Polyamide Backbone Modified Cell Targeting and Penetrating Peptides in Cancer Detection and Treatment.

Sunil S Shah,David Sabatino,Nelson Casanova,Gina Antuono

doi:10.3389/fchem.2020.00218

Abstract

Cell penetrating and targeting peptides (CPPs and CTPs) encompass an important class of biochemically active peptides owning the capabilities of targeting and translocating within selected cell types. As such, they have been widely used in the delivery of imaging and therapeutic agents for the diagnosis and treatment of various diseases, especially in cancer. Despite their potential utility, first generation CTPs and CPPs based on the native peptide sequences are limited by poor biological and pharmacological properties, thereby restricting their efficacy. Therefore, medicinal chemistry approaches have been designed and developed to construct related peptidomimetics. Of specific interest herein, are the design applications which modify the polyamide backbone of lead CTPs and CPPs. These modifications aim to improve the biochemical characteristics of the native peptide sequence in order to enhance its diagnostic and therapeutic capabilities. This review will focus on a selected set of cell penetrating and targeting peptides and their related peptidomimetics whose polyamide backbone has been modified in order to improve their applications in cancer detection and treatment.

Highlights

Cell targeting and penetrating peptides (CTPs and cell penetrating peptides (CPPs)) are a class of peptides that have the capabilities of targeting and translocating within specific cell types
CPPs and CTPs are about 4–30 amino acids in length, derived from biologically active motifs found in proteins or from selection techniques that have ushered in unique peptides with the abilities to target cell surface biological markers and translocate within cells by a variety of cell uptake mechanisms (Habault and Poyet, 2019)
In order to improve the biological properties of cell penetrating and targeting peptides (CPPs and CTPs) several biochemical strategies have been developed to design and construct related peptidomimetics

Summary

Introduction

Cell targeting and penetrating peptides (CTPs and CPPs) are a class of peptides that have the capabilities of targeting and translocating within specific cell types. These modifications have served to improve peptide metabolic stability but with limited capabilities of adopting bio-active peptide α-helical structures necessary for protein binding interactions and downstream biological signaling such as silencing gene expression in certain cancer types (Li et al, 2010, 2015).

Results

Conclusion