Thiocarbamate-Linked Polysulfonate–Peptide Conjugates As Selective Hepatocyte Growth Factor Receptor Binders
| Autor: | Patricia Melnyk, Oleg Melnyk, Anthony Romieu, Hervé Drobecq, Fatima Dahmani, Rémi Desmet, Jérôme Vicogne, Véronique Fafeur, Soizic Besret |
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| Rok vydání: | 2014 |
| Předmět: |
Dendrimers
Biomedical Engineering Pharmaceutical Science Bioengineering Peptide macromolecular substances Plasma protein binding Article Receptor tyrosine kinase Substrate Specificity Structure-Activity Relationship Thiocarbamates medicine Humans Structure–activity relationship Pharmacology chemistry.chemical_classification Dose-Response Relationship Drug Molecular Structure biology Hepatocyte Growth Factor Chemistry Organic Chemistry technology industry and agriculture Proto-Oncogene Proteins c-met Protein Structure Tertiary Thiocarbamate Biochemistry Hepatocyte Growth Factor Receptor biology.protein Hepatocyte growth factor Sulfonic Acids Peptides Protein Binding Biotechnology medicine.drug |
| Zdroj: | Bioconjugate Chemistry |
| ISSN: | 1520-4812 1043-1802 |
| DOI: | 10.1021/bc500137j |
| Popis: | The capacity of many proteins to interact with natural or synthetic polyanions has been exploited for modulating their biological action. However, the polydispersity of these macromolecular polyanions as well as their poor specificity is a severe limitation to their use as drugs. An emerging trend in this field is the synthesis of homogeneous and well-defined polyanion–peptide conjugates, which act as bivalent ligands, with the peptide part bringing the selectivity of the scaffold. Alternately, this strategy can be used for improving the binding of short peptides to polyanion-binding protein targets. This work describes the design and first synthesis of homogeneous polysulfonate–peptide conjugates using thiocarbamate ligation for binding to the extracellular domain of MET tyrosine kinase receptor for hepatocyte growth factor. |
| Databáze: | OpenAIRE |
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