IndraLab

Statements


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"Nevertheless, the probability that CAMPACs are extruded through another set of efflux systems of RND family, 37 cannot be excluded with absolute certainty."

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"This requirement explains our finding that the IC 50 values for CAM and CAMPACs measured in S. aureus are smaller than those measured in E. coli ( Table 1 )."

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"This prompted us to examine the activity of CAMPACs against three multi-drug resistant (MDR) MRSA isolates, GRE2272, GRE2372, and GRE2691."

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"37 Moreover, the PA portion(s) may endow CAMPACs with the ability to penetrate the bacterial inner membrane, by utilizing the polyamine uptake system, a group of polyamine carriers which pertain to t[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Except for compound 2 , all the rest CAMPACs of this subgroup competed more efficiently with putrescine and spermidine for the polyamine uptake system, than with spermine."

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"This finding tempted us to assume that CAMPACs are mainly internalized into the cell through the transporter encoded by the pPT104 operon, which constitutes the spermidine-preferential uptake system."

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"40 Nevertheless, the most effective member of CAMPACs in bacteria, compound 4 , was also able to penetrate eukaryotic cells."

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"41 The rescue in growth observed when CAMPACs and exogenous polyamines are simultaneously added in the medium of bacterial culture may arise either due to a competition between them for the polyamin[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"To differentiate between these two possibilities and to confirm that CAMPACs act on their target after entry into the cells, E. coli cells at an A 560 of 0.020 were grown at 37 °C in M9 medium supple[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"In parallel, cells were grown in the absence of CAMPACs (control cultures)."

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"Although much less than the exogenous doses, the intracellular concentrations of CAMPACs detected were adequate to substantially inhibit protein synthesis, given that the inhibition constant ( K i ∗ [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Nevertheless, polyamines are essential for cell growth and protein synthesis, 43 and therefore the revealed effects on polyamine content suggest that CAMPACs may directly exhibit an additional mode o[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"The origin of this additional effect of CAMPACs is not clear at present."

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"A series of CAMPACs ( 1 – 9 ) were readily synthesized from either CAM, through indirect oxidation of its primary hydroxyl function, or from CLB through N-acylation with succinic or phthalic anhydrid[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Encouragingly, a previous study of CAMPACs has indicated that these compounds are well tolerated by human leukocytes."

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"24 The above information prompted us to design and synthesize a series of CAM–PA conjugates (CAMPACs), expecting that the PA-conjugated portion could strengthen the binding of CAM to the ribosome."

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"25–27 The synthesized series of CAMPACs 1 – 9 is depicted in Figure 1 ."

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"28 Certainly, further work has to be performed to refute the suspicion that toxic properties may be shared by CAMPACs."

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"The protected CAMPACs were obtained in pure form following FCC purification."

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"Recently, we published on the effects of CAMPACs 1 – 9 on peptide bond formation catalyzed by the ribosome in a cell-free system derived from E. coli , the growth of Gram-negative and Gram-positive b[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"In the present study, we focus on the synthesis of CAMPACs 1 – 9 , the mechanisms by which they penetrate the bacterial outer and inner cellular membranes, and the effects of efflux pumps and the CAM[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"The synthesis of CAMPACs 1 – 5 is depicted in Scheme 1 ."

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"27 Therefore, it is tempting to assume that CAMPACs 4 and 5 receive better recognition by the PotD protein, than the non-benzylated ones 2 , 3 , and 7 ."

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"As shown in Table 1 , this efflux system does not seem to affect the antibacterial activity of CAMPACs, as the IC 50 values regarding this strain were similar to those of wild-type E. coli ."