Abstract
The development of new anti-cancer therapeutic agents is necessary to improve antitumor efficacy and reduce toxicities. Here we report using a systematic anticancer drug screening approach we developed previously, to concurrently screen colon and glioma cancer cell lines for 2000 compounds with known bioactivity and 1920 compounds with unknown activity. The hits specific to each tumor cell line were then selected, and further tested with the same cells transfected with EGFP (Enhanced Green Fluorescent Protein) alone. By comparing the percentage of signal reduction from the same cells transfected with the sensor-conjugated reporter system; hits preferably causing apoptosis were identified. Among the known lead compounds, many cardiac glycosides used as cardiotonic drugs were found to effectively and specifically kill colon cancer cells, while statins (hypolipidemic agents) used as cholesterol lowering drugs were relatively more effective in killing glioma cells.
Keywords: Drug discovery, colorectal cancer, glioma; carditonic, HTS, statins.
Combinatorial Chemistry & High Throughput Screening
Title:High Throughput Screening for Colorectal Cancer Specific Compounds
Volume: 19 Issue: 3
Author(s): Jingping Xie, Chunxia Wang and John C. Gore
Affiliation:
Keywords: Drug discovery, colorectal cancer, glioma; carditonic, HTS, statins.
Abstract: The development of new anti-cancer therapeutic agents is necessary to improve antitumor efficacy and reduce toxicities. Here we report using a systematic anticancer drug screening approach we developed previously, to concurrently screen colon and glioma cancer cell lines for 2000 compounds with known bioactivity and 1920 compounds with unknown activity. The hits specific to each tumor cell line were then selected, and further tested with the same cells transfected with EGFP (Enhanced Green Fluorescent Protein) alone. By comparing the percentage of signal reduction from the same cells transfected with the sensor-conjugated reporter system; hits preferably causing apoptosis were identified. Among the known lead compounds, many cardiac glycosides used as cardiotonic drugs were found to effectively and specifically kill colon cancer cells, while statins (hypolipidemic agents) used as cholesterol lowering drugs were relatively more effective in killing glioma cells.
Export Options
About this article
Cite this article as:
Xie Jingping, Wang Chunxia and Gore C. John, High Throughput Screening for Colorectal Cancer Specific Compounds, Combinatorial Chemistry & High Throughput Screening 2016; 19 (3) . https://dx.doi.org/10.2174/1386207319666160202120928
DOI https://dx.doi.org/10.2174/1386207319666160202120928 |
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
-
Therapeutic Potential of Peptide Toxins that Target Ion Channels
Inflammation & Allergy - Drug Targets (Discontinued) Role of Gap Junction Channel in the Development of Beat-to-Beat Action Potential Repolarization Variability and Arrhythmias
Current Pharmaceutical Design Signal Transduction Therapy for Cancer - Whither Now?
Current Signal Transduction Therapy Role of CNS Transporters in the Pharmacotherapy of HIV-1 Associated Neurological Disorders
Current Pharmaceutical Design Perspectives in Biomolecular Therapeutic Intervention in Cancer: From the Early to the New Strategies With Type I Interferons
Current Medicinal Chemistry Structure and Ligand Based Drug Design Strategies in the Development of Novel 5- LOX Inhibitors
Current Medicinal Chemistry Editorial [Hot Topic: Novel Peptide-Based Scaffolds for Drug Discovery (Executive Guest Editor: Julio A. Camarero)]
Current Pharmaceutical Design Polycation-Based Gene Therapy: Current Knowledge and New Perspectives
Current Gene Therapy Anaplastic Lymphoma Kinase as a Therapeutic Target in Anaplastic Large Cell Lymphoma, Non-Small Cell Lung Cancer and Neuroblastoma
Anti-Cancer Agents in Medicinal Chemistry Methylenetetrahydrofolate Reductase (MTHFR): A Novel Target for Cancer Therapy
Current Pharmaceutical Design Irinotecan for Treatment of Childhood Cancers: A Promising Therapeutic Partner
Current Cancer Therapy Reviews Current Status of Clinical Trials for Glioblastoma
Reviews on Recent Clinical Trials Type I Interferons: Ancient Peptides with Still Under-Discovered Anti-Cancer Properties
Protein & Peptide Letters Sp/KLF Family and Tumor Angiogenesis in Pancreatic Cancer
Current Pharmaceutical Design Expression and Function of Bcl-2 Proteins in Melanoma
Current Genomics MicroRNAs-based Therapy: A Novel and Promising Strategy for Cancer Treatment
MicroRNA Ribozymes in the Age of Molecular Therapeutics
Current Molecular Medicine An Integrative Systems Analysis of High-grade Glioma Cell Lines: TLRs, Wnt, BRCA1, Netrins, STXBP1 and MDH1 Provide Putative Molecular Targets for Therapeutic Intervention
Current Pharmacogenomics and Personalized Medicine Yeast as a Powerful Model System for the Study of Apoptosis Regulation by Protein Kinase C Isoforms
Current Pharmaceutical Design A Key Role for Connexin Hemichannels in Spreading Ischemic Brain Injury
Current Drug Targets