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TitleStilbene vinyl sulfonamides as fluorogenic sensors of and traceless covalent kinetic stabilizers of transthyretin that prevent amyloidogenesis.
Journal, issue, pagesJ. Am. Chem. Soc., Vol. 135, Page 17869-17880, Year 2013
Publish dateOct 14, 2012 (structure data deposition date)
AuthorsSuh, E.H. / Liu, Y. / Connelly, S. / Genereux, J.C. / Wilson, I.A. / Kelly, J.W.
External linksJ. Am. Chem. Soc. / PubMed:24180271
MethodsX-ray diffraction
Resolution1.22 - 1.45 Å
Structure data

PDB-4hjs:
Kinetic stabilization of transthyretin through covalent modification of K15 by (E)-N-(4-(4-hydroxy-3,5-dimethylstyryl)ethanesulfonamide
Method: X-RAY DIFFRACTION / Resolution: 1.22 Å

PDB-4hjt:
Kinetic stabilization of transthyretin through covalent modification of K15 by (E)-N-(4-(4-hydroxy-3,5-dimethylstyryl)phenyl)propionamide
Method: X-RAY DIFFRACTION / Resolution: 1.45 Å

PDB-4hju:
Transthyretin in complex with (E)-N-(3-(4-hydroxy-3,5-dimethylstyryl)phenyl)acrylamide
Method: X-RAY DIFFRACTION / Resolution: 1.35 Å

Chemicals

ChemComp-18J:
N-{4-[(E)-2-(4-hydroxy-3,5-dimethylphenyl)ethenyl]phenyl}ethanesulfonamide

ChemComp-HOH:
WATER

ChemComp-18A:
N-{4-[(E)-2-(4-hydroxy-3,5-dimethylphenyl)ethenyl]phenyl}propanamide

ChemComp-16L:
N-{3-[(E)-2-(4-hydroxy-3,5-dimethylphenyl)ethenyl]phenyl}prop-2-enamide

Source
  • homo sapiens (human)
KeywordsHORMONE BINDING PROTEIN / Thyroxine / retinol binding protein / HORMONE BINDING PROTEIN/INHIBITOR / HORMONE BINDING PROTEIN-INHIBITOR complex

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