Article

Structure of a lasso peptide bound ETB receptor provides insights into the mechanism of GPCR inverse agonism

2024-01-01

Abstract excerpt

Lasso peptides exhibit a unique lariat-like knotted structure imparting exceptional stability and thus show promise as therapeutic agents that target cell-surface receptors. One such receptor is the human endothelin ET B receptor, which is implicated in challenging cancers with poor immunotherapy responsiveness. The Streptomyces -derived lasso peptide, RES-701-3, is a selective inhibitor for ET B and a compelli...

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Literature Corpus work: aa5b9d04-962d-5e61-9dac-b697e5d58803
DOI: 10.1101/2023.12.30.573741

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