoma and MAPK Pathways
article

Probing Allosteric Kinase Modulators as Next Game-Changers in Fighting Neurodegeneration

Michela Rosini, Anna Minarini, Filippo Basagni, Elena Roggiolani
article en

Abstract

Kinases represent one of the main targets of interest in recent years, completely revolutionizing small molecule anticancer therapy. Particularly, several medicinal chemistry strategies (e.g., covalent and allosteric inhibitors) allowed overcoming of the challenging selectivity issue, thus enabling the massive clinical translation of kinase inhibitors. However, the same success has not been detected yet for tackling neurodegenerative diseases, despite plenty of experimental evidence regarding kinases' pivotal roles in onset and development of neurodegenerative processes. In this perspective we highlight the therapeutic potential of allosteric kinase modulators in this respect, by showcasing the developmental processes and neuroprotective properties of CNS-directed allosteric kinases modulators developed so far. Moreover, we present additional kinases whose modulation is related to neuroprotection and featured by validated allosteric modulators not yet exploited in this context. This, along with a critical discussion on main drawbacks and future directions, may foster the development of allosteric kinase modulators in neurodegenerative diseases.

Journal of Medicinal Chemistry
University of Bologna (IT)
Università di Bologna
Good health and well-being
Openalex Percentile: Top 7%
Melanoma and MAPK Pathways
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