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Article

Resistance to Allosteric Inhibitors.

Journal of molecular biology - 15 Oct 2025

Outhwaite Ian R, Kwan Isabelle, Leyte-Vidal Ariel, Shah Neil P, Bahar Ivet, Seeliger Markus A

Abstract excerpt

Allosteric inhibitors have emerged as powerful therapeutic agents capable of overcoming resistance mutations that impair the efficacy of orthosteric inhibitors. However, resistance to allosteric inhibitors can also arise, posing a challenge to their long-term effectiveness. Mechanisms of resistance include altered inhibitor affinity and kinetics, disruption of the allosteric mechanism, changes in receptor...

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Identifiers

PMID: 40216016
DOI: 10.1016/j.jmb.2025.169133
PMCID: PMC12926998

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