7XLP

MEK1 bound to DS03090629

Summary for 7XLP

• Entry DOI: 10.2210/pdb7xlp/pdb
• Descriptor: Dual specificity mitogen-activated protein kinase kinase 1, (1~{R},3~{S})-3-[[6-[2-chloranyl-4-(4-methylpyrimidin-2-yl)oxy-phenyl]-3-methyl-1~{H}-indazol-4-yl]oxy]cyclohexan-1-amine, DIMETHYL SULFOXIDE, ... (5 entities in total)
• Functional Keywords: kinase, inhibitor, complex, atp competitive, transferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 1
• Total formula weight: 39579.21

Authors

Kishikawa, S.,Takano, K.,Ubukata, O.,Hanzawa, H. (deposition date: 2022-04-22, release date: 2023-03-01, Last modification date: 2023-11-29)

• Primary citation: Takano, K.,Munehira, Y.,Hatanaka, M.,Murakami, R.,Shibata, Y.,Shida, T.,Takeuchi, K.,Takechi, S.,Tabata, T.,Shimada, T.,Kishikawa, S.,Matsui, Y.,Ubukata, O.,Seki, T.,Kaneta, Y.; Discovery of a Novel ATP-Competitive MEK Inhibitor DS03090629 that Overcomes Resistance Conferred by BRAF Overexpression in BRAF-Mutated Melanoma.; Mol.Cancer Ther., 22:317-332, 2023; PubMed: 36622773; DOI: 10.1158/1535-7163.MCT-22-0306

Experimental method

X-RAY DIFFRACTION (2.1 Å)