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Literature summary for 2.7.7.48 extracted from

  • Mastrangelo, E.; Pezzullo, M.; Tarantino, D.; Petazzi, R.; Germani, F.; Kramer, D.; Robel, I.; Rohayem, J.; Bolognesi, M.; Milani, M.
    Structure-based inhibition of norovirus RNA-dependent RNA polymerases (2012), J. Mol. Biol., 419, 198-210.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
in-silico docking search of inhibitors. The location of inhibitors 8,8'-[carbonylbis(iminobenzene-3,1-diylcarbonylimino)]dinaphthalene-1,3,5-trisulfonic acid and Suramin inner head is stabilized by offset-tilted aromatic/aromatic interaction with residue Trp41 norovirus
in-silico docking search of inhibitors. The location of inhibitors 8,8'-[carbonylbis(iminobenzene-3,1-diylcarbonylimino)]dinaphthalene-1,3,5-trisulfonic acid and Suramin inner head is stabilized by offset-tilted aromatic/aromatic interaction with residue Trp42 Murine norovirus

Protein Variants

Protein Variants Comment Organism
Y41A mutation in inhibitor-binding site, about 5fold increase in IC50 values for inhibitors suramin and 8,8'-[carbonylbis(iminobenzene-3,1-diylcarbonylimino)]dinaphthalene-1,3,5-trisulfonic acid norovirus

Inhibitors

Inhibitors Comment Organism Structure
8,8'-[carbonylbis(iminobenzene-3,1-diylcarbonylimino)]dinaphthalene-1,3,5-trisulfonic acid
-
Murine norovirus
8,8'-[carbonylbis(iminobenzene-3,1-diylcarbonylimino)]dinaphthalene-1,3,5-trisulfonic acid
-
norovirus
suramin
-
Murine norovirus
suramin
-
norovirus

Organism

Organism UniProt Comment Textmining
Murine norovirus
-
-
-
norovirus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
GTP + poly(C) use of poly(C) as template annealed with oligoG12 as primer norovirus diphosphate + ?
-
?
GTP + poly(C) use of poly(C) as template annealed with oligoG12 as primer Murine norovirus diphosphate + ?
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000246
-
wild-type, pH 7.5, 30°C norovirus suramin
0.00007
-
wild-type, pH 7.5, 30°C Murine norovirus suramin
0.0000715
-
wild-type, pH 7.5, 30°C norovirus 8,8'-[carbonylbis(iminobenzene-3,1-diylcarbonylimino)]dinaphthalene-1,3,5-trisulfonic acid
0.00014
-
mutant Y41A, pH 7.5, 30°C norovirus suramin
0.0002
-
mutant Y41A, pH 7.5, 30°C Murine norovirus suramin
0.00028
-
mutant Y41A, pH 7.5, 30°C norovirus 8,8'-[carbonylbis(iminobenzene-3,1-diylcarbonylimino)]dinaphthalene-1,3,5-trisulfonic acid