Abstract
A trimodular activity-based probe was designed, synthesized, characterized, and applied to photoaffinity label the GABA(B) receptors transiently expressed in Chinese hamster ovary (CHO) cells. The probe exhibits specific binding activity at the ligand-binding pocket of GB1 subunits and high specificity of photoaffinity labeling, which makes the probe valuable for studying the localization and function of GABA(B) receptors on living cells.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Benzoates / chemical synthesis*
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Benzoates / metabolism
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Boron Compounds / chemical synthesis*
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Boron Compounds / metabolism
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Cell Line
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Cricetinae
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Cricetulus
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Diazomethane / analogs & derivatives*
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Diazomethane / chemical synthesis*
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Diazomethane / metabolism
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Drug Design
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Humans
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Organophosphorus Compounds / chemical synthesis
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Organophosphorus Compounds / metabolism
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Photoaffinity Labels / chemical synthesis*
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Photoaffinity Labels / metabolism
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Protein Subunits / metabolism
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Receptors, GABA-B / metabolism*
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Structure-Activity Relationship
Substances
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4,4-difluoro-4-bora-3a,4a-diaza-s-indacene
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Benzoates
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Boron Compounds
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Organophosphorus Compounds
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Photoaffinity Labels
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Protein Subunits
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Receptors, GABA-B
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Diazomethane