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Un-LOK-ing a New Approach for Conformational Selective Targeting of STK10 (LOK).

Martina Dettenhöfer1,2, Laura Nadine Tandara1,2, Jennifer Alisa Amrhein1,2

  • 1Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Strasse 9, 60438 Frankfurt am Main, Germany.

ACS Medicinal Chemistry Letters
|November 19, 2025
PubMed
Summary

Researchers optimized a macrocyclic scaffold to develop a urea-based inhibitor targeting serine/threonine kinase 10 (STK10). This new compound demonstrates potent and selective inhibition of STK10, offering a promising therapeutic strategy.

Keywords:
conformational changeinhibitor binding modekinase inhibitor selectivitymacrocyclic inhibitorrational inhibitor designserine/threonine kinase 10

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