Cyclipostins and Cyclophostin Analogues as Multitarget
Inhibitors That Impair Growth of Mycobacterium abscessus
Version 2 2019-07-25, 17:58
Version 1 2019-07-25, 17:46
Posted on 2019-07-25 - 17:58
Twelve
new Cyclophostin and Cyclipostins analogues (CyC19–30) were synthesized, thus
extending our series to 38 CyCs. Their antibacterial
activities were evaluated against four pathogenic mycobacteria (Mycobacterium abscessus, Mycobacterium marinum, Mycobacterium bovis BCG, and Mycobacterium
tuberculosis) and two Gram negative bacteria. The CyCs displayed very low toxicity toward host cells and were only active
against mycobacteria. Importantly, several CyCs were
active against extracellular M. abscessus (CyC17/CyC18β/CyC25/CyC26) or intramacrophage residing mycobacteria
(CyC7(α,β)/CyC8(α,β)) with minimal
inhibitory concentrations (MIC50) values comparable to
or better than those of amikacin or imipenem, respectively. An activity-based
protein profiling combined with mass spectrometry allowed identification
of the potential target enzymes of CyC17/CyC26, mostly being involved
in lipid metabolism and/or in cell wall biosynthesis. Overall, these
results strengthen the selective activity of the CyCs against mycobacteria, including the most drug-resistant M. abscessus, through the cumulative inhibition of a large
number of Ser- and Cys-enzymes participating in key physiological
processes.
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Madani, Abdeldjalil; Ridenour, Jeremy N.; Martin, Benjamin P.; Paudel, Rishi R.; Abdul Basir, Anosha; Le Moigne, Vincent; et al. (2019). Cyclipostins and Cyclophostin Analogues as Multitarget
Inhibitors That Impair Growth of Mycobacterium abscessus. ACS Publications. Collection. https://doi.org/10.1021/acsinfecdis.9b00172
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AUTHORS (13)
AM
Abdeldjalil Madani
JR
Jeremy N. Ridenour
BM
Benjamin P. Martin
RP
Rishi R. Paudel
AA
Anosha Abdul Basir
VL
Vincent Le Moigne
JH
Jean-Louis Herrmann
SA
Stéphane Audebert
LC
Luc Camoin
LK
Laurent Kremer
CS
Christopher D. Spilling
SC
Stéphane Canaan
JC
Jean-François Cavalier