Literature summary for 2.5.1.20 extracted from

Mau, C.J.; Garneau, S.; Scholte, A.A.; Van Fleet, J.E.; Vederas, J.C.; Cornish, K.
Protein farnesyltransferase inhibitors interfere with farnesyl diphosphate binding by rubber transferase (2003), Eur. J. Biochem., 270, 3939-3945.

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Inhibitors

Inhibitors	Comment	Organism	Structure
(Z)-2-farnesyl-3-methylbutenedioic acid dilithium salt	i.e. SG-129, 25% inhibition at 0.18 mM, noncompetitive	Hevea brasiliensis
(Z)-2-farnesyl-3-methylbutenedioic acid dilithium salt	i.e. SG-129, 27-48% inhibition at 0.18 mM, competitive	Parthenium argentatum
(Z)-2-octyl-3-methylbutenedioic acid dilithium salt	i.e. SG-296, 40% inhibition at 0.18 mM	Hevea brasiliensis
alpha-hydroxyfarnesylphosphonic acid	i.e. HFPA, competitive	Hevea brasiliensis
alpha-hydroxyfarnesylphosphonic acid	i.e. HFPA, competitive	Parthenium argentatum
chaetomellic acid	inhibitory in 20fold molar excess over isopentenyl diphosphate or 200fold molar excess over farnesyl diphosphate, competitive	Hevea brasiliensis
chaetomellic acid	27-48% inhibition at 0.18 mM, competitive	Parthenium argentatum
additional information	not inhibitory: (Z)-2-octyl-3-methylbutenedioic acid dilithium salt	Parthenium argentatum

Organism

Organism	UniProt	Comment	Textmining
Hevea brasiliensis	-	-	-
Parthenium argentatum	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
isopentenyl diphosphate + farnesyl diphosphate	-	Hevea brasiliensis	diphosphate + ?	-	?
isopentenyl diphosphate + farnesyl diphosphate	-	Parthenium argentatum	diphosphate + ?	-	?

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.0088	-	chaetomellic acid	pH 7.5, 25°C	Parthenium argentatum
0.025	-	(Z)-2-farnesyl-3-methylbutenedioic acid dilithium salt	pH 7.5, 25°C	Parthenium argentatum
0.042	-	chaetomellic acid	pH 7.5, 25°C	Hevea brasiliensis
0.064	-	alpha-hydroxyfarnesylphosphonic acid	pH 7.5, 25°C	Hevea brasiliensis
0.14	-	(Z)-2-farnesyl-3-methylbutenedioic acid dilithium salt	pH 7.5, 25°C	Hevea brasiliensis
0.42	-	alpha-hydroxyfarnesylphosphonic acid	pH 7.5, 25°C	Parthenium argentatum

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Release 2023.1 (January 2023)