3EKK

Insulin receptor kinase complexed with an inhibitor

3EKK の概要

• エントリーDOI: 10.2210/pdb3ekk/pdb
• 関連するPDBエントリー: 3EKN 3ELJ
• 分子名称: Insulin receptor, 2-[(2-{[1-(N,N-dimethylglycyl)-5-methoxy-1H-indol-6-yl]amino}-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-6-fluoro-N-methylbenzamide (3 entities in total)
• 機能のキーワード: insulin, tyrosine kinase, atp-binding, carbohydrate metabolism, cleavage on pair of basic residues, diabetes mellitus, disease mutation, glycoprotein, kinase, membrane, nucleotide-binding, phosphoprotein, receptor, transferase, transmembrane, tyrosine-protein kinase
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Membrane; Single-pass type I membrane protein: P06213
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 35380.35

構造登録者

Chamberlain, S.,Atkins, C.,Deanda, F.,Dumble, M.,Gerding, R.,Groy, A.,Korenchuk, S.,Kumar, R.,Lei, H.,Mook, R.,Moorthy, G.,Redman, A.,Rowland, J.,Sabbatini, P.,Shewchuk, L. (登録日: 2008-09-19, 公開日: 2008-12-23, 最終更新日: 2023-08-30)

• 主引用文献: Chamberlain, S.D.,Wilson, J.W.,Deanda, F.,Patnaik, S.,Redman, A.M.,Yang, B.,Shewchuk, L.,Sabbatini, P.,Leesnitzer, M.A.,Groy, A.,Atkins, C.,Gerding, R.,Hassell, A.M.,Lei, H.,Mook, R.A.,Moorthy, G.,Rowand, J.L.,Stevens, K.L.,Kumar, R.,Shotwell, J.B.; Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: Potent inhibitors of the IGF-1R receptor tyrosine kinase.; Bioorg.Med.Chem.Lett., 19:469-473, 2009; PubMed: 19056263; DOI: 10.1016/j.bmcl.2008.11.046

実験手法

X-RAY DIFFRACTION (2.1 Å)