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Riding toward Selectivity: Optimization of Covalent 7-Azaindole-Based BMX Kinase Inhibitors.

Xiaojun Julia Liang^1,2,3, Claudia Albertini^3,4, Thales Kronenberger^3,5,6,7

¹Department for Medicinal Chemistry, Institute for Biomedical Engineering, Faculty of Medicine, University of Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany.

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Summary

Researchers developed new BMX inhibitors targeting the TEC kinase family for immune signaling. These novel compounds show high potency and selectivity against BMX, offering improved chemical probes for research.

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Area of Science:

Biochemistry
Immunology
Medicinal Chemistry

Background:

The tyrosine kinase expressed in hepatocellular carcinoma (TEC) family, including BTK, ITK, BMX, TXK, and TEC, is crucial for immune signaling.
While BTK and ITK are well-studied, selective inhibitors for BMX, TXK, and TEC are limited.
Previous 7-azaindole-based BMX inhibitors showed potent activity but lacked selectivity, particularly against BTK.

Purpose of the Study:

To design and synthesize a new generation of BMX inhibitors with enhanced selectivity over BTK and other TEC kinases.
To identify potent and selective chemical probes for studying BMX function in immune signaling.

Main Methods:

Structure-based drug design exploiting subtle differences between BMX and BTK.
Synthesis of novel 7-azaindole derivatives with modifications at the 5-position, linker, and warhead.
Biochemical and cellular assays to evaluate inhibitory activity, selectivity, target engagement, and metabolic stability.

Main Results:

The new compounds demonstrated subnanomolar potency against BMX.
Improved selectivity was observed for BMX over BTK and other TEC kinases.
Compound 11i exhibited strong cellular target engagement, good in vitro metabolic stability, and a favorable kinome profile.
Compound 11i displayed rapid covalent inactivation kinetics.

Conclusions:

The developed BMX inhibitors represent a significant advancement in targeting the TEC kinase family.
Compound 11i is a promising chemical probe for further research into BMX biology and its role in immune signaling.
These findings provide a foundation for developing more selective inhibitors for other TEC kinases.