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TitleA quinolin-8-ol sub-millimolar inhibitor of UGGT, the ER glycoprotein folding quality control checkpoint.
Journal, issue, pagesIscience, Vol. 26, Page 107919-107919, Year 2023
Publish dateApr 12, 2022 (structure data deposition date)
AuthorsGuay, K.P. / Ibba, R. / Kiappes, J.L. / Vasiljevic, S. / Boni, F. / De Benedictis, M. / Zeni, I. / Le Cornu, J.D. / Hensen, M. / Chandran, A.V. ...Guay, K.P. / Ibba, R. / Kiappes, J.L. / Vasiljevic, S. / Boni, F. / De Benedictis, M. / Zeni, I. / Le Cornu, J.D. / Hensen, M. / Chandran, A.V. / Kantsadi, A.L. / Caputo, A.T. / Blanco Capurro, J.I. / Bayo, Y. / Hill, J.C. / Hudson, K. / Lia, A. / Brun, J. / Withers, S.G. / Marti, M. / Biasini, E. / Santino, A. / De Rosa, M. / Milani, M. / Modenutti, C.P. / Hebert, D.N. / Zitzmann, N. / Roversi, P.
External linksIscience / PubMed:37822503
MethodsX-ray diffraction
Resolution1.649 - 2.049 Å
Structure data

PDB-7zkc:
Catalytic domain of UDP-Glucose Glycoprotein Glucosyltransferase from Chaetomium thermophilum (apo form)
Method: X-RAY DIFFRACTION / Resolution: 1.769 Å

PDB-7zll:
Catalytic domain of UDP-Glucose Glycoprotein Glucosyltransferase from Chaetomium thermophilum in complex with the 5-[(morpholin-4-yl)methyl]quinolin-8-ol inhibitor
Method: X-RAY DIFFRACTION / Resolution: 1.649 Å

PDB-7zlu:
Catalytic domain of UDP-Glucose Glycoprotein Glucosyltransferase from Chaetomium thermophilum in complex with UDP-2-deoxy-2-fluoro-D-glucose
Method: X-RAY DIFFRACTION / Resolution: 2.049 Å

Chemicals

ChemComp-CA:
Unknown entry

ChemComp-HOH:
WATER

ChemComp-JM3:
5-(morpholin-4-ylmethyl)quinolin-8-ol

ChemComp-NAG:
2-acetamido-2-deoxy-beta-D-glucopyranose

ChemComp-MAN:
alpha-D-mannopyranose

ChemComp-U2F:
URIDINE-5'-DIPHOSPHATE-2-DEOXY-2-FLUORO-ALPHA-D-GLUCOSE

ChemComp-PDO:
1,3-PROPANDIOL

Source
  • chaetomium thermophilum (fungus)
KeywordsTRANSFERASE / glycoprotein / misfolding / endoplasmic reticulum. UDP-glucose / GT24 / endoplasmic reticulum / 5-[(morpholin-4-yl)methyl]quinolin-8-ol / UDP-2-deoxy-2-fluoro-D-glucose

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