4HJO

Crystal structure of the inactive EGFR tyrosine kinase domain with erlotinib

4HJO の概要

• エントリーDOI: 10.2210/pdb4hjo/pdb
• 分子名称: Epidermal growth factor receptor, [6,7-BIS(2-METHOXY-ETHOXY)QUINAZOLINE-4-YL]-(3-ETHYNYLPHENYL)AMINE (3 entities in total)
• 機能のキーワード: inactive tyrosine kinase domain, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cell membrane; Single-pass type I membrane protein. Isoform 2: Secreted: P00533
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 38950.01

構造登録者

Park, J.H.,Lemmon, M.A. (登録日: 2012-10-13, 公開日: 2012-11-14, 最終更新日: 2023-09-20)

主引用文献

Park, J.H.,Liu, Y.,Lemmon, M.A.,Radhakrishnan, R.
Erlotinib binds both inactive and active conformations of the EGFR tyrosine kinase domain.
Biochem.J., 448:417-423, 2012

PubMed Abstract: Erlotinib and gefitinib, tyrosine kinase inhibitors used to block EGFR (epidermal growth factor receptor) signalling in cancer, are thought to bind only the active conformation of the EGFR-TKD (tyrosine kinase domain). Through parallel computational and crystallographic studies, we show in the present study that erlotinib also binds the inactive EGFR-TKD conformation, which may have significant implications for its use in EGFR-mutated cancers.

PubMed: 23101586
DOI: 10.1042/BJ20121513

実験手法

X-RAY DIFFRACTION (2.75 Å)