7BVF
Cryo-EM structure of Mycobacterium tuberculosis arabinosyltransferase EmbA-EmbB-AcpM2 in complex with ethambutol
7BVF の概要
| エントリーDOI | 10.2210/pdb7bvf/pdb |
| EMDBエントリー | 30218 |
| 分子名称 | Probable arabinosyltransferase B, Probable arabinosyltransferase A, Meromycolate extension acyl carrier protein, ... (7 entities in total) |
| 機能のキーワード | mycobacterium tuberculosis, cell wall synthesis, drug target, ethambutol, arabinosyltransferase, emba, embb, embc, acyl carrier protein, arabinogalactan, lipoarabinomannan, drug resistance, transferase |
| 由来する生物種 | Mycobacterium tuberculosis H37Rv 詳細 |
| タンパク質・核酸の鎖数 | 3 |
| 化学式量合計 | 251817.41 |
| 構造登録者 | |
| 主引用文献 | Zhang, L.,Zhao, Y.,Gao, Y.,Wu, L.,Gao, R.,Zhang, Q.,Wang, Y.,Wu, C.,Wu, F.,Gurcha, S.S.,Veerapen, N.,Batt, S.M.,Zhao, W.,Qin, L.,Yang, X.,Wang, M.,Zhu, Y.,Zhang, B.,Bi, L.,Zhang, X.,Yang, H.,Guddat, L.W.,Xu, W.,Wang, Q.,Li, J.,Besra, G.S.,Rao, Z. Structures of cell wall arabinosyltransferases with the anti-tuberculosis drug ethambutol. Science, 368:1211-1219, 2020 Cited by PubMed Abstract: The arabinosyltransferases EmbA, EmbB, and EmbC are involved in cell wall synthesis and are recognized as targets for the anti-tuberculosis drug ethambutol. In this study, we determined cryo-electron microscopy and x-ray crystal structures of mycobacterial EmbA-EmbB and EmbC-EmbC complexes in the presence of their glycosyl donor and acceptor substrates and with ethambutol. These structures show how the donor and acceptor substrates bind in the active site and how ethambutol inhibits arabinosyltransferases by binding to the same site as both substrates in EmbB and EmbC. Most drug-resistant mutations are located near the ethambutol binding site. Collectively, our work provides a structural basis for understanding the biochemical function and inhibition of arabinosyltransferases and the development of new anti-tuberculosis agents. PubMed: 32327601DOI: 10.1126/science.aba9102 主引用文献が同じPDBエントリー |
| 実験手法 | ELECTRON MICROSCOPY (2.97 Å) |
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