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February 12, 2026Science AdvancesOpen Access

The allosteric landscape of the Src kinase

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Authors

TBToni BeltranMNMohsin M. NaqviAFAndre J. Faure

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Overview

Experimental mapping identifies druggable allosteric sites in Src kinase, suggesting new therapeutic targets.

Key Points

  • The research aims to create an extensive map of allosteric sites in the Src protein kinase, enhancing drug specificity and efficacy.
  • Conducted experiments with over 50,000 amino acid substitutions in Src kinase.
  • Quantified changes in activity and stability due to these substitutions.
  • Used thermodynamic modeling to analyze changes in fold stability and catalysis.
  • Identified multiple druggable allosteric sites in Src kinase not previously reported.
  • Demonstrated that inhibitory allosteric mutations decay in effect with distance from the active site.
  • Revealed extensive allostery in the kinase domain influenced by regulatory domains.

Cite This Study

Beltran et al. (2026) studied this question.

synapsesocial.com/papers/698d6eca5be6419ac0d54a93https://doi.org/10.1126/sciadv.aea2726
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