Abstract
Protein chip technology provides a new and useful tool for high-throughput screening of drugs because of its high performance and low sample consumption. In order to screen elastase inhibitors on a large scale, we designed a composite microarray integrating enzyme chip containing chemical arrays on glass slides to screen for enzymatic inhibitors. The composite microarray includes an active proteinase film, screened chemical arrays distributed on the film, and substrate microarrays to demonstrate change of color. The detection principle is that elastase hydrolyzes synthetic colorless substrates and turns them into yellow products. Because yellow is difficult to detect, bromochlorophenol blue (BPB) was added into substrate solutions to facilitate the detection process. After the enzyme had catalyzed reactions for 2 h, effects of samples on enzymatic activity could be determined by detecting color change of the spots. When chemical samples inhibited enzymatic activity, substrates were blue instead of yellow products. If the enzyme retained its activity, the yellow color of the products combined with blue of BPB to make the spots green. Chromogenic differences demonstrated whether chemicals inhibited enzymatic activity or not. In this assay, 11,680 compounds were screened, and two valuable chemical hits were identified, which demonstrates that this assay is effective, sensitive and applicable for high-throughput screening (HTS).
Keywords: Chemical array, elastase, substrate, inhibitor, high-throughput screening
Combinatorial Chemistry & High Throughput Screening
Title: Application of Chemical Arrays in Screening Elastase Inhibitors
Volume: 9 Issue: 5
Author(s): Feng Gao and Guan-Hua Du
Affiliation:
Keywords: Chemical array, elastase, substrate, inhibitor, high-throughput screening
Abstract: Protein chip technology provides a new and useful tool for high-throughput screening of drugs because of its high performance and low sample consumption. In order to screen elastase inhibitors on a large scale, we designed a composite microarray integrating enzyme chip containing chemical arrays on glass slides to screen for enzymatic inhibitors. The composite microarray includes an active proteinase film, screened chemical arrays distributed on the film, and substrate microarrays to demonstrate change of color. The detection principle is that elastase hydrolyzes synthetic colorless substrates and turns them into yellow products. Because yellow is difficult to detect, bromochlorophenol blue (BPB) was added into substrate solutions to facilitate the detection process. After the enzyme had catalyzed reactions for 2 h, effects of samples on enzymatic activity could be determined by detecting color change of the spots. When chemical samples inhibited enzymatic activity, substrates were blue instead of yellow products. If the enzyme retained its activity, the yellow color of the products combined with blue of BPB to make the spots green. Chromogenic differences demonstrated whether chemicals inhibited enzymatic activity or not. In this assay, 11,680 compounds were screened, and two valuable chemical hits were identified, which demonstrates that this assay is effective, sensitive and applicable for high-throughput screening (HTS).
Export Options
About this article
Cite this article as:
Gao Feng and Du Guan-Hua, Application of Chemical Arrays in Screening Elastase Inhibitors, Combinatorial Chemistry & High Throughput Screening 2006; 9 (5) . https://dx.doi.org/10.2174/138620706777452393
DOI https://dx.doi.org/10.2174/138620706777452393 |
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
-
Nuclear Factor Kappa B: A Potential Target for Anti-HIV Chemotherapy
Current Medicinal Chemistry Synthetic Peptides in the Diagnosis of Neurological Diseases
Current Protein & Peptide Science Fc Receptor-Mediated Immune Responses: New Tools But Increased Complexity in HIV Prevention
Current HIV Research Is Autoimmunity a Component of Natural Immunity to HIV?
Current HIV Research Immunomodulation in Multiple Sclerosis by Phytotherapy
Current Immunology Reviews (Discontinued) Editorial: Rediscovering Drug Discovery
Combinatorial Chemistry & High Throughput Screening Protein Kinases as Small Molecule Inhibitor Targets in Inflammation
Current Medicinal Chemistry Signs and Related Mechanisms of Ethanol Hepatotoxicity
Current Drug Abuse Reviews Role of Prostaglandin (PG) and Peroxisome Proliferator-Activated Gamma (PPAR γ ) in Pulmonary Fibrosis
Current Respiratory Medicine Reviews Plant-food-derived Bioactives in Managing Hypertension: From Current Findings to Upcoming Effective Pharmacotherapies
Current Topics in Medicinal Chemistry Targeting Different Signaling Pathways with Antisense Oligonucleotides Combination for Cancer Therapy
Current Pharmaceutical Design Nutritional Targeting of Cyclooxygenase-2 for Colon Cancer Prevention
Inflammation & Allergy - Drug Targets (Discontinued) Perspectives in Medicinal Chemistry
Current Topics in Medicinal Chemistry Plant-Derived Leading Compounds for Eradication of Helicobacter pylori
Current Medicinal Chemistry - Anti-Infective Agents Meet our Co-Editor-in-Chief
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Neuroprotection for Ischemic Injury in the Immature Brain
Current Pediatric Reviews Mesenchymal Cells in the Treatment of Spinal Cord Injury: Current & Future Perspectives
Current Stem Cell Research & Therapy Plant-based Anti-inflammatory Agents: Progress From Africa and China
Clinical Anti-Inflammatory & Anti-Allergy Drugs (Discontinued) Multiple Hsp70 Isoforms in the Eukaryotic Cytosol: Mere Redundancy or Functional Specificity?
Current Genomics Cancer-Related Fatigue: Still an Enigma to be Solved Quickly
Reviews on Recent Clinical Trials