N,C-Capped Dipeptides with Selectivity for Mycobacterial Proteasome over Human Proteasomes: Role of S3 and S1 Binding Pockets
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- 作者：Gang Lin ; Tamutenda Chidawanyika ; Christopher Tsu ; Thulasi Warrier ; Julien Vaubourgeix ; Christopher Blackburn ; Kenneth Gigstad ; Michael Sintchak ; Lawrence Dick ; Carl Nathan
- 刊名：The Journal of the American Chemical Society
- 出版年：2013
- 出版时间：July 10, 2013
- 年：2013
- 卷：135
- 期：27
- 页码：9968-9971
- 全文大小：296K
- 年卷期：v.135,no.27(July 10, 2013)
- ISSN：1520-5126
文摘
We identified N,C-capped dipeptides that are selective for the Mycobacterium tuberculosis proteasome over human constitutive and immunoproteasomes. Differences in the S3 and S1 binding pockets appeared to account for the species selectivity. The inhibitors can penetrate mycobacteria and kill nonreplicating M. tuberculosis under nitrosative stress.