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Mechanistic insights into DCPIB inhibition of VRAC: Electrostatic control and binding plasticity.

The Journal of general physiology - 7 Sept 2026

Gaitán-Peñas Héctor, Llabrés Salomé, Pedrola Marina, González-Subías Marc, Juárez-Jiménez Jordi, Pusch Michael, Lavilla Rodolfo, Estévez Raúl

Abstract excerpt

The volume-regulated anion channel (VRAC), formed by LRRC8 heteromers, regulates cell volume and is a promising therapeutic target. DCPIB is the most widely used VRAC inhibitor, yet its binding mechanism remains poorly defined. Although structural studies suggested a role of residue R103 in LRRC8A in DCPIB binding, its functional relevance has been unclear. Here, we combined electrophysiology in Xenopus oocytes...

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PMID: 42348849
DOI: 10.1085/jgp.202513953

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