title: Development of a p38δ mitogen activated protein kinase ELISA assay for the quantitative determination of inhibitor activity.
abstract: The p38 mitogen activated protein kinase (MAPK) has emerged as a target for treating inflammatory diseases, like rheumatoid arthritis (RA). Expression of p38δ is induced in rheumatoid arthritis synovial fibroblasts (RASFs) by a cytokine-independent pathway substantially different from other MAPK pathways. To identify inhibitors of p38δ MAPK, we developed a direct ELISA assay based on a previously described p38α assay for monitoring the phosphorylation of ATF-2. This work presents a straightforward assay for evaluating the potency of small-molecule inhibitors. To validate the assay under optimized conditions, we used reference compounds and achieved results comparable to published data.
authors.affiliation: Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Eberhard Karls University of Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany.
authors.forename: Márcia
authors.initials: M
authors.lastname: Goettert
authors.forename: Nouran
authors.initials: N
authors.lastname: Shaalan
authors.forename: Ralph
authors.initials: R
authors.lastname: Graeser
authors.forename: Stefan A
authors.initials: SA
authors.lastname: Laufer
mesh_terms: D051698:Activating Transcription Factor 2 / Q000378:metabolism; D001172:Arthritis, Rheumatoid / Q000188:drug therapy / Q000503:physiopathology; D004797:Enzyme-Linked Immunosorbent Assay / Q000379:methods*; D005347:Fibroblasts / Q000378:metabolism; D048292:Mitogen-Activated Protein Kinase 13 / Q000037:antagonists & inhibitors*; D010766:Phosphorylation; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*
chemical_list: D051698:Activating Transcription Factor 2; D047428:Protein Kinase Inhibitors; D048292:Mitogen-Activated Protein Kinase 13