Abstract
A new p38α inhibitor: Using a D-recruitment site (DRS) probe for p38α which exploits covalent interaction with Cys119 and alkyne-azide "click" chemistry to identify small molecules that recognize the p38α DRS, the anti-inflammatory natural product rooperol was identified as a novel p38α inhibitor.
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
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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Binding Sites / drug effects
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Catechols / metabolism*
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Catechols / pharmacology*
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Drug Evaluation, Preclinical
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Imidazoles / chemical synthesis
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Imidazoles / chemistry
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Imidazoles / metabolism
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Imidazoles / pharmacology
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Models, Molecular
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Phosphoproteins / antagonists & inhibitors
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Phosphoproteins / chemistry
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Phosphoproteins / metabolism
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Protein Binding
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Protein Conformation
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Protein Kinase Inhibitors / metabolism*
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Protein Kinase Inhibitors / pharmacology*
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Spectrometry, Fluorescence
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Temperature
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p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*
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p38 Mitogen-Activated Protein Kinases / chemistry
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p38 Mitogen-Activated Protein Kinases / metabolism*
Substances
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Catechols
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Imidazoles
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Phosphoproteins
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Protein Kinase Inhibitors
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rooperol
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p38 Mitogen-Activated Protein Kinases