Literature summary for 2.5.1.58 extracted from

Clark, M.K.; Scott, S.A.; Wojtkowiak, J.; Chirco, R.; Mathieu, P.; Reiners, J.J.; Mattingly, R.R.; Borch, R.F.; Gibbs, R.A.
Synthesis, biochemical, and cellular evaluation of farnesyl monophosphate prodrugs as farnesyltransferase inhibitors (2007), J. Med. Chem., 50, 3274-3282.

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Inhibitors

Inhibitors	Comment	Organism	Structure
(2Z,6E)-3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2,6,10-triene monophosphate	IC50: 16 nM	Homo sapiens
(2Z,6E)-3-allyl-7,11-dimethyldodeca-2,6,10-trien-1-yl 5-nitrofurfuryl N-methyl-N-(4-chlorobutyl)phosphoramidate	-	Homo sapiens
(2Z,6E)-3-allyl-7,11-dimethyldodeca-2,6,10-triene monophosphate	-	Homo sapiens
(2Z,6E)-3-tert-butyl-7,11-dimethyldodeca-2,6,10-trien-1-yl 5-nitrofurfuryl N-methyl-N-(4-chlorobutyl)phosphoramidate	-	Homo sapiens
(2Z,6E)-3-tert-butyl-7,11-dimethyldodeca-2,6,10-triene monophosphate	IC50: 13 nM	Homo sapiens
(2Z,6E,10E)-3-(3-methyl-1-but-2-enyl)-7,11-dimethyldodeca-2,6,10-trien-1-yl 5-nitrofurfuryl N-methyl-N-(4-chlorobutyl)phosphoramidate	-	Homo sapiens
3-allylfarnesol	potent inhibitor	Homo sapiens
3-allylfarnesyl diphosphate	IC50: 189 nM	Homo sapiens
3-tert-butylfarnesyl diphosphate	IC50: 31 nM	Homo sapiens
R-115777	-	Homo sapiens
SCH66336	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
Schwann cell line	-	Homo sapiens	-
STS-26T cell	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
farnesyl diphosphate + protein-cysteine	-	Homo sapiens	diphosphate + S-farnesyl protein	-	?

Synonyms

Synonyms	Comment	Organism
FTase	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000013	-	IC50: 13 nM	Homo sapiens	(2Z,6E)-3-tert-butyl-7,11-dimethyldodeca-2,6,10-triene monophosphate
0.000016	-	IC50: 16 nM	Homo sapiens	(2Z,6E)-3-(3-methylbut-2-enyl)-7,11-dimethyldodeca-2,6,10-triene monophosphate
0.000031	-	IC50: 31 nM	Homo sapiens	3-tert-butylfarnesyl diphosphate
0.000189	-	IC50: 189 nM	Homo sapiens	3-allylfarnesyl diphosphate

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Release 2023.1 (January 2023)