8DC6

Crystal structure of p53 Y220C covalently bound to indole KG6

8DC6 の概要

• エントリーDOI: 10.2210/pdb8dc6/pdb
• 分子名称: Cellular tumor antigen p53, ZINC ION, SULFATE ION, ... (6 entities in total)
• 機能のキーワード: p53, tp53, tumor suppressor, cell cycle
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 101924.12

構造登録者

Guiley, K.Z.,Shokat, K.M. (登録日: 2022-06-15, 公開日: 2022-10-12, 最終更新日: 2024-10-23)

主引用文献

Guiley, K.Z.,Shokat, K.M.
A Small Molecule Reacts with the p53 Somatic Mutant Y220C to Rescue Wild-type Thermal Stability.
Cancer Discov, 13:56-69, 2023

PubMed Abstract: The transcription factor and tumor suppressor protein p53 is the most frequently mutated and inactivated gene in cancer. Mutations in p53 result in deregulated cell proliferation and genomic instability, both hallmarks of cancer. There are currently no therapies available that directly target mutant p53 to rescue wild-type function. In this study, we identify covalent compsounds that selectively react with the p53 somatic mutant cysteine Y220C and restore wild-type thermal stability.

PubMed: 36197521
DOI: 10.1158/2159-8290.CD-22-0381

実験手法

X-RAY DIFFRACTION (1.60000908706 Å)