title: A fluorescence-based assay for p38α recruitment site binders: identification of rooperol as a novel p38α kinase inhibitor.
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.
authors.affiliation: Department of Cell Biology, Harvard Medical School, 240 Longwood Ave, Boston, MA 02115, USA.
authors.forename: Jing
authors.initials: J
authors.lastname: Li
authors.forename: Tamer S
authors.initials: TS
authors.lastname: Kaoud
authors.forename: Jake
authors.initials: J
authors.lastname: LeVieux
authors.forename: Brad
authors.initials: B
authors.lastname: Gilbreath
authors.forename: Swapna
authors.initials: S
authors.lastname: Moharana
authors.forename: Kevin N
authors.initials: KN
authors.lastname: Dalby
authors.forename: Sean M
authors.initials: SM
authors.lastname: Kerwin
mesh_terms: D001665:Binding Sites / Q000187:drug effects; D002396:Catechols / Q000378:metabolism* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D008958:Models, Molecular; D010750:Phosphoproteins / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism; D011485:Protein Binding; D011487:Protein Conformation; D047428:Protein Kinase Inhibitors / Q000378:metabolism* / Q000494:pharmacology*; D013050:Spectrometry, Fluorescence; D013696:Temperature; D048051:p38 Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism*
chemical_list: D002396:Catechols; D007093:Imidazoles; D010750:Phosphoproteins; D047428:Protein Kinase Inhibitors; C079659:rooperol; D048051:p38 Mitogen-Activated Protein Kinases