6U5M

Discovery and optimization of salicyclic acid-derived sulfonamide inhibitors of the WDR5:MYC protein-protein interaction

6U5M の概要

• エントリーDOI: 10.2210/pdb6u5m/pdb
• 分子名称: WD repeat-containing protein 5, 5-bromo-2-hydroxy-N-[3-(methylsulfonyl)-5-(pentafluoro-lambda~6~-sulfanyl)phenyl]benzene-1-sulfonamide (3 entities in total)
• 機能のキーワード: wdr5, myc, rbbp5, structure-based design, high-throughput screening, transcription
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 68048.68

構造登録者

Zhao, B.,Wang, F. (登録日: 2019-08-28, 公開日: 2019-12-04, 最終更新日: 2023-10-11)

• 主引用文献: Macdonald, J.D.,Chacon Simon, S.,Han, C.,Wang, F.,Shaw, J.G.,Howes, J.E.,Sai, J.,Yuh, J.P.,Camper, D.,Alicie, B.M.,Alvarado, J.,Nikhar, S.,Payne, W.,Aho, E.R.,Bauer, J.A.,Zhao, B.,Phan, J.,Thomas, L.R.,Rossanese, O.W.,Tansey, W.P.,Waterson, A.G.,Stauffer, S.R.,Fesik, S.W.; Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction.; J.Med.Chem., 62:11232-11259, 2019; PubMed: 31724864; DOI: 10.1021/acs.jmedchem.9b01411

実験手法

X-RAY DIFFRACTION (1.8 Å)