Thiocarbamate-Linked Polysulfonate–Peptide
Conjugates As Selective Hepatocyte Growth Factor Receptor Binders
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Abstract
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