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ID: ALA5143643

Journal: Bioorg Med Chem

Title: Development of disulfide-functionalized peptides covalently binding G protein-coupled receptors.

Authors: Einsiedel J, Schmidt MF, Hübner H, Gmeiner P.

Abstract: A broadly applicable synthesis of peptides incorporating mixed disulfides between cysteine and homocysteine and cysteamine was developed. The method was established using pharmacologically relevant G protein-coupled receptor (GPCR) ligands including the μ-receptor agonist Dmt-DALDA and extended to the orexin derivative Oxa(17-33) and NT(8-13), the C-terminal hexapeptide of neurotensin. The newly developed NT(8-13) analog 6b incorporating an S-functionalized homocysteine revealed covalent binding of the neurotensin receptor 1 (NTSR1) in a radioligand depletion study.

CiteXplore: 35334449

DOI: 10.1016/j.bmc.2022.116720