3CBM

SET7/9-ER-AdoMet complex

3CBM の概要

• エントリーDOI: 10.2210/pdb3cbm/pdb
• 関連するPDBエントリー: 3CBO 3CBP
• 分子名称: Histone-lysine N-methyltransferase SETD7, Estrogen receptor, S-ADENOSYL-L-HOMOCYSTEINE, ... (5 entities in total)
• 機能のキーワード: estrogen receptor, protein lysine methylation, activator, chromatin regulator, chromosomal protein, methyltransferase, nucleus, s-adenosyl-l-methionine, transcription, transcription regulation, transferase, alternative splicing, dna-binding, lipid-binding, metal-binding, phosphoprotein, polymorphism, steroid-binding, zinc, zinc-finger, transferase-transferase receptor complex, transferase/transferase receptor
• 由来する生物種: Homo sapiens (Human); 詳細
• 細胞内の位置: Nucleus: Q8WTS6
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 30344.01

構造登録者

Cheng, X.,Jia, D. (登録日: 2008-02-22, 公開日: 2008-05-13, 最終更新日: 2023-08-30)

主引用文献

Subramanian, K.,Jia, D.,Kapoor-Vazirani, P.,Powell, D.R.,Collins, R.E.,Sharma, D.,Peng, J.,Cheng, X.,Vertino, P.M.
Regulation of estrogen receptor alpha by the SET7 lysine methyltransferase.
Mol.Cell, 30:336-347, 2008

PubMed Abstract: Estrogen receptor alpha (ER) is a ligand-dependent transcription factor. Upon binding estrogen, ER recruits coactivator complexes with histone acetyltransferase or methyltransferase activities to activate downstream target genes. In addition to histones, coactivators can modify ER itself and other proteins in the transactivation complex. Here, we show that ER is directly methylated at lysine 302 (K302) by the SET7 methyltransferase. SET7-mediated methylation stabilizes ER and is necessary for the efficient recruitment of ER to its target genes and for their transactivation. The SET7-ER complex structure reveals the molecular basis for ER peptide recognition and predicts that modifications or mutations of nearby residues would affect K302 methylation. Indeed, a breast cancer-associated mutation at K303 (K303R) alters methylation at K302 in vitro and in vivo. These findings raise the possibility that generation, recognition, and removal of modifications within the ER hinge region generate "ER modification cassettes" that yield distinct patterns for signaling downstream events.

PubMed: 18471979
DOI: 10.1016/j.molcel.2008.03.022

実験手法

X-RAY DIFFRACTION (1.69 Å)