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Literature summary for 2.5.1.29 extracted from

  • Zhou, X.; Ferree, S.D.; Wills, V.S.; Born, E.J.; Tong, H.; Wiemer, D.F.; Holstein, S.A.
    Geranyl and neryl triazole bisphosphonates as inhibitors of geranylgeranyl diphosphate synthase (2014), Bioorg. Med. Chem., 22, 2791-2798.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.5.1.29

Inhibitors

Inhibitors Comment Organism Structure
(2-[1-[(2E)-3,7-dimethylocta-2,6-dien-1-yl]-1H-1,2,3-triazol-4-yl]ethane-1,1-diyl)bis(phosphonic acid) a mixture of olefin isomers Homo sapiens
(E)-(2-(1-((3-methyl-3-(4-methylpent-3-en-1-yl)oxiran-2-yl)methyl)-1H-1,2,3-triazol-4-yl)ethane-1,1-diyl)bis(phosphonate)
-
 Homo sapiens
(E)-(2-(1-(3,7-dimethylocta-2,6-dien-1-yl)-1H-1,2,3-triazol-4-yl)ethane-1,1-diyl)bis(phosphonate)
-
 Homo sapiens
(Z)-(2-(1-((3-methyl-3-(4-methylpent-3-en-1-yl)oxiran-2-yl)methyl)-1H-1,2,3-triazol-4-yl)ethane-1,1-diyl)bis(phosphonate)digeranyl bisphosphonate cell treatment with inhibitor DGBP results in the accumulation of unmodified Rap1a and Rab6 Homo sapiens
(Z)-(2-(1-(3,7-dimethylocta-2,6-dien-1-yl)-1H-1,2,3-triazol-4-yl)ethane-1,1-diyl)bis(phosphonate)
-
 Homo sapiens
additional information evaluation of geranyl and neryl triazole bisphosphonates as inhibitors of geranylgeranyl diphosphate synthase, overview. Stereoselective synthesis of these triazoles through the use of epoxy azides for the cycloaddition reaction followed by regeneration of the desired olefin, a Z-olefin isomer is a potent and selective inhibitor of geranylgeranyl diphosphate synthase Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
(2E,6E)-farnesyl diphosphate + isopentenyl diphosphate Homo sapiens
-
 diphosphate + geranylgeranyl diphosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
myeloma cell
-
 Homo sapiens
-
RPMI-8226 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(2E,6E)-farnesyl diphosphate + isopentenyl diphosphate
-
 Homo sapiens diphosphate + geranylgeranyl diphosphate
-
 ?

Synonyms

Synonyms Comment Organism
GGDPS
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
 assay at room temperature Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.7
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00038
-
 pH 7.7, 22°C Homo sapiens (Z)-(2-(1-(3,7-dimethylocta-2,6-dien-1-yl)-1H-1,2,3-triazol-4-yl)ethane-1,1-diyl)bis(phosphonate)
0.0022
-
 pH 7.7, 22°C Homo sapiens (2-[1-[(2E)-3,7-dimethylocta-2,6-dien-1-yl]-1H-1,2,3-triazol-4-yl]ethane-1,1-diyl)bis(phosphonic acid)
0.017
-
 pH 7.7, 22°C Homo sapiens (E)-(2-(1-(3,7-dimethylocta-2,6-dien-1-yl)-1H-1,2,3-triazol-4-yl)ethane-1,1-diyl)bis(phosphonate)
0.017
-
 pH 7.7, 22°C Homo sapiens (Z)-(2-(1-((3-methyl-3-(4-methylpent-3-en-1-yl)oxiran-2-yl)methyl)-1H-1,2,3-triazol-4-yl)ethane-1,1-diyl)bis(phosphonate)digeranyl bisphosphonate
0.023
-
 pH 7.7, 22°C Homo sapiens (E)-(2-(1-((3-methyl-3-(4-methylpent-3-en-1-yl)oxiran-2-yl)methyl)-1H-1,2,3-triazol-4-yl)ethane-1,1-diyl)bis(phosphonate)