3E8N

X-ray structure of the human mitogen-activated protein kinase kinase 1 (MEK1) complexed with a potent inhibitor RDEA119 and MgATP

Summary for 3E8N

• Entry DOI: 10.2210/pdb3e8n/pdb
• Descriptor: Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, ADENOSINE-5'-TRIPHOSPHATE, ... (5 entities in total)
• Functional Keywords: protein kinase-ligand-mgatp complex, rdea119, rdea-119, mek1, mek1-rdea119 complex, acetylation, atp-binding, disease mutation, kinase, nucleotide-binding, phosphoprotein, serine/threonine-protein kinase, transferase, tyrosine-protein kinase
• Biological source: Homo sapiens
• Total number of polymer chains: 1
• Total formula weight: 39034.43

Authors

Yan, S.,Wang, Z.M. (deposition date: 2008-08-20, release date: 2009-09-01, Last modification date: 2023-08-30)

• Primary citation: Iverson, C.,Larson, G.,Lai, C.,Yeh, L.T.,Dadson, C.,Weingarten, P.,Appleby, T.,Vo, T.,Maderna, A.,Vernier, J.M.,Hamatake, R.,Miner, J.N.,Quart, B.; RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer.; Cancer Res., 69:6839-6847, 2009; PubMed: 19706763; DOI: 10.1158/0008-5472.CAN-09-0679

Experimental method

X-RAY DIFFRACTION (2.5 Å)