Abstract
Artificial control of gene expression has great potential in the treatment of many human diseases, and peptide nucleic acids (PNAs) offer several potential advantages for silencing gene expression in mammalian cells. The pseudopeptide backbone of the PNA makes it resistant to enzymatic degradation, and PNAs bind complementary DNA and RNA with high affinity and specificity. PNAs are potentially leading agents for antigene and antisense therapeutics, but the application of PNAs in the in vivo setting is hampered by their poor intracellular delivery. This problem has been addressed by PNA conjugation to lipophilic moieties, peptides, and cell-specific receptor ligands. The biological activity of PNAs can also benefit from conjugation to DNA interactive compounds like intercalators and alkylators. Here we review the most interesting literature concerning PNA conjugation with small molecules, emphasizing synthetic approaches, properties and applications of the PNA conjugates.
Keywords: gene expression, antisense oligonucleotides, dna mimetics, intercalators, photoreactive agents, antigene
Current Topics in Medicinal Chemistry
Title: Peptide Nucleic Acid Conjugates: Synthesis, Properties and Applications
Volume: 5 Issue: 12
Author(s): Zhanna V. Zhilina, Amy J. Ziemba and Scot W. Ebbinghaus
Affiliation:
Keywords: gene expression, antisense oligonucleotides, dna mimetics, intercalators, photoreactive agents, antigene
Abstract: Artificial control of gene expression has great potential in the treatment of many human diseases, and peptide nucleic acids (PNAs) offer several potential advantages for silencing gene expression in mammalian cells. The pseudopeptide backbone of the PNA makes it resistant to enzymatic degradation, and PNAs bind complementary DNA and RNA with high affinity and specificity. PNAs are potentially leading agents for antigene and antisense therapeutics, but the application of PNAs in the in vivo setting is hampered by their poor intracellular delivery. This problem has been addressed by PNA conjugation to lipophilic moieties, peptides, and cell-specific receptor ligands. The biological activity of PNAs can also benefit from conjugation to DNA interactive compounds like intercalators and alkylators. Here we review the most interesting literature concerning PNA conjugation with small molecules, emphasizing synthetic approaches, properties and applications of the PNA conjugates.
Export Options
About this article
Cite this article as:
Zhilina V. Zhanna, Ziemba J. Amy and Ebbinghaus W. Scot, Peptide Nucleic Acid Conjugates: Synthesis, Properties and Applications, Current Topics in Medicinal Chemistry 2005; 5 (12) . https://dx.doi.org/10.2174/156802605774370892
DOI https://dx.doi.org/10.2174/156802605774370892 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Targeting EGFR in Pancreatic Cancer Treatment
Current Drug Targets Recombinant Human p53 Adenovirus Injection (rAd-p53) Combined with Chemotherapy for 4 Cases of High-grade Serous Ovarian Cancer
Current Gene Therapy Immune Modulation by Ionizing Radiation and its Implications for Cancer Immunotherapy
Current Pharmaceutical Design Atypical PKCι as Target for Glioblastoma Therapy
Current Cancer Drug Targets Stem Cell Therapy for Alzheimers Disease
CNS & Neurological Disorders - Drug Targets Cachexia and Herbal Medicine: Perspective
Current Pharmaceutical Design PTD/CPP Peptide-Mediated Delivery of siRNAs
Current Pharmaceutical Design Real-Time PCR: Revolutionizing Detection and Expression Analysis of Genes
Current Genomics Perspectives in Nanomedicine-Based Research Towards Cancer Therapies
Current Nanoscience Role of Natural Phenolic Compounds in Cancer Chemoprevention via Regulation of the Cell Cycle
Current Pharmaceutical Biotechnology C5,C6-Disubstituted 1H-Indole-2-Carboxamides: Synthesis and Cytotoxic Activity in the Human Non-Small Lung Cancer Cell Line NSCLC-N16-L16
Letters in Drug Design & Discovery Symmetrical Derivatives of C2-Substituted Pyrrolo[2,3-f]quinolines:Synthesis, Cytotoxicity and Drug Delivery Studies
Letters in Drug Design & Discovery Antioxidant Effect of a Nitrated Cyclic Nucleotide Functioning as an Endogenous Electrophile
Current Topics in Medicinal Chemistry Autophagy and Ubiquitination as Two Major Players in Colorectal Cancer: A Review on Recent Patents
Recent Patents on Anti-Cancer Drug Discovery Human Insulin Genome Sequence Map, Biochemical Structure of Insulin for Recombinant DNA Insulin
Mini-Reviews in Medicinal Chemistry Topical Melatonin Niosome Gel for the Treatment of 5-FU-Induced Oral Mucositis in Mice
Current Drug Delivery Dissecting Virus-Plant Interactions Through Proteomics Approaches
Current Proteomics Synthesis and Antitumor Activity of Novel N-Benzoyl-N'-substituted Pyrimidinyl (Thio)semicarbazide Derivatives
Letters in Drug Design & Discovery Synthetic Lethality to Overcome Cancer Drug Resistance
Current Medicinal Chemistry Transposons for Gene Therapy!
Current Gene Therapy