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Literature summary 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)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.59 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
2.5.1.59 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)

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

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.59 Homo sapiens
-
-
-
2.5.1.59 Sus scrofa
-
-
-

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.5.1.59 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