Thioether-stapled macrocyclic inhibitors of the EH domain of EHD1

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Structured Cyclic Peptides That Bind the EH Domain of EHD1

EHD1 mediates long-loop recycling of many receptors by forming signaling complexes using its EH domain. We report the design and optimization of cyclic peptides as ligands for the EH domain of EHD1. We demonstrate that the improved affinity from cyclization allows fluorescence-based screening applications for EH domain inhibitors. The cyclic peptide is also unusually well-structured in aqueous ...

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ژورنال

عنوان ژورنال: Bioorganic & Medicinal Chemistry

سال: 2018

ISSN: 0968-0896

DOI: 10.1016/j.bmc.2017.09.007