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Literature summary for 2.5.1.59 extracted from

  • Rao, P.V.; Peterson, Y.K.; Inoue, T.; Casey, P.J.
    Effects of pharmacologic inhibition of protein geranylgeranyltransferase type I on aqueous humor outflow through the trabecular meshwork (2008), Invest. Ophthalmol. Vis. Sci., 49, 2464-2471.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
PCR-amplification of human enzyme for RT-PCR analysis of expression in human trabecular mesh cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
GGTI-DU40 1-40 microM dissolved in dimethyl sulfoxide, affects actin cytoskeletal integrity, cell adhesion, cell-cell junctions, myosin II phosphorylation, and membrane localization of GTP-binding proteins in trabecular meshwork cells is tested using immunofluorescence detection and immunoblotting analysis and the effect on aqueous humor outflow Homo sapiens
GGTI-DU40 5-40 microM dissolved in dimethyl sulfoxide influence cell morphology in a dose and time dependent manner, affects actin cytoskeletal integrity, cell adhesion, cell-cell junctions, myosin II phosphorylation, and membrane localization of GTP-binding proteins in trabecular meshwork cells is tested using immunofluorescence detection and immunoblotting analysis and the effect on aqueous humor outflow (25 and 40 microM) Sus scrofa

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
geranylgeranyl diphosphate + Ras protein Homo sapiens
-
S-geranylgeranyl-Ras protein + diphosphate
-
?
geranylgeranyl diphosphate + Ras protein Sus scrofa
-
S-geranylgeranyl-Ras protein + diphosphate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Sus scrofa
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
eye human trabecular meshwork cells, lysate for activity assay Homo sapiens
-
eye porcine trabecular meshwork cells, freshly isolated, and organ culture Sus scrofa
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
geranylgeranyl diphosphate + Ras protein
-
Homo sapiens S-geranylgeranyl-Ras protein + diphosphate
-
?
geranylgeranyl diphosphate + Ras protein
-
Sus scrofa S-geranylgeranyl-Ras protein + diphosphate
-
?

Synonyms

Synonyms Comment Organism
GGTase-I
-
Homo sapiens
GGTase-I
-
Sus scrofa
protein geranylgeranyltransferase type I
-
Homo sapiens
protein geranylgeranyltransferase type I
-
Sus scrofa

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00007
-
complete inhibition at 5 microM, tritium-labelled geranylgeranyl diphosphate for activity assay with lysate of trabecular mesh cells, 30°C Sus scrofa GGTI-DU40