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Literature summary for 2.5.1.29 extracted from

  • Wills, V.S.; Allen, C.; Holstein, S.A.; Wiemer, D.F.
    Potent triazole bisphosphonate inhibitor of geranylgeranyl diphosphate synthase (2015), ACS Med. Chem. Lett., 6, 1195-1198.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.5.1.29

Inhibitors

Inhibitors Comment Organism Structure
(2-[1-[(3E)-4,8-dimethylnona-3,7-dien-1-yl]-1H-1,2,3-triazol-4-yl]ethane-1,1-diyl)bis(phosphonic acid) identification of a potent triazole bisphosphonate inhibitor of geranylgeranyl diphosphate synthase with very good selectivity for this enzyme over farnesyl diphosphate synthase. This compound also potently disrupts geranylgeranylation and induces cytotoxicity in human myeloma cells at submicromolar levels, suggesting that it may serve as a lead compound for treatment of malignancies characterized by excessive protein secretion Homo sapiens
pamidronate
-
 Homo sapiens
risedronate
-
 Homo sapiens
zoledronate
-
 Homo sapiens
[(6E)-2,6-dimethyl-10-[1-(4-methylpent-3-en-1-yl)-1H-1,2,3-triazol-4-yl]deca-2,6-diene-9,9-diyl]bis(phosphonic acid)
-
 Homo sapiens
[2-[1-(4-methylpent-3-en-1-yl)-1H-1,2,3-triazol-4-yl]ethane-1,1-diyl]bis(phosphonic acid)
-
 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 O95749
-
-

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000045
-
 pH and temperature not specified in the publication Homo sapiens (2-[1-[(3E)-4,8-dimethylnona-3,7-dien-1-yl]-1H-1,2,3-triazol-4-yl]ethane-1,1-diyl)bis(phosphonic acid)
0.00038
-
 pH and temperature not specified in the publication Homo sapiens [(6E)-2,6-dimethyl-10-[1-(4-methylpent-3-en-1-yl)-1H-1,2,3-triazol-4-yl]deca-2,6-diene-9,9-diyl]bis(phosphonic acid)
0.00043
-
 pH and temperature not specified in the publication Homo sapiens [2-[1-(4-methylpent-3-en-1-yl)-1H-1,2,3-triazol-4-yl]ethane-1,1-diyl]bis(phosphonic acid)