Thiocarbamate-Linked Polysulfonate鈥揚eptide Conjugates As Selective Hepatocyte Growth Factor Receptor Binders

详细信息    查看全文

• 作者：Soizic Besret ; J茅r么me Vicogne ; Fatima Dahmani ; V茅ronique Fafeur ; R茅mi Desmet ; Herv茅 Drobecq ; Anthony Romieu ; Patricia Melnyk ; Oleg Melnyk
• 刊名：Bioconjugate Chemistry
• 出版年：2014
• 出版时间：May 21, 2014
• 年：2014
• 卷：25
• 期：5
• 页码：1000-1010
• 全文大小：576K
• 年卷期：v.25,no.5(May 21, 2014)
• ISSN：1520-4812

文摘

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鈥損eptide 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鈥損eptide conjugates using thiocarbamate ligation for binding to the extracellular domain of MET tyrosine kinase receptor for hepatocyte growth factor.