Peptide stapling with the retention of double native side-chains
Sign Up to like & getrecommendations! Published in 2021 at "Chinese Chemical Letters"
DOI: 10.1016/j.cclet.2021.04.030
Abstract: ABSTRACT All-hydrocarbon stapling strategy has been widely applied for enhancing the proteolytic stability of peptides. However, two major technical hurdles to some extent limit the development of stapled peptides for therapeutic usage: rational selection of… read more here.
Keywords: native side; side chains; retention double; peptide stapling ... See more keywords
Peptide Stapling through Site-Directed Conjugation of Triazine Moieties to the Tyrosine Residues of a Peptide.
Sign Up to like & getrecommendations! Published in 2023 at "Organic letters"
DOI: 10.1021/acs.orglett.3c00499
Abstract: Peptide stapling is a strategy for improving the biological properties of peptides. Herein, we report a novel method for stapling peptides that utilizes bifunctional triazine moieties for two-component conjugation to the phenolic hydroxyl groups of… read more here.
Keywords: triazine moieties; conjugation; site directed; peptide stapling ... See more keywords
Bioinspired peptide stapling generates stable enzyme inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical communications"
DOI: 10.1039/d2cc03510c
Abstract: Stapling of peptides renders them better drug candidates. We report a new peptide staple resembling the natural metabolite lanthionine ketenamine. The strategy is orthogonal to canonical amino acids, proceeds in water and allows for tailored… read more here.
Keywords: stable enzyme; stapling generates; enzyme inhibitors; peptide stapling ... See more keywords
Peptide stapling by late-stage Suzuki–Miyaura cross-coupling
Sign Up to like & getrecommendations! Published in 2022 at "Beilstein Journal of Organic Chemistry"
DOI: 10.3762/bjoc.18.1
Abstract: The development of peptide stapling techniques to stabilise α-helical secondary structure motifs of peptides led to the design of modulators of protein–protein interactions, which had been considered undruggable for a long time. We disclose a… read more here.
Keywords: cross coupling; suzuki miyaura; stage suzuki; peptide stapling ... See more keywords