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Fucosyltransferase-specific inhibition via next generation of fucose mimetics.
Martin, Kyle C; Tricomi, Jacopo; Corzana, Francisco; García-García, Ana; Ceballos-Laita, Laura; Hicks, Thomas; Monaco, Serena; Angulo, Jesus; Hurtado-Guerrero, Ramon; Richichi, Barbara; Sackstein, Robert.
Afiliación
  • Martin KC; Department of Translational Medicine, Translational Glycobiology Institute, Herbert Wertheim College of Medicine, Florida International University, Miami, FL 33199, USA. sackstein@fiu.edu and Department of Dermatology, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA and P
  • Tricomi J; Department of Chemistry 'Ugo Schiff', University of Florence, Via della Lastruccia 13, 50019 Sesto Fiorentino, FI, Italy. barbara.richichi@unifi.it.
  • Corzana F; Departamento de Química, Universidad de La Rioja, Centro de Investigación en Síntesis Química, 26006 Logroño, Spain.
  • García-García A; Institute of Biocomputation and Physics of Complex Systems (BIFI), University of Zaragoza, Mariano Esquillor s/n, Campus Rio Ebro, Edificio I + D, Zaragoza, Spain.
  • Ceballos-Laita L; Institute of Biocomputation and Physics of Complex Systems (BIFI), University of Zaragoza, Mariano Esquillor s/n, Campus Rio Ebro, Edificio I + D, Zaragoza, Spain.
  • Hicks T; School of Pharmacy, University of East Anglia, Norwich Research Park, NR47TJ, Norwich, UK.
  • Monaco S; School of Pharmacy, University of East Anglia, Norwich Research Park, NR47TJ, Norwich, UK.
  • Angulo J; School of Pharmacy, University of East Anglia, Norwich Research Park, NR47TJ, Norwich, UK and Departamento de Química Orgánica, Universidad de Sevilla, C/Prof. García González, 1, 41012 Sevilla, Spain and Instituto de Investigaciones Químicas (CSIC-US), Avda. Américo Vespucio, 49, 41092 Sevilla, Spa
  • Hurtado-Guerrero R; Institute of Biocomputation and Physics of Complex Systems (BIFI), University of Zaragoza, Mariano Esquillor s/n, Campus Rio Ebro, Edificio I + D, Zaragoza, Spain and Fundación ARAID, 50018, Zaragoza, Spain and Copenhagen Center for Glycomics, Department of Cellular and Molecular Medicine, School of
  • Richichi B; Department of Chemistry 'Ugo Schiff', University of Florence, Via della Lastruccia 13, 50019 Sesto Fiorentino, FI, Italy. barbara.richichi@unifi.it.
  • Sackstein R; Department of Translational Medicine, Translational Glycobiology Institute, Herbert Wertheim College of Medicine, Florida International University, Miami, FL 33199, USA. sackstein@fiu.edu and Department of Dermatology, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA and P
Chem Commun (Camb) ; 57(9): 1145-1148, 2021 Jan 28.
Article en En | MEDLINE | ID: mdl-33411866
ABSTRACT
The ability to custom-modify cell surface glycans holds great promise for treatment of a variety of diseases. We propose a glycomimetic of l-fucose that markedly inhibits the creation of sLeX by FTVI and FTVII, but has no effect on creation of LeX by FTIX. Our findings thus indicate that selective suppression of sLex display can be achieved, and STD-NMR studies surprisingly reveal that the mimetic does not compete with GDP-fucose at the enzymatic binding site.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Fucosa / Fucosiltransferasas Límite: Humans Idioma: En Revista: Chem Commun (Camb) Asunto de la revista: QUIMICA Año: 2021 Tipo del documento: Article
Texto completo
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Fucosa / Fucosiltransferasas Límite: Humans Idioma: En Revista: Chem Commun (Camb) Asunto de la revista: QUIMICA Año: 2021 Tipo del documento: Article