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Article

Functional rescue and AI analysis of a human inactivating GPCR mutation using a small molecule.

EMBO molecular medicine - 1 Feb 2026

Das Debajyoti, Wyatt Amanda, Sivaprasad Sarath, Wahl Vanessa, Qiao Sen, Ectors Fabien, Moosa Zulfiah M, Newton Claire L, Fritz Mario, Millar Robert P, Boehm Ulrich

Abstract excerpt

G protein-coupled receptors (GPCRs) carry out the majority of cellular transmembrane signaling. Many pathologies have underlying GPCR mutations, most of which cause misfolding and GPCR cell surface trafficking failure. Large libraries of existing small molecule GPCR ligands could be repurposed as pharmacological chaperones (PCs) which restore mutant GPCR folding and function, presenting an exciting alternative to...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 41507463
DOI: 10.1038/s44321-025-00369-2
PMCID: PMC12905377

Genes

PC

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 2 Sept 2026.

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