N,C-Capped dipeptides with selectivity for mycobacterial proteasome over human proteasomes: role of S3 and S1 binding pockets.
N,C-Capped dipeptides with selectivity for mycobacterial proteasome over human proteasomes: role of S3 and S1 binding pockets.
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DOI:
10.1021/ja400021x
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发表时间:
2013-07-10
影响因子:
15
通讯作者:
Nathan, Carl
中科院分区:
文献类型:
--
作者:
Lin, Gang;Chidawanyika, Tamutenda;Tsu, Christopher;Warrier, Thulasi;Vaubourgeix, Julien;Blackburn, Christopher;Gigstad, Kenneth;Sintchak, Michael;Dick, Lawrence;Nathan, Carl
We identified N,C-capped dipeptides that are selective for the Mycobacterium tuberculosis proteasome over human constitutive and immunoproteasomes. Differences in S3 and S1 binding pockets appeared to account for species-selectivity. The inhibitors are able to penetrate mycobacteria and kill non-replicating M. tuberculosis under nitrosative stress.
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