Abstract
We synthesized affinity-based chemical probes of cytosine-adenosine bisubstrate analogs and identified several potential targets by proteomic analysis. The validation of the proteomic analysis identified the chemical probe as a specific inhibitor of glucose-regulated protein 94 (GRP94), a potential drug target for several types of cancers. Therefore, as a result of the use of bisubstrate-type chemical probes and a chemical-biology methodology, this work opens the way to the development of a new family of GRP94 inhibitors that could potentially be of therapeutic interest.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenosine / analogs & derivatives*
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Adenosine / pharmacology*
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Adenosine / radiation effects
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Affinity Labels / chemical synthesis
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Affinity Labels / pharmacology*
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Affinity Labels / radiation effects
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Cell Line, Tumor
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Click Chemistry
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Cytosine / analogs & derivatives*
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Cytosine / pharmacology*
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Cytosine / radiation effects
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Humans
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Membrane Glycoproteins / antagonists & inhibitors*
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Membrane Glycoproteins / chemistry
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Proteome / chemistry
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Proteomics
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Ultraviolet Rays
Substances
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Affinity Labels
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Membrane Glycoproteins
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Proteome
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endoplasmin
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Cytosine
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Adenosine