2013
DOI: 10.1021/ja400021x
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N,C-Capped Dipeptides with Selectivity for Mycobacterial Proteasome over Human Proteasomes: Role of S3 and S1 Binding Pockets

Abstract: 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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Cited by 52 publications
(92 citation statements)
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References 18 publications
(57 reference statements)
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“…1C), similar to DPLG-2 20 . Based on the dose-dependence curves, we calculated the IC 50 values of these compounds (Table 1) against Mtb20SOG; all were in the narrow range of 0.010–0.041 μM.…”
Section: Resultssupporting
confidence: 53%
See 2 more Smart Citations
“…1C), similar to DPLG-2 20 . Based on the dose-dependence curves, we calculated the IC 50 values of these compounds (Table 1) against Mtb20SOG; all were in the narrow range of 0.010–0.041 μM.…”
Section: Resultssupporting
confidence: 53%
“…IC 50 values of compounds against Mtb20SOG, β5i and β5c were determined from tests in a 96-well format as reported 20 . In brief, 1 μL of compound in a 3x series dilution in DMSO at concentrations from 100 μM to 0.0017 μM were spotted to the bottom of a black 96-well plate having a solid bottom.…”
Section: Methodsmentioning
confidence: 99%
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“…The potential to target persistent or latent bacteria has made the Mtb proteasome system a prioritized target for the development of antituberculosis drugs (10,11). Indeed, Mtb-specific proteasome inhibitors have been identified that may provide a promising lead for new drugs to treat tuberculosis (12,13).…”
mentioning
confidence: 99%
“…The synthetic route and methods of compound characterization were similar to those reported for N,C-capped dipeptidomimetics (15,28), with modifications as given in the supplemental online material. All compounds were >95% pure.…”
Section: Methodsmentioning
confidence: 99%