Abstract
The objective of this study was to design and synthesize a new CPP-PNA conjugate that would be able to penetrate endothelial cells, bind STAT1 mRNA and thereby block the activity of STAT1 (the Signal Transducer and Activator of Transcription 1), which is important in cases of vessel inflammation. In the course of the study, the TAMRA-PTD-4- Hal(traziole-Gly-PNA)-conjugate was successfully synthesized using a specific 1,3-dipolar Huisgen cycloaddition reaction known as a “click reaction”. The hybridization properties of the conjugate to complementary hSTAT1 mRNA and hSTAT1 ssDNA fragments was verified by capillary electrophoresis (CE). Studies have shown that the attachment of a fluorescence-labeled peptide to a PNA sequence via a 1,2,3-triazole ring did not alter the binding properties of the PNA to the complementary hSTAT1 mRNA or hSTAT1 ssDNA fragments maintaining similar binding affinity. Furthermore, the data obtained suggest that the use of such a conjugate to modulate the activity and expression of STAT1 could provide a new therapeutic strategy for atherosclerosis treatment.
Keywords: Capillary electrophoresis, cell penetrating peptides, click reaction, CPP-PNA conjugate, peptide nucleic acids.
Protein & Peptide Letters
Title:Synthesis and Hybridization Studies of a New CPP-PNA Conjugate as a Potential Therapeutic Agent in Atherosclerosis Treatment
Volume: 21 Issue: 7
Author(s): Monika Wojciechowska, Jaroslaw Ruczynski, Piotr Rekowski, Magdalena Alenowicz, Piotr Mucha, Malgorzata Pieszko, Anna Miszka, Michal Dobkowski and Hans Bluijssen
Affiliation:
Keywords: Capillary electrophoresis, cell penetrating peptides, click reaction, CPP-PNA conjugate, peptide nucleic acids.
Abstract: The objective of this study was to design and synthesize a new CPP-PNA conjugate that would be able to penetrate endothelial cells, bind STAT1 mRNA and thereby block the activity of STAT1 (the Signal Transducer and Activator of Transcription 1), which is important in cases of vessel inflammation. In the course of the study, the TAMRA-PTD-4- Hal(traziole-Gly-PNA)-conjugate was successfully synthesized using a specific 1,3-dipolar Huisgen cycloaddition reaction known as a “click reaction”. The hybridization properties of the conjugate to complementary hSTAT1 mRNA and hSTAT1 ssDNA fragments was verified by capillary electrophoresis (CE). Studies have shown that the attachment of a fluorescence-labeled peptide to a PNA sequence via a 1,2,3-triazole ring did not alter the binding properties of the PNA to the complementary hSTAT1 mRNA or hSTAT1 ssDNA fragments maintaining similar binding affinity. Furthermore, the data obtained suggest that the use of such a conjugate to modulate the activity and expression of STAT1 could provide a new therapeutic strategy for atherosclerosis treatment.
Export Options
About this article
Cite this article as:
Wojciechowska Monika, Ruczynski Jaroslaw, Rekowski Piotr, Alenowicz Magdalena, Mucha Piotr, Pieszko Malgorzata, Miszka Anna, Dobkowski Michal and Bluijssen Hans, Synthesis and Hybridization Studies of a New CPP-PNA Conjugate as a Potential Therapeutic Agent in Atherosclerosis Treatment, Protein & Peptide Letters 2014; 21 (7) . https://dx.doi.org/10.2174/0929866521666140320102034
DOI https://dx.doi.org/10.2174/0929866521666140320102034 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
- 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
Related Articles
-
Current Advances in Antibody Immobilization on Different Surfaces and Beads
Current Proteomics Bioluminescence Imaging in Rodents: When Light Illuminates Cancer Research
Current Molecular Imaging (Discontinued) Liposome Circulation Time is Prolonged by CD47 Coating
Protein & Peptide Letters Role of Phytochelators in Land Reclamation: Recent Progress and Perspectives
Current Environmental Engineering An Update to the Combined Vibrational- Diffraction Experimental and Theoretical Studies of Small Biologically Important Cyclic Imides:Reference to Saccharin
Current Organic Chemistry Preparation of Quercetin Loaded Microparticles and their Antitumor Activity against Human Lung Cancer Cells (A549) in vitro
Current Pharmaceutical Biotechnology Fatty Acid-Mediated Inhibition of Metal Binding to the Multi-Metal Site on Serum Albumin: Implications for Cardiovascular Disease
Current Topics in Medicinal Chemistry Safety of Nanoparticles in Medicine
Current Drug Targets High-Throughput Screening by Nuclear Magnetic Resonance (HTS by NMR) for the Identification of PPIs Antagonists
Current Topics in Medicinal Chemistry Biomedical Application of Polymers: A Case Study of Non-CNS Drugs Becoming CNS Acting Drugs
Central Nervous System Agents in Medicinal Chemistry NbCl5 as an Expeditious Catalyst for the Synthesis of Quinoxalinyl and Dibenzodioxepinyl Phosphonates/Phosphinates via Michaelis-Arbuzov Reaction and their Biological Evaluation
Letters in Organic Chemistry Review of Recent Clinical Developments and Patents for the Treatment of Autoimmune and Inflammatory Diseases by Mesenchymal Stromal Cells
Recent Patents on Regenerative Medicine Impact of Buprenorphine on Learning and Memory Ability, Oxidative Status and Inflammation in the Hippocampus of Rats
Current Molecular Pharmacology Biological Role of Formaldehyde, and Cycles Related to Methylation, Demethylation, and Formaldehyde Production
Mini-Reviews in Medicinal Chemistry Inhibitors of the Immunoproteasome: Current Status and Future Directions
Current Pharmaceutical Design Pros and Cons of Medical Cannabis use by People with Chronic Brain Disorders
Current Neuropharmacology Current and Potential Use of Citrus Essential Oils
Current Organic Chemistry The Role of Folate-supplementation in Depression: A Narrative Review
Current Psychopharmacology Stem Cells: In Sickness and in Health
Current Stem Cell Research & Therapy Recent Applications of Nanomaterials Based on Electrochemical Drug Analysis
Current Analytical Chemistry