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January 1, 2025RSC Medicinal Chemistry

Hinge Binder Modification into Imidazopyridine for Targeting Actionable Mutations of RET Kinase

Arunkranthi Maturi Vinay Pogaku Surendra Kumar Mi‐Hyun Kim

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Key Points

Targeting RET mutations resulted in improved efficacy against several cancers, enhancing treatment options for patients.
The study highlights the role of RET as a significant oncogenic driver, with existing inhibitors presenting limited response rates.
Hinge binder modifications into imidazopyridine were assessed, aiming to overcome the limitations of current RET-targeted therapies.
While some inhibitors exist, their effectiveness remains low, indicating a need for novel approaches to target these mutations.

Implication

Research demonstrates modified imidazopyridine targets RET mutations in cancers, suggesting therapeutic potential.

Abstract

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Cite This Study

Maturi et al. (2025) studied this question.

synapsesocial.com/papers/68c1a90554b1d3bfb60e20cb https://doi.org/10.1039/d5md00397k

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Keep reading

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

1Side Chain Investigation of Imidazopyridazine as a Hinge Binder for Targeting Actionable Mutations of RET Kinase2024 · 4 citations
2Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET MutationsOriginal Research · 2024 · 20 citations
3Discovery of APS03118, a Potent and Selective Next-Generation RET Inhibitor with a Novel Kinase Hinge Scaffold2025 · 5 citations
4Developing Dynamic Structure‐Based Pharmacophore and ML‐Trained QSAR Models for the Discovery of Novel Resistance‐Free RET Tyrosine Kinase Inhibitors Through Extensive MD Trajectories and NRI Analysis2024 · 6 citations
5Computational Identification of Potential RET Inhibitors for Targeted Lung Cancer Therapy through Molecular Docking and ADMET Profiling2024

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