Dithiocarbamate-inspired side chain stapling chemistry for peptide drug design
نویسندگان
چکیده
منابع مشابه
Click Chemistry in Peptide-Based Drug Design
Click chemistry is an efficient and chemoselective synthetic method for coupling molecular fragments under mild reaction conditions. Since the advent in 2001 of methods to improve stereochemical conservation, the click chemistry approach has been broadly used to construct diverse chemotypes in both chemical and biological fields. In this review, we discuss the application of click chemistry in ...
متن کاملSide chain chemistry mediates backbone fragmentation in hydrogen deficient peptide radicals.
A crown ether based, photolabile radical precursor which forms noncovalent complexes with peptides has been prepared. The peptide/precursor complexes can be electrosprayed, isolated in an ion trap, and then subjected to laser photolysis and collision induced dissociation to generate hydrogen deficient peptide radicals. It is demonstrated that these peptide radicals behave very differently from ...
متن کاملMonosubstituted alkenyl amino acids for peptide "stapling".
Alkenylglycine amino acids were assessed as potential candidates for hydrocarbon stapling and shown to be effective in stapling of the BID BH3 peptide.
متن کاملPeptide ligation via side-chain auxiliary.
A new peptide ligation strategy based on a side-chain auxiliary was developed; the auxiliary is fairly simple and can be removed, without product isolation, under basic conditions.
متن کاملA Perfluoroaryl-Cysteine S[subscript N]Ar Chemistry Approach to Unprotected Peptide Stapling
We report the discovery of a facile transformation between perfluoroaromatic molecules and a cysteine thiolate, which is arylated at room temperature. This new approach enabled us to selectively modify cysteine residues in unprotected peptides, providing access to variants containing rigid perfluoroaromatic staples. This stapling modification performed on a peptide sequence designed to bind the...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Chemical Science
سال: 2019
ISSN: 2041-6520,2041-6539
DOI: 10.1039/c8sc03275k