Abstract
Pradimicins (PRM) are a unique class of nonpeptidic carbohydrate-binding agents that inhibit HIV infection by efficiently binding to the HIV-1 envelope gp120 glycans in the obligatory presence of Ca2+. Surface plasmon resonance (SPR) data revealed that addition of EDTA dose-dependently results in lower binding signals of PRM-A to immobilized gp120. Pradimicin derivatives that lack the free carboxylic acid group on the C-18 position failed to bind gp120 and were devoid of significant antiviral activity. Ca2+ was much more efficient for PRM-A binding to gp120 than Cd2+, Ba2+ or Sr2+. Instead, calcium could not be replaced by any other mono- (i.e. K+), di- (i.e. Cu2+, Mg2+, Mn2+, Fe2+, Zn2+) or trivalent (i.e. Al,sup>3+, Fe3+) cation without complete loss of gp120 binding. However, Zn2+, Mg2+ and Mn2+ added to a Ca2+- pradimicin mixture, prevented pradimicin from efficient binding to gp120 glycans. These data suggest that these bivalent cations may bind to pradimicins but lead to pradimicin-cation complexes that are unable to further coordinate with the glycans of gp120. Thus, in order to afford antiviral activity, only a few cations can (i) bind to pradimicin to form a dimeric complex and (ii) subsequently coordinate the pradimicin/cation interaction with gp120 glycans
Keywords: carbohydrate-binding agent (CBA), cation complexes, glycans, HIV envelope gp120, pradimicin, surface plasmon resonance (SPR).
Current Topics in Medicinal Chemistry
Title:Role of Cations in the Interaction of Pradimicins with HIV-1 Envelope gp120
Volume: 13 Issue: 16
Author(s): Bart Hoorelbeke, Youngju Kim, Toshikazu Oki, Yasuhiro Igarashi and Jan Balzarini
Affiliation:
Keywords: carbohydrate-binding agent (CBA), cation complexes, glycans, HIV envelope gp120, pradimicin, surface plasmon resonance (SPR).
Abstract: Pradimicins (PRM) are a unique class of nonpeptidic carbohydrate-binding agents that inhibit HIV infection by efficiently binding to the HIV-1 envelope gp120 glycans in the obligatory presence of Ca2+. Surface plasmon resonance (SPR) data revealed that addition of EDTA dose-dependently results in lower binding signals of PRM-A to immobilized gp120. Pradimicin derivatives that lack the free carboxylic acid group on the C-18 position failed to bind gp120 and were devoid of significant antiviral activity. Ca2+ was much more efficient for PRM-A binding to gp120 than Cd2+, Ba2+ or Sr2+. Instead, calcium could not be replaced by any other mono- (i.e. K+), di- (i.e. Cu2+, Mg2+, Mn2+, Fe2+, Zn2+) or trivalent (i.e. Al,sup>3+, Fe3+) cation without complete loss of gp120 binding. However, Zn2+, Mg2+ and Mn2+ added to a Ca2+- pradimicin mixture, prevented pradimicin from efficient binding to gp120 glycans. These data suggest that these bivalent cations may bind to pradimicins but lead to pradimicin-cation complexes that are unable to further coordinate with the glycans of gp120. Thus, in order to afford antiviral activity, only a few cations can (i) bind to pradimicin to form a dimeric complex and (ii) subsequently coordinate the pradimicin/cation interaction with gp120 glycans
Export Options
About this article
Cite this article as:
Hoorelbeke Bart, Kim Youngju, Oki Toshikazu, Igarashi Yasuhiro and Balzarini Jan, Role of Cations in the Interaction of Pradimicins with HIV-1 Envelope gp120, Current Topics in Medicinal Chemistry 2013; 13 (16) . https://dx.doi.org/10.2174/15680266113139990124
DOI https://dx.doi.org/10.2174/15680266113139990124 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Medicinal Chemistry Advancement in Life-Threatening Diseases
The current issue will highlight concise reports that specify ground-breaking insights, including the novel discovery of drug targets and their action mechanism or drugs of novel classes. These are projected to encourage medicinal chemistry future efforts to address the most challenging medical needs. The current issue highlights further efforts to ...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
-
The Current Outbreak of COVID-19 with Reference to India
Coronaviruses The Potential Use of Cyclosporine Ultrafine Solution Pressurised Metered- Dose Inhaler in the Treatment of COVID-19 Patients
Recent Advances in Drug Delivery and Formulation Prevention, Diagnosis and Treatment of COVID-19: A Nanotechnological Perspective
Current Nanoscience Quercetin and its Relative Therapeutic Potential Against COVID-19: A Retrospective Review and Prospective Overview
Current Molecular Medicine Antisense Oligonucleotide Drug Design
Current Pharmaceutical Design Nucleoside Inhibitors of Coronaviruses
Current Medicinal Chemistry Homology Modeling of Coronavirus Structural Proteins and Molecular Docking of Potential Drug Candidates for the Treatment of COVID-19
Coronaviruses Impact of BCG Vaccine Against the Pandemic of Corona (COVID-19): A Review
Coronaviruses Nanotechnology-based Approaches for COVID-19: A Path Forward
Current Nanomaterials The Effect of Potato Almond Orange Cookies on their Weight, BMI, Hemoglobin, and Lymphocyte Status of Undernourished Older People during COVID-19 Pandemic
Current Nutrition & Food Science Machine Intelligence Techniques for the Identification and Diagnosis of COVID-19
Current Medicinal Chemistry Combination Therapy with Favipiravir for Treatment of Hospitalized COVID-19 Adults
New Emirates Medical Journal Characterization and Inhibition of SARS-Coronavirus Main Protease
Current Topics in Medicinal Chemistry Theoretical Study of the Molecular Mechanism of Maxingyigan Decoction Against COVID-19: Network Pharmacology-based Strategy
Combinatorial Chemistry & High Throughput Screening Recent Developments in Isothermal Titration Calorimetry Label Free Screening
Combinatorial Chemistry & High Throughput Screening Critical Insight into the Attributes of Emerging Novel Coronavirus (COVID-19) in India and Across the World
Coronaviruses A Viewpoint on Angiotensin-Converting Enzyme 2, Anti-Hypertensives and Coronavirus Disease 2019 (COVID-19)
Infectious Disorders - Drug Targets False Positives in the Early Stages of Drug Discovery
Current Medicinal Chemistry COVID-19 Pandemic: Current Scenario, Challenges and Future Perspectives
Coronaviruses Codon Usage Biases in Alzheimers Disease and Other Neurodegenerative Diseases
Protein & Peptide Letters