8RIW

T2R-TTL-1-L01 complex

これはPDB形式変換不可エントリーです。

8RIW の概要

• エントリーDOI: 10.2210/pdb8riw/pdb
• 関連するPDBエントリー: 8RIV
• 分子名称: Tubulin alpha-1B chain, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, (2-methyl-1~{H}-indol-5-yl) 3,4,5-trimethoxybenzenesulfonate, ... (14 entities in total)
• 機能のキーワード: cell cycle, tubulin fold, cytoskeleton, microtubule
• 由来する生物種: Rattus norvegicus (Norway rat); 詳細
• タンパク質・核酸の鎖数: 6
• 化学式量合計: 265543.49

構造登録者

Prota, A.E.P.,Boiarska, Z.,Homer, J.A.,Steinmetz, M.O.,Moses, J.E. (登録日: 2023-12-19, 公開日: 2024-03-27)

主引用文献

Homer, J.A.,Koelln, R.A.,Barrow, A.S.,Gialelis, T.L.,Boiarska, Z.,Steinohrt, N.S.,Lee, E.F.,Yang, W.H.,Johnson, R.M.,Chung, T.,Habowski, A.N.,Vishwakarma, D.S.,Bhunia, D.,Avanzi, C.,Moorhouse, A.D.,Jackson, M.,Tuveson, D.A.,Lyons, S.K.,Lukey, M.J.,Fairlie, W.D.,Haider, S.M.,Steinmetz, M.O.,Prota, A.E.,Moses, J.E.
Modular synthesis of functional libraries by accelerated SuFEx click chemistry.
Chem Sci, 15:3879-3892, 2024

PubMed Abstract: Accelerated SuFEx Click Chemistry (ASCC) is a powerful method for coupling aryl and alkyl alcohols with SuFEx-compatible functional groups. With its hallmark favorable kinetics and exceptional product yields, ASCC streamlines the synthetic workflow, simplifies the purification process, and is ideally suited for discovering functional molecules. We showcase the versatility and practicality of the ASCC reaction as a tool for the late-stage derivatization of bioactive molecules and in the array synthesis of sulfonate-linked, high-potency, microtubule targeting agents (MTAs) that exhibit nanomolar anticancer activity against multidrug-resistant cancer cell lines. These findings underscore ASCC's promise as a robust platform for drug discovery.

PubMed: 38487227
DOI: 10.1039/d3sc05729a

実験手法

X-RAY DIFFRACTION (2.57 Å)