3ACL

Crystal Structure of Human Pirin in complex with Triphenyl Compound

3ACL の概要

• エントリーDOI: 10.2210/pdb3acl/pdb
• 関連するPDBエントリー: 1J1L
• 分子名称: Pirin, FE (II) ION, N-{[4-(benzyloxy)phenyl](methyl)-lambda~4~-sulfanylidene}-4-methylbenzenesulfonamide, ... (4 entities in total)
• 機能のキーワード: cupin, inhibitor, complex, iron, metal binding protein
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Nucleus : O00625
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 33443.64

構造登録者

Okumura, H.,Miyazaki, I.,Simizu, S.,Osada, H. (登録日: 2010-01-05, 公開日: 2010-08-18, 最終更新日: 2023-11-01)

主引用文献

Miyazaki, I.,Simizu, S.,Okumura, H.,Takagi, S.,Osada, H.
A small-molecule inhibitor shows that pirin regulates migration of melanoma cells
Nat.Chem.Biol., 6:667-673, 2010

PubMed Abstract: The discovery of small molecules that bind to a specific target and disrupt the function of proteins is an important step in chemical biology, especially for poorly characterized proteins. Human pirin is a nuclear protein of unknown function that is widely expressed in punctate subnuclear structures in human tissues. Here, we report the discovery of a small molecule that binds to pirin. We determined how the small molecule bound to pirin by solving the cocrystal structure. Either knockdown of pirin or treatment with the small molecule inhibited melanoma cell migration. Thus, inhibition of pirin by the small molecule has led to a greater understanding of the function of pirin and represents a new method of studying pirin-mediated signaling pathways.

PubMed: 20711196
DOI: 10.1038/nchembio.423

実験手法

X-RAY DIFFRACTION (2.35 Å)