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Showing results for laman polakova
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1,4-Dideoxy-1,4-imino-D- and L-lyxitol-based inhibitors bind to Golgi alpha-mannosidase II in different protonation forms.
Kóňa J, Šesták S, Wilson IBH, Poláková M. Kóňa J, et al. Org Biomol Chem. 2022 Nov 23;20(45):8932-8943. doi: 10.1039/d2ob01545e. Org Biomol Chem. 2022. PMID: 36322142 Free PMC article.
The development of effective inhibitors of Golgi alpha-mannosidase II (GMII, E.C.3.2.1.114) with minimal off-target effects on phylogenetically-related lysosomal alpha-mannosidase (LMan, E.C.3.2.1.24) is a complex task due to the complicated structural …
The development of effective inhibitors of Golgi alpha-mannosidase II (GMII, E.C.3.2.1.114) with minimal off-target effects on …
Synthesis, alpha-mannosidase inhibition studies and molecular modeling of 1,4-imino-D-lyxitols and their C-5-altered N-arylalkyl derivatives.
Kalník M, Šesták S, Kóňa J, Bella M, Poláková M. Kalník M, et al. Beilstein J Org Chem. 2023 Mar 6;19:282-293. doi: 10.3762/bjoc.19.24. eCollection 2023. Beilstein J Org Chem. 2023. PMID: 36925565 Free PMC article.
Their inhibitory activity and selectivity toward four GH38 alpha-mannosidases (two Golgi types: GMIIb from Drosophila melanogaster and AMAN-2 from Caenorhabditis elegans, and two lysosomal types: LManII from Drosophila melanogaster and JBMan from Canavalia ensiformis) were invest …
Their inhibitory activity and selectivity toward four GH38 alpha-mannosidases (two Golgi types: GMIIb from Drosophila melanogaster and AMAN- …
N-Benzyl Substitution of Polyhydroxypyrrolidines: The Way to Selective Inhibitors of Golgi alpha-Mannosidase II.
Šesták S, Bella M, Klunda T, Gurská S, Džubák P, Wöls F, Wilson IBH, Sladek V, Hajdúch M, Poláková M, Kóňa J. Šesták S, et al. ChemMedChem. 2018 Feb 20;13(4):373-383. doi: 10.1002/cmdc.201700607. Epub 2018 Feb 6. ChemMedChem. 2018. PMID: 29323461 Free PMC article.
Inhibition of the biosynthesis of complex N-glycans in the Golgi apparatus influences progress of tumor growth and metastasis. Golgi alpha-mannosidase II (GMII) has become a therapeutic target for drugs with anticancer activities. One critical task for successful ap …
Inhibition of the biosynthesis of complex N-glycans in the Golgi apparatus influences progress of tumor growth and metastasis. Golgi alph …
Synthesis of modified D-mannose core derivatives and their impact on GH38 α-mannosidases.
Poláková M, Horák R, Šesták S, Holková I. Poláková M, et al. Carbohydr Res. 2016 Jun 16;428:62-71. doi: 10.1016/j.carres.2016.04.004. Epub 2016 Apr 11. Carbohydr Res. 2016. PMID: 27152630
Moreover, it was found that another GH38 enzyme, commercial jack bean alpha-mannosidase, was inhibited by triazole conjugates regardless of the carbohydrate core while the corresponding sulfones were inactive....
Moreover, it was found that another GH38 enzyme, commercial jack bean alpha-mannosidase, was inhibited by triazole conjugates …
Synthesis of 1,4-imino-L-lyxitols modified at C-5 and their evaluation as inhibitors of GH38 α-mannosidases.
Bella M, Šesták S, Moncoľ J, Koóš M, Poláková M. Bella M, et al. Beilstein J Org Chem. 2018 Aug 17;14:2156-2162. doi: 10.3762/bjoc.14.189. eCollection 2018. Beilstein J Org Chem. 2018. PMID: 30202468 Free PMC article.
An impact of the C-5 modification on the inhibition and selectivity against GH38 alpha-mannosidases from Drosophila melanogaster, the Golgi (GMIIb) and lysosomal (LManII) mannosidases and commercial jack bean alpha-mannosidase from Canavalia ensiformis was evaluated …
An impact of the C-5 modification on the inhibition and selectivity against GH38 alpha-mannosidases from Drosophila melanogaster, the Golgi …
alpha-D-mannose derivatives as models designed for selective inhibition of Golgi alpha-mannosidase II.
Poláková M, Šesták S, Lattová E, Petruš L, Mucha J, Tvaroška I, Kóňa J. Poláková M, et al. Eur J Med Chem. 2011 Mar;46(3):944-52. doi: 10.1016/j.ejmech.2011.01.012. Epub 2011 Jan 15. Eur J Med Chem. 2011. PMID: 21295890
Human Golgi alpha-mannosidase II (hGM) is a pharmaceutical target for the design of inhibitors with anti-tumor activity. Nanomolar inhibitors of hGM exhibit unwanted co-inhibition of the human lysosomal alpha-mannosidase (hLM). Hence, improving specifi …
Human Golgi alpha-mannosidase II (hGM) is a pharmaceutical target for the design of inhibitors with anti-tumor activity. Nanom …
'Click chemistry' synthesis of 1-(α-D-mannopyranosyl)-1,2,3-triazoles for inhibition of α-mannosidases.
Poláková M, Stanton R, Wilson IB, Holková I, Šesták S, Machová E, Jandová Z, Kóňa J. Poláková M, et al. Carbohydr Res. 2015 Apr 10;406:34-40. doi: 10.1016/j.carres.2015.01.004. Epub 2015 Jan 19. Carbohydr Res. 2015. PMID: 25658064 Free PMC article.
Three new triazole conjugates derived from d-mannose were synthesized and assayed in in vitro assays to investigate their ability to inhibit alpha-mannosidase enzymes from the glycoside hydrolase (GH) families 38 and 47. The triazole conjugates were more selective f …
Three new triazole conjugates derived from d-mannose were synthesized and assayed in in vitro assays to investigate their ability to inhibit …