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18 results

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Page 1
The Chemistry and Biology of Cyclophostin, the Cyclipostins and Related Compounds.
Spilling CD. Spilling CD. Molecules. 2019 Jul 16;24(14):2579. doi: 10.3390/molecules24142579. Molecules. 2019. PMID: 31315184 Free PMC article. Review.
Cyclophostin, the cyclipostins and the salinipostins are structurally related cyclic enolphosphate natural products. ...
Cyclophostin, the cyclipostins and the salinipostins are structurally related cyclic enolphosphate natural products. ...
Cyclipostins and Cyclophostin Analogues as Multitarget Inhibitors That Impair Growth of Mycobacterium abscessus.
Madani A, Ridenour JN, Martin BP, Paudel RR, Abdul Basir A, Le Moigne V, Herrmann JL, Audebert S, Camoin L, Kremer L, Spilling CD, Canaan S, Cavalier JF. Madani A, et al. ACS Infect Dis. 2019 Sep 13;5(9):1597-1608. doi: 10.1021/acsinfecdis.9b00172. Epub 2019 Jul 25. ACS Infect Dis. 2019. PMID: 31299146
Twelve new Cyclophostin and Cyclipostins analogues (CyC(19-30)) were synthesized, thus extending our series to 38 CyCs. ...
Twelve new Cyclophostin and Cyclipostins analogues (CyC(19-30)) were synthesized, thus extending our series to 38 CyCs. ...
Lipolytic enzymes inhibitors: A new way for antibacterial drugs discovery.
Cavalier JF, Spilling CD, Durand T, Camoin L, Canaan S. Cavalier JF, et al. Eur J Med Chem. 2021 Jan 1;209:112908. doi: 10.1016/j.ejmech.2020.112908. Epub 2020 Oct 12. Eur J Med Chem. 2021. PMID: 33071055 Review.
The results highlighted here include a complete overview of the antibacterial activities, either in broth medium or inside infected macrophages, of two families of promising and potent anti-mycobacterial multi-target agents, i.e. oxadiazolone-core compounds (OX) and Cyclophost …
The results highlighted here include a complete overview of the antibacterial activities, either in broth medium or inside infected macropha …
Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis.
Nguyen PC, Delorme V, Bénarouche A, Martin BP, Paudel R, Gnawali GR, Madani A, Puppo R, Landry V, Kremer L, Brodin P, Spilling CD, Cavalier JF, Canaan S. Nguyen PC, et al. Sci Rep. 2017 Sep 18;7(1):11751. doi: 10.1038/s41598-017-11843-4. Sci Rep. 2017. PMID: 28924204 Free PMC article.
A new class of Cyclophostin and Cyclipostins (CyC) analogs have been investigated against Mycobacterium tuberculosis H37Rv (M. tb) grown either in broth medium or inside macrophages. ...
A new class of Cyclophostin and Cyclipostins (CyC) analogs have been investigated against Mycobacterium tuberculosis H37Rv (M. tb) gr …
Cyclophostin and Cyclipostins analogues, new promising molecules to treat mycobacterial-related diseases.
Nguyen PC, Madani A, Santucci P, Martin BP, Paudel RR, Delattre S, Herrmann JL, Spilling CD, Kremer L, Canaan S, Cavalier JF. Nguyen PC, et al. Int J Antimicrob Agents. 2018 Apr;51(4):651-654. doi: 10.1016/j.ijantimicag.2017.12.001. Epub 2017 Dec 11. Int J Antimicrob Agents. 2018. PMID: 29241819
This study evaluated the efficacy and selectivity of a panel of Cyclophostin and Cyclipostins analogues (CyCs) against various bacteria and mycobacteria. ...
This study evaluated the efficacy and selectivity of a panel of Cyclophostin and Cyclipostins analogues (CyCs) against various bacter …
Direct capture, inhibition and crystal structure of HsaD (Rv3569c) from M. tuberculosis.
Barelier S, Avellan R, Gnawali GR, Fourquet P, Roig-Zamboni V, Poncin I, Point V, Bourne Y, Audebert S, Camoin L, Spilling CD, Canaan S, Cavalier JF, Sulzenbacher G. Barelier S, et al. FEBS J. 2023 Mar;290(6):1563-1582. doi: 10.1111/febs.16645. Epub 2022 Oct 13. FEBS J. 2023. PMID: 36197115 Free article.
However, the enzymes and mechanisms underlying such metabolism are still largely unknown. We previously reported that the Cyclophostin & Cyclipostins (CyC) analogues, a new family of potent antimycobacterial molecules, react specifically and covalently with (Ser/Cys)-b …
However, the enzymes and mechanisms underlying such metabolism are still largely unknown. We previously reported that the Cyclophostin …
Synthesis and Biological Characterization of Fluorescent Cyclipostins and Cyclophostin Analogues: New Insights for the Diagnosis of Mycobacterial-Related Diseases.
Sarrazin M, Martin BP, Avellan R, Gnawali GR, Poncin I, Le Guenno H, Spilling CD, Cavalier JF, Canaan S. Sarrazin M, et al. ACS Infect Dis. 2022 Dec 9;8(12):2564-2578. doi: 10.1021/acsinfecdis.2c00448. Epub 2022 Nov 15. ACS Infect Dis. 2022. PMID: 36379042 Free article.
We report here the synthesis of fluorescent Dansyl derivatives of four active cyclipostins and cyclophostin analogues (CyCs) and provide new insights regarding the CyC's lack of activity against Gram-negative and Gram-positive bacteria, and above all into their mode of act …
We report here the synthesis of fluorescent Dansyl derivatives of four active cyclipostins and cyclophostin analogues (CyCs) and prov …
Cyclipostins and cyclophostin analogs inhibit the antigen 85C from Mycobacterium tuberculosis both in vitro and in vivo.
Viljoen A, Richard M, Nguyen PC, Fourquet P, Camoin L, Paudal RR, Gnawali GR, Spilling CD, Cavalier JF, Canaan S, Blaise M, Kremer L. Viljoen A, et al. J Biol Chem. 2018 Feb 23;293(8):2755-2769. doi: 10.1074/jbc.RA117.000760. Epub 2018 Jan 4. J Biol Chem. 2018. PMID: 29301937 Free PMC article.
We previously reported the discovery of a new class of cyclipostins and cyclophostin (CyC) analogs exhibiting potent activity against Mycobacterium tuberculosis both in vitro and in infected macrophages. ...
We previously reported the discovery of a new class of cyclipostins and cyclophostin (CyC) analogs exhibiting potent activity against …
Rat hormone sensitive lipase inhibition by cyclipostins and their analogs.
Vasilieva E, Dutta S, Malla RK, Martin BP, Spilling CD, Dupureur CM. Vasilieva E, et al. Bioorg Med Chem. 2015 Mar 1;23(5):944-52. doi: 10.1016/j.bmc.2015.01.028. Epub 2015 Jan 22. Bioorg Med Chem. 2015. PMID: 25678014 Free PMC article.
The smaller lactone ring is not critical to activity, a similarity shared with cyclophostin and AChE. The HSL kinetics of inhibition for the cyclipostin P trans diastereomer were examined in detail. The reaction is irreversible with a KI of 40nM and a rate constant for ina …
The smaller lactone ring is not critical to activity, a similarity shared with cyclophostin and AChE. The HSL kinetics of inhibition …
18 results