Abstract
Antimicrobial peptides (AMPs) are ubiquitous in nature where they play important roles in host defense and microbial control. Despite their natural origin, antimicrobial spectrum and potency, the lead peptide candidates that so far have entered pharmaceutical development have all been further optimized by rational or semi-rational approaches. In recent years, several high throughput screening (HTS) systems have been developed to specifically address optimization of AMPs. These include a range of computational in silico systems and cell-based in vivo systems. The in silico-based screening systems comprise several computational methods such as Quantitative Structure / Activity Relationships (QSAR) as well as simulation methods mimicking peptide / membrane interactions. The in vivo-based systems can be divided in cis-acting and trans-acting screening systems. The cisacting pre-screens, where the AMP exerts its antimicrobial effect on the producing cell, allow screening of millions or even billions of lead candidates for their basic antimicrobial or membrane-perturbating activity. The transacting screens, where the AMP is secreted or actively liberated from the producing cell and interacts with cells different from the producing cell, allow for screening under more complex and application-relevant conditions. This review describes the application of HTS systems employed for AMPs and lists advantages as well as limitations of these systems.
Keywords: antimicrobial peptide (amp), high throughput screening (hts), suicide expression system (ses), trans-acting peptide system (taps), novispirin, plectasin, quantitative structure-activity relationship (qsar)
Combinatorial Chemistry & High Throughput Screening
Title: Improving on Natures Defenses: Optimization & High Throughput Screening of Antimicrobial Peptides
Volume: 8 Issue: 3
Author(s): D. Raventos, O. Taboureau, P. H. Mygind, J. D. Nielsen, C. P. Sonksen and H.- H. Kristensen
Affiliation:
Keywords: antimicrobial peptide (amp), high throughput screening (hts), suicide expression system (ses), trans-acting peptide system (taps), novispirin, plectasin, quantitative structure-activity relationship (qsar)
Abstract: Antimicrobial peptides (AMPs) are ubiquitous in nature where they play important roles in host defense and microbial control. Despite their natural origin, antimicrobial spectrum and potency, the lead peptide candidates that so far have entered pharmaceutical development have all been further optimized by rational or semi-rational approaches. In recent years, several high throughput screening (HTS) systems have been developed to specifically address optimization of AMPs. These include a range of computational in silico systems and cell-based in vivo systems. The in silico-based screening systems comprise several computational methods such as Quantitative Structure / Activity Relationships (QSAR) as well as simulation methods mimicking peptide / membrane interactions. The in vivo-based systems can be divided in cis-acting and trans-acting screening systems. The cisacting pre-screens, where the AMP exerts its antimicrobial effect on the producing cell, allow screening of millions or even billions of lead candidates for their basic antimicrobial or membrane-perturbating activity. The transacting screens, where the AMP is secreted or actively liberated from the producing cell and interacts with cells different from the producing cell, allow for screening under more complex and application-relevant conditions. This review describes the application of HTS systems employed for AMPs and lists advantages as well as limitations of these systems.
Export Options
About this article
Cite this article as:
Raventos D., Taboureau O., Mygind H. P., Nielsen D. J., Sonksen P. C. and Kristensen H. H.-, Improving on Natures Defenses: Optimization & High Throughput Screening of Antimicrobial Peptides, Combinatorial Chemistry & High Throughput Screening 2005; 8 (3) . https://dx.doi.org/10.2174/1386207053764549
DOI https://dx.doi.org/10.2174/1386207053764549 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
Call for Papers in Thematic Issues
Artificial Intelligence Methods for Biomedical, Biochemical and Bioinformatics Problems
Recently, a large number of technologies based on artificial intelligence have been developed and applied to solve a diverse range of problems in the areas of biomedical, biochemical and bioinformatics problems. By utilizing powerful computing resources and massive amounts of data, methods based on artificial intelligence can significantly improve the ...read more
Eco-friendly Agents for Biological Control of Pathogenic Diseases
The discovery of an alternative biological approach to disease management includes work on medicinal products derived from natural sources as a starting point for the development of eco-friendly agents for these diseases and the injuries they cause, as well as reducing human contact with hazardous chemicals and their residues. We ...read more
Emerging trends in diseases mechanisms, noble drug targets and therapeutic strategies: focus on immunological and inflammatory disorders
Recently infectious and inflammatory diseases have been a key concern worldwide due to tremendous morbidity and mortality world Wide. Recent, nCOVID-9 pandemic is a good example for the emerging infectious disease outbreak. The world is facing many emerging and re-emerging diseases out breaks at present however, there is huge lack ...read more
Exploring Spectral Graph Theory in Combinatorial Chemistry
Scope of the Thematic Issue: Combinatorial chemistry involves the synthesis and analysis of a large number of diverse compounds simultaneously. Traditional methods rely on brute force experimentation, which can be time-consuming and resource-intensive. Spectral Graph Theory, a branch of mathematics dealing with the properties of graphs in relation to the ...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
Related Articles
-
Developments of Combretastatin A-4 Derivatives as Anticancer Agents
Current Medicinal Chemistry Modulation of P-Glycoprotein (PGP) Mediated Multidrug Resistance (MDR) Using Chemosensitizers: Recent Advances in the Design of Selective MDR Modulators
Current Medicinal Chemistry - Anti-Cancer Agents Calculating Water Thermodynamics in the Binding Site of Proteins – Applications of WaterMap to Drug Discovery
Current Topics in Medicinal Chemistry Preface
Current Stem Cell Research & Therapy Novel Rule-Based Method for Multi-Parametric Multi-Objective Decision Support in Lead Optimization Using KEM
Current Computer-Aided Drug Design Inflammasomes as Potential Therapeutic Targets in Atherosclerotic Cardiovascular Disease
Endocrine, Metabolic & Immune Disorders - Drug Targets COVID-19: The Unprecedented Malady- A Holistic Review
Coronaviruses A Study About the Impact of Weather, Life Expectancy and Tourism on the Transmission of COVID-19
Coronaviruses Clinical Outcomes of Zinc Supplementation Among COVID-19 Patients
Current Drug Safety Tinocordiside from <i>Tinospora cordifolia</i> (Giloy) May Curb SARS-CoV-2 Contagion by Disrupting the Electrostatic Interactions between Host ACE2 and Viral S-Protein Receptor Binding Domain
Combinatorial Chemistry & High Throughput Screening A Comparative Adsorption Study on Low-cost Synthetic, Nano and Doped ZnO for the Removal of Copper Surfactants Urea Complexes: Equilibrium, Kinetics, and Thermodynamics
Nanoscience & Nanotechnology-Asia MicroRNA Polymorphisms, MicroRNA Pharmacogenomics and Cancer Susceptibility
Current Pharmacogenomics and Personalized Medicine Recent Advances of Natural and Synthetic β-Carbolines as Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry CT Diagnosis of Coronavirus Infection
Current Medical Imaging The Two Faces of Iminoalditols: Powerful Inhibitors Trigger Glycosidase Activation
Current Enzyme Inhibition Current Trends and Future Directions of Fluoroquinolones
Current Medicinal Chemistry <i>In-silico</i> Discovery of Fungal Metabolites Bergenin, Quercitrin and Dihydroartemisinin as Potential Inhibitors against Main Protease of SARSCoV- 2
Coronaviruses Recent Advances of Diaryl Ether Family as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors
Current Pharmaceutical Design Design, Synthesis and Biological Evaluation of Novel Heterocyclic Fluoroquinolone Citrate Conjugates as Potential Inhibitors of Topoisomerase IV: A Computational Molecular Modeling Study
Current Drug Discovery Technologies Metabolic Syndrome, Alzheimer’s Disease, and Covid 19: A Possible Correlation
Current Alzheimer Research