Aziridine mediated native chemical ligation
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United States of America Patent
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Mar 17, 2015
Grant Date -
May 23, 2013
app pub date -
Nov 13, 2012
filing date -
Nov 18, 2011
priority date (Note) -
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Abstract
Improved methods of native chemical ligation are provided. The methods involve reacting a thioacid (e.g. a peptide thioacid) with an aziridinyl compound (e.g. an aziridinyl peptide) under mild conditions without the use of protecting groups, and without requiring that a cysteine residue be present in the ligation product. Initial coupling of the thioacid and the aziridinyl compound yields a ligation product which contains an aziridinyl ring. Subsequent opening of the aziridinyl ring (e.g. via a nucleophilic attack) produces a linearized and modified ligation product.
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