Peptide Nucleic Acids (PNA) in Chemical Biology and Drug Discovery

Abstract

Introduction. -Since the introduction almost 20 years ago [1], peptide nucleic acids (PNAs) have caught the interest in many fields of science from pure chemistry, over (molecular) biology, drug discovery, and (genetic) diagnostics, to nanotechnology and prebiotic chemistry. Thus, a very wide variety of PNA derivatives and PNA-type molecules have been synthesized and characterized in terms of chemical properties and in terms of possible exploitation within nucleic acid recognition applications. Despite this wealth of novel structures, most applications are still centered around the original aminoethylglycine (aeg) PNA. This review will focus on the general properties of PNA, the main applications as they appear today, and with emphasis on the most recent developments.

Genomic targeting of epigenetic probes using a chemically tailored Cas9 system

“…This opens the door for subnuclear targeting of epigenetic probes, including small molecules and modified proteinaceous material (17,18). Examples of synthetic targeting agents include pyrrole-imidazole polyamides and peptide nucleic acids (19,20). Despite the elegance of these strategies, however, their widespread application has been limited by the need for specialized chemical synthesis methods and by constraints associated with their genomic targeting (i.e., locus specificity) (19,21).…”

Peptide Conjugated Phosphorodiamidate Morpholino Oligomers Increase Survival of Mice Challenged with AmesBacillus anthracis

“…Gene-silencing oligomers decrease expression of reporter genes such as luciferase, activate endogenous genes such as b-galactosidase, and inhibit growth by targeting essential genes . Some of the attractive targets for antisense antibacterial therapy include essential genes such as acyl carrier protein (acpP) encoding the fatty acid biosynthesis protein Greenberg et al, 2010), bacterial RNA polymerases (Bai et al, 2011), fabIencoding enoyl-acyl carrier protein reductase and 16S rRNA (Nielsen, 2010). Prior studies have shown that PMO targeting the acpP gene was able to inhibit E. coli viability in vitro and in vivo in mice .…”

A convenient and highly efficient synthesis of one kind of peptide nucleic acid monomer

“…Over the past two decades, a growing number of PNA derivatives have been synthesized and successfully applied in molecular biology, diagnostics and therapeutics [4][5][6][7]. Recently, a novel non-classical PNA monomer, S-thyminyl-L-cysteine hydrochloride (compound 2), which consists of natural chiral cysteine and 5-hydroxymethyluracil [8], was reported by Yu and his co-workers [9,10].…”