8B7C

Tubulin-maytansinoid-12 complex

8B7C の概要

• エントリーDOI: 10.2210/pdb8b7c/pdb
• 分子名称: Tubulin alpha-1B chain, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, [(1~{S},2~{R},3~{S},5~{S},6~{S},16~{E},18~{E},20~{R},21~{S})-11-chloranyl-12,20-dimethoxy-2,5,9,16-tetramethyl-21-oxidanyl-8,23-bis(oxidanylidene)-4,24-dioxa-9,22-diazatetracyclo[19.3.1.1^{10,14}.0^{3,5}]hexacosa-10(26),11,13,16,18-pentaen-6-yl] 4-[2-(2-azanylhydrazinyl)ethyl]benzoate, ... (13 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: 265353.68

構造登録者

Boiarska, Z.,Perez-Pena, H.,Abel, A.-C.,Marzullo, P.,Alvarez-Bernad, B.,Bonato, F.,Santini, B.,Horvath, D.,Lucena-Agell, D.,Vasile, F.,Sironi, M.,Diaz, J.F.,Steinmetz, M.O.,Prota, A.E.,Pieraccini, S.,Passarella, D. (登録日: 2022-09-29, 公開日: 2023-08-23)

主引用文献

Boiarska, Z.,Perez-Pena, H.,Abel, A.C.,Marzullo, P.,Alvarez-Bernad, B.,Bonato, F.,Santini, B.,Horvath, D.,Lucena-Agell, D.,Vasile, F.,Sironi, M.,Diaz, J.F.,Prota, A.E.,Pieraccini, S.,Passarella, D.
Maytansinol Functionalization: Towards Useful Probes for Studying Microtubule Dynamics.
Chemistry, 29:e202203431-e202203431, 2023

PubMed Abstract: Maytansinoids are a successful class of natural and semisynthetic tubulin binders, known for their potent cytotoxic activity. Their wider application as cytotoxins and chemical probes to study tubulin dynamics has been held back by the complexity of natural product chemistry. Here we report the synthesis of long-chain derivatives and maytansinoid conjugates. We confirmed that bulky substituents do not impact their high activity or the scaffold's binding mode. These encouraging results open new avenues for the design of new maytansine-based probes.

PubMed: 36468686
DOI: 10.1002/chem.202203431

実験手法

X-RAY DIFFRACTION (1.9 Å)