2Z8C

Phosphorylated insulin receptor tyrosine kinase in complex with (4-{[5-carbamoyl-4-(3-methylanilino)pyrimidin-2-yl]amino}phenyl)acetic acid

2Z8C の概要

• エントリーDOI: 10.2210/pdb2z8c/pdb
• 関連するPDBエントリー: 2Z7L
• 分子名称: Insulin receptor, 6-mer peptide from Insulin receptor substrate 1, [4-({5-(AMINOCARBONYL)-4-[(3-METHYLPHENYL)AMINO]PYRIMIDIN-2-YL}AMINO)PHENYL]ACETIC ACID (3 entities in total)
• 機能のキーワード: transferase, alternative splicing, atp-binding, carbohydrate metabolism, cleavage on pair of basic residues, diabetes mellitus, disease mutation, glycoprotein, kinase, membrane, nucleotide-binding, phosphorylation, polymorphism, receptor, transmembrane, tyrosine-protein kinase, transducer
• 由来する生物種: Homo sapiens (Human); 詳細
• 細胞内の位置: Cell membrane; Single-pass type I membrane protein: P06213
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 35826.57

構造登録者

Katayama, N.,Kurihara, H. (登録日: 2007-09-05, 公開日: 2008-08-12, 最終更新日: 2024-11-20)

主引用文献

Katayama, N.,Orita, M.,Yamaguchi, T.,Hisamichi, H.,Kuromitsu, S.,Kurihara, H.,Sakashita, H.,Matsumoto, Y.,Fujita, S.,Niimi, T.
Identification of a key element for hydrogen-bonding patterns between protein kinases and their inhibitors.
Proteins, 73:795-801, 2008

PubMed Abstract: In this article, we report crystal structures for inhibitor-kinase complexes in which the inhibitor has different binding orientations and hydrogen-bonding patterns with extracellular-signal regulated kinase 2 and insulin receptor tyrosine kinase. Our crystallographic studies, and sequence and structural analyses of 532 coordinates of kinases held in the Protein Data Bank, suggest that the length of the "specificity linker" described here is a key structural element of the hydrogen-bonding patterns between protein kinases and their inhibitors.

PubMed: 18767165
DOI: 10.1002/prot.22207

実験手法

X-RAY DIFFRACTION (3.25 Å)