Stabilized alpha helical peptides and uses thereof
Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death.
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Sheet 2
(2016/05/19)
DISUBSTITUTED AMINO ACIDS AND METHODS OF PREPARATION AND USE THEREOF
Provided are crystalline α, α-disubstituted amino acids and their crystalline salts containing a terminal alkene on one of their side chains, as well as optionally crystalline halogenated and deuterated analogs of the α, α-disubstituted amino acids and their salts; methods of making these, and methods of using these.
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Paragraph 0087; 0156; 0157
(2014/05/20)
Robust asymmetric synthesis of unnatural alkenyl amino acids for conformationally constrained α-helix peptides
The efficient asymmetric synthesis of unnatural alkenyl amino acids required for peptide 'stapling' has been achieved using alkylation of a fluorine-modified NiII Schiff base complex as the key step.
Aillard, Boris,Robertson, Naomi S.,Baldwin, Adam R.,Robins, Siobhan,Jamieson, Andrew G.
supporting information
p. 8775 - 8782
(2014/12/11)
An all-hydrocarbon cross-linking system for enhancing the helicity and metabolic stability of peptides [8]
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Schafmeister, Christian E.,Po, Julia,Verdine, Gregory L.
p. 5891 - 5892
(2007/10/03)
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