PEPTIDOMIMETIC MACROCYCLES

摘要

PROBLEM TO BE SOLVED: To provide peptidomimetic macrocycles.SOLUTION: The invention provides biologically active cross-linked polypeptides with improved properties in comparison with their corresponding precursor polypeptide, having good cell penetration properties and reduced binding to human proteins. The invention further provides methods for identifying and preparing such improved polypeptides. In one embodiment, the invention provides a method comprising the steps of: synthesizing analogs of a parent cross-linked polypeptide; performing cellular assays in the absence of human serum proteins and also in the presence of human serum in one or more concentrations so as to determine the apparent affinity of each cross-linked polypeptide to human serum proteins.SELECTED DRAWING: None