Structure of a lasso peptide bound ETB receptor provides insights into the mechanism of GPCR inverse agonism
Osamu Nureki,
Wataru Shihoya,
Hiroaki Akasaka
et al.
Abstract: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 ETB receptor, which is implicated in challenging cancers with poor immunotherapy responsiveness. The Streptomyces-derived lasso peptide, RES-701-3, is a selective inhibitor for ETB and a compelling candidate for therapeutic development. However, meager production from a genetically recalcitrant hos… Show more
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