Abstract
In an effort to identify new approaches to lead discovery a polyvalent assay was developed to allow identification of weak inhibitors. This approach involves the polyvalent display of a protein binder off a Tenta-gel scaffold and the generation of a polyvalent display of protein by biotinylation followed by complexation with fluorescently labeled streptavidin. Subsequent exposure of the streptavidin complexed protein to Tenta-gel beads with active protein binders results in fluorescent beads, which are easily viewed under a fluorescent microscope.
MeSH terms
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Biotinylation
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Drug Design*
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Fluorescent Dyes / chemistry
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Ligands
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Microscopy, Fluorescence / methods
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Molecular Mimicry
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Phosphotyrosine / chemistry*
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Polystyrenes / chemistry
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Protein Binding
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Protein Tyrosine Phosphatase, Non-Receptor Type 1
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Protein Tyrosine Phosphatases / antagonists & inhibitors*
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Protein Tyrosine Phosphatases / chemistry*
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Streptavidin / chemistry
Substances
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Fluorescent Dyes
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Ligands
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Polystyrenes
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Tentagel resin
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Phosphotyrosine
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Streptavidin
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Protein Tyrosine Phosphatase, Non-Receptor Type 1
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Protein Tyrosine Phosphatases