Abstract
There is increasing evidence that redox regulation of transcription, particularly activator protein-1 (AP-1) and nuclear factor kappa B (NF-kB), is important in inflammatory diseases. Human thioredoxin (TRX), a member of the oxidoreductase superfamily, was initially identified, as a factor which augments the production of interleukin-2 receptor alpha (IL-2R α) in human T-cell lymphotropic virus type 1 (HTLV-1) infected patient T-cells. Substrates for the redox activity of TRX bind the active site cleft in extended strand structure. The rapid generation of high numbers of peptide secondary structure mimetics through solid-phase synthesis is a key technology for the identification of pharmaceutical leads based on such protein-peptide interactions. In this manuscript, we describe a chemogenomic approach utilizing an extended strand templated library to develop small molecule inhibitors to validate oxidoreductase molecular targets in a murine asthma model.
Keywords: chemogenomics, peptide secondary, structure mimetics, activator protein-1, nuclear factor kappa b, human thioredoxin
Combinatorial Chemistry & High Throughput Screening
Title: Chemogenomics with Peptide Secondary Structure Mimetics
Volume: 6 Issue: 7
Author(s): Masakatsu Eguchi, Michael McMillan, Cu Nguyen, Jia-Ling Teo, Emil Y. Chi, William R. Henderson Jr. and Michael Kahn
Affiliation:
Keywords: chemogenomics, peptide secondary, structure mimetics, activator protein-1, nuclear factor kappa b, human thioredoxin
Abstract: There is increasing evidence that redox regulation of transcription, particularly activator protein-1 (AP-1) and nuclear factor kappa B (NF-kB), is important in inflammatory diseases. Human thioredoxin (TRX), a member of the oxidoreductase superfamily, was initially identified, as a factor which augments the production of interleukin-2 receptor alpha (IL-2R α) in human T-cell lymphotropic virus type 1 (HTLV-1) infected patient T-cells. Substrates for the redox activity of TRX bind the active site cleft in extended strand structure. The rapid generation of high numbers of peptide secondary structure mimetics through solid-phase synthesis is a key technology for the identification of pharmaceutical leads based on such protein-peptide interactions. In this manuscript, we describe a chemogenomic approach utilizing an extended strand templated library to develop small molecule inhibitors to validate oxidoreductase molecular targets in a murine asthma model.
Export Options
About this article
Cite this article as:
Eguchi Masakatsu, McMillan Michael, Nguyen Cu, Teo Jia-Ling, Chi Y. Emil, Henderson Jr. R. William and Kahn Michael, Chemogenomics with Peptide Secondary Structure Mimetics, Combinatorial Chemistry & High Throughput Screening 2003; 6 (7) . https://dx.doi.org/10.2174/138620703771981197
DOI https://dx.doi.org/10.2174/138620703771981197 |
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
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
Integrating Network Pharmacology and Traditional Medicine: A New Perspective in Drug Mechanism Research
Network pharmacology is a network construction and network topology analysis strategy that combines pharmacology and pharmacodynamics. In recent years, network pharmacology has emerged as a powerful tool that can be integrated with pharmacology. Natural products commonly function in multicomponent, multitarget, and multipathway systems. Some examples encompass Ayurveda, traditional Chinese medicines ...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
-
Cachexia and Herbal Medicine: Perspective
Current Pharmaceutical Design Physiological Roles for K posative Channels and Gap Junctions in Urogenital Smooth Muscle Implications for Improved Understanding of Urogenital Function, Disease and Therapy
Current Drug Targets Passive Smoking, Asthma and Allergy in Children
Inflammation & Allergy - Drug Targets (Discontinued) Emerging Anti-inflammatory Therapies for Atherosclerosis
Current Pharmaceutical Design Benzimidazole Derivatives as Kinase Inhibitors
Current Medicinal Chemistry Metabolic Syndrome the Gynecologist’s Approach
Current Women`s Health Reviews Silicosis in Current Scenario: A Review of Literature
Current Respiratory Medicine Reviews Development and Clinical use of Prasugrel and Ticagrelor
Current Pharmaceutical Design Vitamin D and the Adaptive Immune System with Special Emphasis to Allergic Reactions and Allograft Rejection
Inflammation & Allergy - Drug Targets (Discontinued) In Silico Studies on DARC
Infectious Disorders - Drug Targets How Internet Technology Can Improve the Quality of Care for Substance Use Disorders
Current Drug Abuse Reviews Altering the Sphingosine-1-Phosphate/Ceramide Balance: A Promising Approach for Tumor Therapy
Current Pharmaceutical Design Role of Nitric Oxide in the Modulation of Angiogenesis
Current Pharmaceutical Design Towards a Personalised Approach to Managing Influenza Infections in Infants and Children – Food for Thought and a Note on Oseltamivir
Infectious Disorders - Drug Targets Beta-2 Agonists in Asthma: Medicine or Murderer?
Current Respiratory Medicine Reviews Poly-Pharmacy Among the Elderly: Analyzing the Co-Morbidity of Hypertension and Diabetes
Current Pharmaceutical Design Potential Therapeutic Targets for Steroid-Resistant Asthma
Current Drug Targets Editorial (Thematic Issue: Advances in Drug Discovery for the Treatment of Cancer: Many Approaches, One Goal)
Current Topics in Medicinal Chemistry Cow’s Milk Allergenicity
Endocrine, Metabolic & Immune Disorders - Drug Targets Clinical Characteristics and CT Imaging Features of COVID-19 on Admission: A Retrospective Study
Current Medical Imaging