Page last updated: 2024-08-05 15:41:19

EC 2.5.1.59 (protein geranylgeranyltransferase type I) inhibitor

An EC 2.5.1.* (non-methyl-alkyl or aryl transferase) inhibitor that interferes with the action of protein geranylgeranyltransferase type I (EC 2.5.1.59).

ChEBI ID: 67267

Members (4)

MemberDefinitionClass
ggti-2133An organoammonium salt resulting from the mixing of equimolar amounts of GGTI-2133 free base and trifluoroacetic acid. An inhibitor of geranylgeranyltransferase type I.GGTI-2133
l 778,123The hydrochloride salt of L-778,123. It is a dual inhibitor of FPTase and GGPTase-I (IC50 of 2nM and 98nm, respectively) and exhibits anti-cancer properties.L-778,123 hydrochloride
l 778,123A member of the class of imidazoles that is 1H-imidazole substituted by (4-cyanophenyl)methyl and [4-(3-chlorophenyl)-3-oxopiperazin-1-yl]methyl groups at positions 1 and 5, respectively. It is a dual inhibitor of FPTase and GGPTase-I.L-778,123 (free base)
massadineAn alkaloid isolated from Stylissa massa.massadine

Research

Studies (61)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's34 (55.74)29.6817
2010's23 (37.70)24.3611
2020's4 (6.56)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials3 (4.76%)5.53%
Reviews12 (19.05%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other48 (76.19%)84.16%

Protein Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Interferon betaHomo sapiens (human)Potency16.538813
PPM1D proteinHomo sapiens (human)Potency16.538812

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Chain A, Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunitHomo sapiens (human)Ki0.002412
Chain A, Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunitRattus norvegicus (Norway rat)Ki0.002412
Chain B, Geranylgeranyl transferase type I beta subunitRattus norvegicus (Norway rat)Ki0.002412
Chain B, Protein farnesyltransferase beta subunitHomo sapiens (human)Ki0.002412
Geranylgeranyl transferase type-1 subunit betaHomo sapiens (human)IC5024.573844
GTPase HRasHomo sapiens (human)Ki0.001611
GTPase NRasHomo sapiens (human)Ki0.000311
Protein farnesyltransferase subunit betaBos taurus (cattle)IC500.048522
Protein farnesyltransferase subunit betaHomo sapiens (human)IC500.40201010
Protein farnesyltransferase subunit betaRattus norvegicus (Norway rat)IC500.003611
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaBos taurus (cattle)IC500.048522
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)IC507.30821414
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaRattus norvegicus (Norway rat)IC500.003611

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Geranylgeranyl transferase type-1 subunit betaHomo sapiens (human)EC503.446022
Protein farnesyltransferase subunit betaHomo sapiens (human)EC500.092011
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)EC503.446022

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Geranylgeranyl transferase type-1 subunit betaHomo sapiens (human)Inhibition0.098011
Geranylgeranyl transferase type-1 subunit betaHomo sapiens (human)MIC1.000022
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)Inhibition0.098011
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)MIC1.000022