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1,3,4-oxadiazole derivatives as potential antimicrobial agents.
Tiwari D, Narang R, Sudhakar K, Singh V, Lal S, Devgun M. Tiwari D, et al. Chem Biol Drug Des. 2022 Dec;100(6):1086-1121. doi: 10.1111/cbdd.14100. Epub 2022 Jun 27. Chem Biol Drug Des. 2022. PMID: 35676800 Review.
The present review elaborates the therapeutic targets and mode of interaction of 1,3,4-oxadiazoles as antimicrobial agents. 1,3,4-oxadiazole derivatives target enoyl reductase (InhA), 14alpha-demethylase in the mycobacterial cell; GlcN-6-P synthase, thymidylate synthase, peptide …
The present review elaborates the therapeutic targets and mode of interaction of 1,3,4-oxadiazoles as antimicrobial agents. 1,3,4-oxadiazole …
Head-to-Head Prenyl Synthases in Pathogenic Bacteria.
Schwalen CJ, Feng X, Liu W, O-Dowd B, Ko TP, Shin CJ, Guo RT, Mitchell DA, Oldfield E. Schwalen CJ, et al. Chembiochem. 2017 Jun 1;18(11):985-991. doi: 10.1002/cbic.201700099. Epub 2017 Apr 25. Chembiochem. 2017. PMID: 28340291 Free PMC article.
Many organisms contain head-to-head isoprenoid synthases; we investigated three such types of enzymes from the pathogens Neisseria meningitidis, Neisseria gonorrhoeae, and Enterococcus hirae. The E. hirae enzyme was found to produce dehydrosqualene, and we solved an inhibi …
Many organisms contain head-to-head isoprenoid synthases; we investigated three such types of enzymes from the pathogens Neisseria meningiti …
A novel carotenoid biosynthetic route via oxidosqualene.
Otani Y, Maoka T, Kawai-Noma S, Saito K, Umeno D. Otani Y, et al. Biochem Biophys Res Commun. 2022 Apr 9;599:75-80. doi: 10.1016/j.bbrc.2022.01.105. Epub 2022 Feb 3. Biochem Biophys Res Commun. 2022. PMID: 35176628
Over 800 known carotenoids are synthesized from phytoene or 4,4'-diapophytoene (dehydrosqualene) characterized by three conjugated double bonds. In this paper, we report that carotenoid desaturase CrtN from Staphylococcus aureus and Methylomonas can accept oxidosqualene, w …
Over 800 known carotenoids are synthesized from phytoene or 4,4'-diapophytoene (dehydrosqualene) characterized by three conjugated do …
Recent insights into antibacterial potential of benzothiazole derivatives.
Kashyap P, Verma S, Gupta P, Narang R, Lal S, Devgun M. Kashyap P, et al. Med Chem Res. 2023 May 29:1-31. doi: 10.1007/s00044-023-03077-z. Online ahead of print. Med Chem Res. 2023. PMID: 37362317 Free PMC article. Review.
Reported data indicated that benzothiazole derivatives displayed antibacterial activity by inhibiting the dihydroorotase, DNA gyrase, uridine diphosphate-n-acetyl enol pyruvyl glucosamine reductase (MurB), peptide deformylase, aldose reductase, casdihydrofolate reductase, enoyl a …
Reported data indicated that benzothiazole derivatives displayed antibacterial activity by inhibiting the dihydroorotase, DNA gyrase, uridin …
Potential antimicrobial agents from triazole-functionalized 2H-benzo[b][1,4]oxazin-3(4H)-ones.
Bollu R, Banu S, Bantu R, Reddy AG, Nagarapu L, Sirisha K, Kumar CG, Gunda SK, Shaik K. Bollu R, et al. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5158-5162. doi: 10.1016/j.bmcl.2017.10.061. Epub 2017 Oct 28. Bioorg Med Chem Lett. 2017. PMID: 29103973
Further, molecular docking studies were accomplished to explore the binding interactions between 1,2,3-triazol-4-yl-2H-benzo[b][1,4]oxazin-3(4H)-one and the active site of Staphylococcus aureus (CrtM) dehydrosqualene synthase (PDB ID: 2ZCS). These docking studies revealed …
Further, molecular docking studies were accomplished to explore the binding interactions between 1,2,3-triazol-4-yl-2H-benzo[b][1,4]oxazin-3 …
The Promiscuity of Squalene Synthase-Like Enzyme: Dehydrosqualene Synthase, a Natural Squalene Hyperproducer?
Guan Z, Song Y, de Vries M, Permentier H, Tepper P, van Merkerk R, Setroikromo R, Quax WJ. Guan Z, et al. J Agric Food Chem. 2024 Feb 14;72(6):3017-3024. doi: 10.1021/acs.jafc.3c05770. Epub 2024 Feb 5. J Agric Food Chem. 2024. PMID: 38315649 Free PMC article.
Dehydrosqualene synthase (CrtM), as a squalene synthase-like enzyme from Staphylococcus aureus, can naturally utilize farnesyl diphosphate to produce dehydrosqualene (C(30)H(48)). ...Here, based on an HPLC-Q-Orbitrap-MS/MS study, we report that the expression of crt …
Dehydrosqualene synthase (CrtM), as a squalene synthase-like enzyme from Staphylococcus aureus, can naturally utilize farnesyl diphos …
Glyceryl trinitrate blocks staphyloxanthin and biofilm formation in Staphylococcus aureus.
Abbas HA, Elsherbini AM, Shaldam MA. Abbas HA, et al. Afr Health Sci. 2019 Mar;19(1):1376-1384. doi: 10.4314/ahs.v19i1.10. Afr Health Sci. 2019. PMID: 31148964 Free PMC article.
Molecular docking study was used to investigate the ability of GTN to bind to dehydrosqualene synthase enzyme. RESULTS: GTN showed a significant inhibition of biofilm, staphyloxanthin and tolerance to oxidative stress. In the molecular docking study, it was found that GTN …
Molecular docking study was used to investigate the ability of GTN to bind to dehydrosqualene synthase enzyme. RESULTS: GTN showed a …
Mechanism of action and inhibition of dehydrosqualene synthase.
Lin FY, Liu CI, Liu YL, Zhang Y, Wang K, Jeng WY, Ko TP, Cao R, Wang AH, Oldfield E. Lin FY, et al. Proc Natl Acad Sci U S A. 2010 Dec 14;107(50):21337-42. doi: 10.1073/pnas.1010907107. Epub 2010 Nov 23. Proc Natl Acad Sci U S A. 2010. PMID: 21098670 Free PMC article.
Here, we report the structures of Staphylococcus aureus dehydrosqualene synthase (CrtM) complexed with its reaction intermediate, presqualene diphosphate (PSPP), the dehydrosqualene (DHS) product, as well as a series of inhibitors. ...
Here, we report the structures of Staphylococcus aureus dehydrosqualene synthase (CrtM) complexed with its reaction intermediate, pre …
Studies with Guanidinium- and Amidinium-Based Inhibitors Suggest Minimal Stabilization of Allylic Carbocation Intermediates by Dehydrosqualene and Squalene Synthases.
Abdelmagid WM, Adak T, Freeman JO, Tanner ME. Abdelmagid WM, et al. Biochemistry. 2018 Sep 25;57(38):5591-5601. doi: 10.1021/acs.biochem.8b00731. Epub 2018 Sep 13. Biochemistry. 2018. PMID: 30179505
Dehydrosqualene and squalene synthases catalyze the redox neutral and the reductive, head-to-head dimerization of farnesyl diphosphate, respectively. ...The positively charged inhibitors acted as competitive inhibitors against Staphylococcus aureus dehydrosqualene s …
Dehydrosqualene and squalene synthases catalyze the redox neutral and the reductive, head-to-head dimerization of farnesyl diphosphat …
Directed evolution of squalene synthase for dehydrosqualene biosynthesis.
Furubayashi M, Li L, Katabami A, Saito K, Umeno D. Furubayashi M, et al. FEBS Lett. 2014 Sep 17;588(18):3375-81. doi: 10.1016/j.febslet.2014.07.028. Epub 2014 Aug 2. FEBS Lett. 2014. PMID: 25093296 Free article.
In this study, SQSs from yeast, human, and bacteria were independently subjected to directed evolution for the production of the C30 carotenoid backbone, dehydrosqualene. This was accomplished via high-throughput screening with Pantoea ananatis phytoene desaturase, which c …
In this study, SQSs from yeast, human, and bacteria were independently subjected to directed evolution for the production of the C30 caroten …
52 results