| 题名 | Identification of Serine 119 as an Effective Inhibitor Binding Site of M. tuberculosis Ubiquitin-like Protein Ligase PafA Using Purified Proteins and M. smegmatis |
| 作者 | Jiang, He-Wei1; Czajkowsky, Daniel M.2,3; Wang, Tao4,5  ; Wang, Xu-De6; Wang, Jia-bin1; Zhang, Hai-Nan1; Liu, Cheng-Xi1; Wu, Fan-Lin1; He, Xiang1; Xu, Zhao-Wei1; Chen, Hong1; Guo, Shu-Juan1; Li, Yang1; Bi, Li-Jun7,8,9,10; Deng, Jiao-Yu6; Xie, Jin11; Pei, Jian-Feng11; Zhang, Xian-En7,8; Tao, Sheng-Ce1,3,12
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| 通讯作者 | Tao, Sheng-Ce |
| 发表日期 | 2018-04
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| DOI | |
| 发表期刊 | |
| ISSN | 2352-3964
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| 卷号 | 30页码:225-236 |
| 摘要 | Owing to the spread of multidrug resistance (MDR) and extensive drug resistance (XDR), there is a pressing need to identify potential targets for the development of more-effective anti-M. tuberculosis (Mtb) drugs. PafA, as the sole Prokaryotic Ubiquitin-like Protein ligase in the Pup-proteasome System (PPS) of Mtb, is an attractive drug target. Here, we show that the activity of purified Mtb PafA is significantly inhibited upon the association of AEBSF (4-(2-aminoethyl) benzenesulfonyl fluoride) to PafA residue Serine 119 (S119). Mutation of S119 to amino acids that resemble AEBSF has similar inhibitory effects on the activity of purified Mtb PafA. Structural analysis reveals that although S119 is distant from the PafA catalytic site, it is located at a critical position in the groove where PafA binds the C-terminal region of Pup. Phenotypic studies demonstrate that S119 plays critical roles in the function of Mtb PafA when tested in M. smegmatis. Our study suggests that targeting S119 is a promising direction for developing an inhibitor of M. tuberculosis PafA. (C) 2018 The Author(s). Published by Elsevier B.V. |
| 关键词 | |
| 相关链接 | [来源记录] |
| 收录类别 | |
| 语种 | 英语
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| 学校署名 | 其他
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| 资助项目 | Shanghai Jiao Tong University[16X120030015]
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| WOS研究方向 | General & Internal Medicine
; Research & Experimental Medicine
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| WOS类目 | Medicine, General & Internal
; Medicine, Research & Experimental
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| WOS记录号 | WOS:000430303000028
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| 出版者 | |
| 来源库 | Web of Science
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| 引用统计 |
被引频次[WOS]：8
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| 成果类型 | 期刊论文 |
| 条目标识符 | http://sustech.caswiz.com/handle/2SGJ60CL/27906 |
| 专题 | 生命科学学院_生物系 |
| 作者单位 | 1.Shanghai Jiao Tong Univ, Minist Educ, Key Lab Syst Biomed, Shanghai Ctr Syst Biomed, Shanghai 200240, Peoples R China 2.Shanghai Jiao Tong Univ, BioID Ctr, Sch Biomed Engn, Shanghai 200240, Peoples R China 3.Shanghai Jiao Tong Univ, Sch Biomed Engn, Shanghai 200240, Peoples R China 4.Southern Univ Sci & Technol, Dept Biol, Shenzhen 518055, Peoples R China 5.Shenzhen Ctr Dis Control & Prevent, SZCDC SUSTech Joint Key Lab Trop Dis, Shenzhen 518055, Peoples R China 6.Chinese Acad Sci, Wuhan Inst Virol, State Key Lab Virol, Wuhan 430071, Hubei, Peoples R China 7.Chinese Acad Sci, Inst Biophys, Natl Key Lab Biomacromol, Key Lab Noncoding RNA, Beijing 100101, Peoples R China 8.Chinese Acad Sci, Inst Biophys, Key Lab Prot & Peptide Pharmaceut, Beijing 100101, Peoples R China 9.TB Healthcare Biotechnol Co Ltd, Foshan 528000, Guangdong, Peoples R China 10.Foshan Univ, Sch Stomatol & Med, Foshan 528000, Guangdong, Peoples R China 11.Peking Univ, Acad Adv Interdisciplinary Studies, Ctr Quantitat Biol, Beijing 100871, Peoples R China 12.Shanghai Jiao Tong Univ, State Key Lab Oncogenes & Related Genes, Shanghai 200240, Peoples R China |
| 推荐引用方式 GB/T 7714 |
Jiang, He-Wei,Czajkowsky, Daniel M.,Wang, Tao,et al. Identification of Serine 119 as an Effective Inhibitor Binding Site of M. tuberculosis Ubiquitin-like Protein Ligase PafA Using Purified Proteins and M. smegmatis[J]. EBioMedicine,2018,30:225-236.
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| APA |
Jiang, He-Wei.,Czajkowsky, Daniel M..,Wang, Tao.,Wang, Xu-De.,Wang, Jia-bin.,...&Tao, Sheng-Ce.(2018).Identification of Serine 119 as an Effective Inhibitor Binding Site of M. tuberculosis Ubiquitin-like Protein Ligase PafA Using Purified Proteins and M. smegmatis.EBioMedicine,30,225-236.
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| MLA |
Jiang, He-Wei,et al."Identification of Serine 119 as an Effective Inhibitor Binding Site of M. tuberculosis Ubiquitin-like Protein Ligase PafA Using Purified Proteins and M. smegmatis".EBioMedicine 30(2018):225-236.
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