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Can I read A synthetic diterpene analogue inhibits mycobacterial persistence and biofilm formation by targeting (p)ppGpp synthetases on EtoBox?
A synthetic diterpene analogue inhibits mycobacterial persistence and biofilm formation by targeting (p)ppGpp synthetases by Alexander G. Tkachenko; Natalya M. Kashevarova; Roman Yu. Sidorov; Larisa Yu. Nesterova; Anna V. Akhova; Ivan V. Tsyganov; Vladimir Yu. Vaganov; Sergei A. Shipilovskikh; Aleksandr E. Rubtsov; Andrei V. Malkov is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is A synthetic diterpene analogue inhibits mycobacterial persistence and biofilm formation by targeting (p)ppGpp synthetases about?
Bacterial persistence coupled with biofilm formation is directly associated with failure of antibiotic treatment of tuberculosis. We have now identified 4-(4,7-DiMethyl-1,2,3,4-tetrahydroNaphthalene-1-yl)Pentanoic acid (DMNP), a synthetic diterpene analogue, as a lead compound that was capable of suppressing persistence and eradicating biofilms in Mycobacterium smegmatis. By using two reciprocal experimental approaches - Δrel and ΔrelZ gene knockout mutations versus rel and relZ overexpression technique - we showed that both Rel and RelZ (p)ppGpp synthetases are plausible candidates for serving as targets for DMNP. In vitro, DMNP inhibited (p)ppGpp-synthesizing activity of purified Rel in a concentration-dependent manner. These findings, supplemented by molecular docking simulation, suggest that DMNP targets the structural sites shared by Rel, RelZ, and presumably by a few others as yet unidentified (p)ppGpp producers, thereby inhibiting persister cell formation and eradicating biofilms. Therefore, DMNP may serve as a promising lead for development of antimycobacterial drugs.
Who reads A synthetic diterpene analogue inhibits mycobacterial persistence and biofilm formation by targeting (p)ppGpp synthetases?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Alexander G. Tkachenko; Natalya M. Kashevarova; Roman Yu. Sidorov; Larisa Yu. Nesterova; Anna V. Akhova; Ivan V. Tsyganov; Vladimir Yu. Vaganov; Sergei A. Shipilovskikh; Aleksandr E. Rubtsov; Andrei V. Malkov
- Publisher
- Elsevier BV
- Published
- 2021
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)