A Fluorescence-Based Assay for p38α Recruitment Site Binders: Identification of Rooperol as a Novel p38α Kinase Inhibitor

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....

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Veröffentlicht in:	Chembiochem : a European journal of chemical biology 2013-01, Vol.14 (1), p.66-71
Hauptverfasser:	Li, Jing, Kaoud, Tamer S., LeVieux, Jake, Gilbreath, Brad, Moharana, Swapna, Dalby, Kevin N., Kerwin, Sean M.
Format:	Artikel
Sprache:	eng
Schlagworte:	alkyne-azide click reaction Binding Sites - drug effects Catechols - metabolism Catechols - pharmacology cysteine D-recruitment site Drug Evaluation, Preclinical Imidazoles - chemical synthesis Imidazoles - chemistry Imidazoles - metabolism Imidazoles - pharmacology Models, Molecular non-ATP inhibitors p38 Mitogen-Activated Protein Kinases - antagonists & inhibitors p38 Mitogen-Activated Protein Kinases - chemistry p38 Mitogen-Activated Protein Kinases - metabolism p38α Phosphoproteins - antagonists & inhibitors Phosphoproteins - chemistry Phosphoproteins - metabolism polyphenols Protein Binding Protein Conformation Protein Kinase Inhibitors - metabolism Protein Kinase Inhibitors - pharmacology Spectrometry, Fluorescence Temperature
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Zusammenfassung:	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.
ISSN:	1439-4227 1439-7633
DOI:	10.1002/cbic.201200529