Work

Pharmacological Relevance of β‐, γ‐, and LINGO Auxiliary Subunits in BK Channel Modulation

Year: 2026

Type: article

Abstract: -activated potassium (BK) channels are essential regulators of physiological processes including smooth muscle tone, neurotransmitter release, and neuronal excitability. While the pore-forming α-subunit is sufficient for channel function, the remarkable diversity of BK currents in native tissues arises from its association with three structurally distinct auxiliary subunit families: β, γ, and the recently identified LINGO, each one containing four members. These auxiliary subunits significantly alter channel gating, kinetics, and pharmacological responsiveness. Moreover, their tissue-specific expression patterns, together with the distinct pharmacological sensitivities they confer, provide a promising strategy for the development of subunit-selective modulators capable of minimizing the side effects commonly associated with the widespread systemic distribution of the α-subunit. In this review, we summarize the tissue-specific distribution of auxiliary subunits and provide a systematic update on the pharmacological profile of BK channel modulation as a function of its subunit composition.

Source: ChemMedChem

DOI: 10.1002/cmdc.70398

Authors: Juliana Monat, Federico Orsi, Agustín Manzur De Nardi, Verónica Milesi, Pedro Martín

Institutions: Consejo Nacional de Investigaciones Científicas y Técnicas, Universidad Nacional de La Plata

Language: English

Topic: Ion channel regulation and function

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

Open Access status: green

Funders: Consejo Nacional de Investigaciones Científicas y Técnicas, Universidad Nacional de La Plata

Award: G3675151156