A hybrid polymer to target blood group dependence of cholera toxin

Autor: Haksar, Diksha, Quarles Van Ufford, Linda, Pieters, Roland J., Afd Chemical Biology and Drug Discovery, Chemical Biology and Drug Discovery

Publikováno v: Organic and Biomolecular Chemistry, 18(1), 52. Royal Society of Chemistry

Cholera is a potentially fatal bacterial infection caused by the cholera toxin (CT), an AB5 toxin secreted by Vibrio cholera. GM1 has long been known as the receptor of the cholera toxin in the intestine. However, increasing evidence is pointing towa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5a16619959fad6f46c10cb4f2c3fab63
https://pubmed.ncbi.nlm.nih.gov/31802094

Functional Characterization of Cholera Toxin Inhibitors Using Human Intestinal Organoids

Autor: Zomer-Van Ommen, Domenique D., Pukin, Aliaksei V., Fu, Ou, Quarles Van Ufford, Linda H C, Janssens, Hettie M., Beekman, Jeffrey M., Pieters, Roland J., Medicinal Chemistry and Chemical Biology, Sub Medicinal Chemistry & Chemical biol.

Publikováno v: Journal of Medicinal Chemistry, 59(14), 6968. American Chemical Society : Division of Carbohydrate Chemistry
Journal of Medicinal Chemistry, 59(14), 6968. American Chemical Society
Journal of Medicinal Chemistry, 59(14), 6968-6972. American Chemical Society

Preclinical drug testing in primary human cell models that recapitulate disease can significantly reduce animal experimentation and time-to-the-clinic. We used intestinal organoids to quantitatively study the potency of multivalent cholera toxin inhi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eaa5823b64fe6454b9bd1a7a4a4ab4d9
https://doi.org/10.1021/acs.jmedchem.6b00770

Tetra- versus Pentavalent Inhibitors of Cholera Toxin

Autor: Fu, Ou, Pukin, Aliaksei V., Quarles Van Ufford, Linda, Branson, Thomas R., Thies-Weesie, Dominique M E, Turnbull, W. Bruce, Visser, Gerben M., Pieters, Roland J., Medicinal Chemistry and Chemical Biology, Sub Medicinal Chemistry & Chemical biol., Sub Physical and Colloid Chemistry, Faculty of Veterinary Medicine Research Groups

Publikováno v: ChemistryOpen, 4(4), 471. John Wiley and Sons Inc.
ChemistryOpen

The five B-subunits (CTB5) of the Vibrio cholerae (cholera) toxin can bind to the intestinal cell surface so the entire AB5 toxin can enter the cell. Simultaneous binding can occur on more than one of the monosialotetrahexosylganglioside (GM1) units

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3120590dcf7bfbb56088edac55178c98
https://dspace.library.uu.nl/handle/1874/322956

Orthoester functionalized: N -guanidino derivatives of 1,5-dideoxy-1,5-imino-d-xylitol as pH-responsive inhibitors of β-glucocerebrosidase

Autor: Sevsek, Alen, Sastre Toraño, Javier, Quarles Van Ufford, Linda, Moret, Ed E., Pieters, Roland J., Martin, Nathaniel I., Chemical Biology and Drug Discovery, Afd Chemical Biology and Drug Discovery

Publikováno v: MedChemComm, 8(11), 2050. Royal Society of Chemistry

Alkylated guanidino derivatives of 1,5-dideoxy-1,5-imino-d-xylitol bearing an orthoester moiety were prepared using a concise synthetic protocol. Inhibition assays with a panel of glycosidases revealed that one of the compounds prepared displays pote

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e9adc20892976753402c61402a803820
https://hdl.handle.net/1874/359059

Bicyclic isoureas derived from 1-deoxynojirimycin are potent inhibitors of β-glucocerebrosidase

Autor: Sevšek, Alen, Čelan, Maša, Erjavec, Bibi, Quarles van Ufford, Linda, Sastre Toraño, Javier, Moret, Ed E, Pieters, Roland J, Martin, Nathaniel I, Sub Medicinal Chemistry & Chemical biol., Sub Biomolecular analysis, Medicinal Chemistry and Chemical Biology

Publikováno v: Organic & Biomolecular Chemistry, 14(37), 8670. Royal Society of Chemistry

A series of bicyclic isourea derivatives were prepared from 1-deoxynojirimycin using a concise synthetic protocol proceeding via a guanidino intermediate. Inhibition assays with a panel of glycosidases revealed that these deoxynojirimycin-derived bic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7cd114d9fea84ee30e75f0399eec5d7
https://doi.org/10.1039/c6ob01735e