Structural optimization of reversible dibromomaleimide peptide stapling
نویسندگان
چکیده
منابع مشابه
Double quick, double click reversible peptide "stapling".
The development of constrained peptides for inhibition of protein-protein interactions is an emerging strategy in chemical biology and drug discovery. This manuscript introduces a versatile, rapid and reversible approach to constrain peptides in a bioactive helical conformation using BID and RNase S peptides as models. Dibromomaleimide is used to constrain BID and RNase S peptide sequence varia...
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We report here a chemoselective peptide "stapling" method that can be performed on ligand-receptor complexes in situ. An appropriately structured macrocyclic bis-oxime linkage is shown to improve the affinity of a peptide ligand for its native protein receptor. The presence of the receptor as a template to preorganize the ligand into its bioactive conformation is found to bias reaction outcomes...
متن کاملPeptide stapling techniques based on different macrocyclisation chemistries.
Peptide stapling is a strategy for constraining short peptides typically in an alpha-helical conformation. Stapling is carried out by covalently linking the side-chains of two amino acids, thereby forming a peptide macrocycle. There is an expanding repertoire of stapling techniques based on different macrocyclisation chemistries. In this tutorial review, we categorise and analyse key examples o...
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ژورنال
عنوان ژورنال: Peptide Science
سال: 2020
ISSN: 2475-8817,2475-8817
DOI: 10.1002/pep2.24157