Chemogenomics with Peptide Secondary Structure Mimetics
| Autor: | Michael G. Kahn, William R. Henderson, Cu Nguyen, Emil Y. Chi, Jia Ling Teo, Masakatsu Eguchi, Michael McMillan |
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| Rok vydání: | 2003 |
| Předmět: |
Transcription
Genetic Peptide Protein Structure Secondary Receptors G-Protein-Coupled Mice chemistry.chemical_compound Peptide Library Transcription (biology) Oxidoreductase Drug Discovery Chemogenomics Animals Combinatorial Chemistry Techniques Humans Enzyme Inhibitors Receptor Protein secondary structure chemistry.chemical_classification Activator (genetics) Molecular Mimicry Organic Chemistry General Medicine Small molecule Asthma Computer Science Applications chemistry Biochemistry Peptides |
| Zdroj: | Combinatorial Chemistry & High Throughput Screening. 6:611-621 |
| ISSN: | 1386-2073 |
| Popis: | There is increasing evidence that redox regulation of transcription, particularly activator protein-1 (AP-1) and nuclear factor kappa B (NF-kappaB), 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 alpha) 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. |
| Databáze: | OpenAIRE |
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