Acid-cleavable linkers exhibiting altered rates of acid hydrolysis

摘要

An acid-cleavable peptide linker comprising aspartic acid and proline residues is disclosed. The acid-cleavable peptide linker provides an altered sensitivity to acid-hydrolytic release of peptides of interest from fusion peptides of the formula PEP1-L-PEP2. The inventive linker, L, is described in various embodiments, each of which provides substantially more rapid acid-release of peptides of interest than does a single aspartic acid-proline pair. In an additional aspect, a method of increasing the stability of an acid cleavable linkage to acid hydrolysis is also provided.

主权项

1. A fusion peptide comprising two peptides separated by an acid-cleavable linker according to the following general formula:
PEP1-L-PEP2wherein,
a) PEP1 and PEP2 are independently functional peptides wherein at least one is a peptide of interest (“POI”); and b) L is an acid-cleavable linker comprising a peptide DPPDPPDP (SEQ ID N0:7), wherein D is aspartic acid and P is proline.