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Literature summary for 2.5.1.29 extracted from

  • Wiemer, A.J.; Yu, J.S.; Lamb, K.M.; Hohl, R.J.; Wiemer, D.F.
    Mono- and dialkyl isoprenoid bisphosphonates as geranylgeranyl diphosphate synthase inhibitors (2008), Bioorg. Med. Chem., 16, 390-399.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in BL21 gold bacteria Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2E,6E)-farnesyl-bis(phosphonic acid) both inhibition of in vitro reaction as well as of cellular geranylgeranylation Homo sapiens
(2E,6E)-farnesyl-geranyl-bis(phosphonic acid) both inhibition of in vitro reaction as well as of cellular geranylgeranylation Homo sapiens
(2E,6Z)-farnesyl-bis(phosphonic acid) both inhibition of in vitro reaction as well as of cellular geranylgeranylation Homo sapiens
(3E,7Z)-4,8,12-trimethyl-1-phosphonitotrideca-3,7,11-trienylphosphonate
-
Homo sapiens
(3Z,7E)-4,8,12-trimethyl-1-phosphonitotrideca-3,7,11-trienylphosphonate
-
Homo sapiens
(3Z,7Z)-4,8,12-trimethyl-1-phosphonitotrideca-3,7,11-trienylphosphonate
-
Homo sapiens
(6Z,11E)-2,6,12,16-tetramethylheptadeca-2,6,11,15-tetraene-9,9-diyldiphosphonate
-
Homo sapiens
(6Z,11Z)-2,6,12,16-tetramethylheptadeca-2,6,11,15-tetraene-9,9-diyldiphosphonate
-
Homo sapiens
(Z)-2,8,12-trimethyltrideca-2,7,11-triene-5,5-diyldiphosphonate
-
Homo sapiens
bis[(6E)-2,6-dimethylnona-2,6-diene-9,9-diyl]bis(phosphonic acid) both inhibition of in vitro reaction as well as of cellular geranylgeranylation Homo sapiens
digeranyl bisphosphonate
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Homo sapiens
-
recombinant
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
trans,trans-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
0.0001
-
pH 7.5, 37°C Homo sapiens (2E,6E)-farnesyl-bis(phosphonic acid)
0.0002
-
-
Homo sapiens digeranyl bisphosphonate
0.0002
-
pH 7.5, 37°C Homo sapiens bis[(6E)-2,6-dimethylnona-2,6-diene-9,9-diyl]bis(phosphonic acid)
0.0003
-
pH 7.5, 37°C Homo sapiens (2E,6E)-farnesyl-geranyl-bis(phosphonic acid)
0.0006
-
-
Homo sapiens (3E,7Z)-4,8,12-trimethyl-1-phosphonitotrideca-3,7,11-trienylphosphonate
0.0006
-
pH 7.5, 37°C Homo sapiens (2E,6Z)-farnesyl-bis(phosphonic acid)
0.003
-
-
Homo sapiens (6Z,11Z)-2,6,12,16-tetramethylheptadeca-2,6,11,15-tetraene-9,9-diyldiphosphonate
0.006
-
-
Homo sapiens (6Z,11E)-2,6,12,16-tetramethylheptadeca-2,6,11,15-tetraene-9,9-diyldiphosphonate
0.007
-
-
Homo sapiens (Z)-2,8,12-trimethyltrideca-2,7,11-triene-5,5-diyldiphosphonate
0.04
-
-
Homo sapiens (3Z,7E)-4,8,12-trimethyl-1-phosphonitotrideca-3,7,11-trienylphosphonate
0.07
-
-
Homo sapiens (3Z,7Z)-4,8,12-trimethyl-1-phosphonitotrideca-3,7,11-trienylphosphonate