Heterobifunctional Multivalent Inhibitor-Adaptor Mediates Specific Aggregation between Shiga Toxin and a Pentraxin

The first example of a multivalent heterofunctional inhibitor-adaptor, called “BAIT”, is described. This multivalent inhibitor-adaptor is able to capture a “target” receptor (Shiga toxin) through its recognition of one ligand of a heterobivalent headgroup while the other ligand binds to an endogenou...

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Bibliographic Details
Published in:Organic letters 2005-09, Vol.7 (20), p.4369-4372
Main Authors: Solomon, Dmitry, Kitov, Pavel I, Paszkiewicz, Eugenia, Grant, Gordon A, Sadowska, Joanna M, Bundle, David R
Format: Article
Language:English
Subjects:
C-Reactive Protein - chemistry
C-Reactive Protein - metabolism
Glycosylation
Ligands
Molecular Structure
Nerve Tissue Proteins - chemistry
Nerve Tissue Proteins - metabolism
Serum Amyloid P-Component - chemistry
Serum Amyloid P-Component - metabolism
Shiga Toxin - antagonists & inhibitors
Shiga Toxin - chemistry
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Summary:The first example of a multivalent heterofunctional inhibitor-adaptor, called “BAIT”, is described. This multivalent inhibitor-adaptor is able to capture a “target” receptor (Shiga toxin) through its recognition of one ligand of a heterobivalent headgroup while the other ligand binds to an endogenous “trap” protein (serum amyloid P component, SAP). BAIT showed markedly enhanced inhibition of toxin activity. An efficient synthesis of this multivalent cluster containing heterobifunctional ligands was accomplished by chemical and chemoenzymatic approaches.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol051529+