Abstract
siRNA has become an indispensable tool for functional characterization of genes. It has also demonstrated tremendous potential as a new generation of drug candidates. Although the technology works very well to a great panel of cells in vitro, it is still a challenge to translate the success into in vivo target validation easiness and, even more difficult, into therapeutic applications. With a number of chemically modified compounds under initial clinical trial from several commercial entities, the interests in chemical modification of siRNA have become heightened. In this review we have tried to touch on most of the chemical modifications of RNA that have been tested in the siRNA landscape, but maintained a focus on the backbone modifications, and 2-modifications on the ribose ring. It is anticipated that more modifications and more systematic comparisons between different modifications will be performed to draw more educated conclusions over some of the modifications.
Keywords: terminal modifications, RNA sugar ring, lactosylated-PEG-siRNA conjugates, oligonucleotides, Backbone modifications
Current Topics in Medicinal Chemistry
Title: RNA Interference with Chemically Modified siRNA
Volume: 6 Issue: 9
Author(s): Hong-Yan Zhang, Quan Du, Claes Wahlestedt and Zicai Liang
Affiliation:
Keywords: terminal modifications, RNA sugar ring, lactosylated-PEG-siRNA conjugates, oligonucleotides, Backbone modifications
Abstract: siRNA has become an indispensable tool for functional characterization of genes. It has also demonstrated tremendous potential as a new generation of drug candidates. Although the technology works very well to a great panel of cells in vitro, it is still a challenge to translate the success into in vivo target validation easiness and, even more difficult, into therapeutic applications. With a number of chemically modified compounds under initial clinical trial from several commercial entities, the interests in chemical modification of siRNA have become heightened. In this review we have tried to touch on most of the chemical modifications of RNA that have been tested in the siRNA landscape, but maintained a focus on the backbone modifications, and 2-modifications on the ribose ring. It is anticipated that more modifications and more systematic comparisons between different modifications will be performed to draw more educated conclusions over some of the modifications.
Export Options
About this article
Cite this article as:
Zhang Hong-Yan, Du Quan, Wahlestedt Claes and Liang Zicai, RNA Interference with Chemically Modified siRNA, Current Topics in Medicinal Chemistry 2006; 6 (9) . https://dx.doi.org/10.2174/156802606777303676
DOI https://dx.doi.org/10.2174/156802606777303676 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...read more
- 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
-
Novel Antisense Anti-MDM2 Mixed-Backbone Oligonucleotides: Proof of Principle, In Vitro and In Vivo Activities, and Mechanisms
Current Cancer Drug Targets Follow the ATP: Tumor Energy Production: A Perspective
Anti-Cancer Agents in Medicinal Chemistry Alzheimer's Disease: Emerging Trends in Small Molecule Therapies
Current Medicinal Chemistry Design, Synthesis and Biological Evaluation of Novel 1, 3- thiazolidine-2, 4-diones as Anti-prostate Cancer Agents
Anti-Cancer Agents in Medicinal Chemistry HIV-1 Infection: Recent Developments in Treatment and Current Management Strategies
Anti-Infective Agents in Medicinal Chemistry Identification of Key mRNAs, miRNAs, and mRNA-miRNA Network Involved in Papillary Thyroid Carcinoma
Current Bioinformatics Diabetic CVD – Soluble Epoxide Hydrolase as A Target
Cardiovascular & Hematological Agents in Medicinal Chemistry Two Identical Twin Nitrogen Mustard Agents that Express Rapid Alkylation Activity at Physiological pH 7.4 and 37°C
Letters in Drug Design & Discovery Commercial Opportunities and Ethical Pitfalls in Personalized Medicine: A Myriad of Reasons to Revisit the Myriad Genetics Saga
Current Pharmacogenomics and Personalized Medicine Tailored Mesoporous Silica Nanoparticles for Controlled Drug Delivery: Platform Fabrication, Targeted Delivery, and Computational Design and Analysis
Mini-Reviews in Medicinal Chemistry The Thymus During HIV Disease: Role in Pathogenesis and in Immune Recovery
Current HIV Research Utility of Molecular Imaging with 2-Deoxy-2-[Fluorine-18] Fluoro-D-Glucose Positron Emission Tomography (18F-FDG PET) for Small Cell Lung Cancer (SCLC): A Radiation Oncology Perspective
Current Radiopharmaceuticals Advances in the Treatment of Triple-negative Early Breast Cancer
Medicinal Chemistry Patent Selections
Recent Patents on Nanotechnology The Adenosine A2b Receptor: Its Role in Inflammation
Endocrine, Metabolic & Immune Disorders - Drug Targets Aberrant Immunoglobulin Variations as Indicators of Eventual Clonal Changes in Symptomatic Multiple Myeloma Patients' Course
Current Cancer Therapy Reviews Targeting RAS Signaling Pathways in Juvenile Myelomonocytic Leukemia
Current Drug Targets Outcome Measures for Clinical Trials in Interstitial Lung Diseases
Current Respiratory Medicine Reviews Actions of Selected Cardiovascular Hormones on Arterial Stiffness and Wave Reflections
Current Pharmaceutical Design Bioanalytical Applications of Au Nanoparticles
Recent Patents on Nanotechnology