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 11 but no more than 20 amino acid residues having the formula I: wherein A1 is either tryptophan or d-tryptophan; wherein A2 is biphenylalanine (“Bip”); wherein A4 is an amino acid with polar side chain that can form strong hydrogen bonding or salt bridge, the hydrogen bonding or salt bridge having a bond strength from 10 to >155 kJ mol−1; wherein A5 is a small hydrophobic amino acid selected from the group consisting of isoleucine, alanine, valine, leucine and methionine; wherein A6 is an amino acid with polar side chain that can form strong hydrogen bonding, the hydrogen bonding having a bond strength from 10 to >155 kJ mol−1; 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.