CYCLIC LACTADHERIN PEPTIDE MIMETICS AND THEIR USES

摘要

Provided herein is a new class of cyclic lactadherin peptides (cLac) that mimic the natural phosphatidylserine (PS)-binding activity of the parent lactadherin protein. These cLacs are useful as small molecule indicators of early stage of apoptosis and of treatment efficacy evaluation.

主权项

1. A cyclic peptide comprising at least 10 but no more than 20 amino acid residues having the formula I: wherein A1 and A2 are hydrophobic amino acid residues that are appropriate for lipid membrane binding, wherein the side chains of these hydrophobic amino acid have an added cLogP value of between 5 and 9, and wherein the hydrophobic amino acid residues are in the D or L configuration, are natural or unnatural, and hydrophobic amino acid are substituted or unsubstituted; wherein A4 is an amino acid with polar side chain that can form strong hydrogen bonding or salt bridge; wherein A5 is a small hydrophobic amino acid; wherein A6 is an amino acid with polar side chain that can form strong hydrogen bonding; wherein A3, A7 and A9 are neutral amino acid residues, wherein n=1-3, x=1-5 and y=2-6, and when there are multiples of A3, A7 and A9, they can be the same amino acid residues or different amino acid residues; wherein A8 is a positively charged amino acid; and wherein A10 is an amino acid with a negatively charged side chain.