Page last updated: 2024-12-10

ggti 286

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Description

GGTI 286: the methyl ester of GGTI-287; inhibits geranylgeranyltransferase [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3012117
CHEMBL ID28325
SCHEMBL ID1802360
MeSH IDM0402147

Synonyms (14)

Synonym
bdbm50076142
(s)-2-{[5-((r)-2-amino-3-mercapto-propylamino)-biphenyl-2-carbonyl]-amino}-4-methyl-pentanoic acid methyl ester
ggti 286
CHEMBL28325 ,
methyl (2s)-2-[[4-[[(2r)-2-amino-3-sulfanylpropyl]amino]-2-phenylbenzoyl]amino]-4-methylpentanoate
SCHEMBL1802360
171744-11-9
J-010750
methyl (5-(((r)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-carbonyl)-l-leucinate
HY-115489
EX-A6002
n-4-[2(r)-amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(l)-leucine methyl ester
CS-0087163
PD061095
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)IC50 (µMol)8.00610.00050.471610.0000AID1371364; AID1371365; AID72813; AID74648
Protein farnesyltransferase subunit betaHomo sapiens (human)IC50 (µMol)15.00850.00050.21772.5000AID1371365; AID72813
Geranylgeranyl transferase type-1 subunit betaHomo sapiens (human)IC50 (µMol)1.00370.00732.364210.0000AID1371364; AID74648
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (9)

Processvia Protein(s)Taxonomy
transforming growth factor beta receptor signaling pathwayProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
protein farnesylationProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
protein geranylgeranylationProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
positive regulation of Rac protein signal transductionProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
skeletal muscle acetylcholine-gated channel clusteringProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
positive regulation of tubulin deacetylationProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
positive regulation of deacetylase activityProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
positive regulation of skeletal muscle acetylcholine-gated channel clusteringProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
lipid metabolic processProtein farnesyltransferase subunit betaHomo sapiens (human)
protein farnesylationProtein farnesyltransferase subunit betaHomo sapiens (human)
protein geranylgeranylationGeranylgeranyl transferase type-1 subunit betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
protein farnesyltransferase activityProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
protein farnesyltransferase activityProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
protein geranylgeranyltransferase activityProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
Rab geranylgeranyltransferase activityProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
protein bindingProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
microtubule bindingProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
receptor tyrosine kinase bindingProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
alpha-tubulin bindingProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
molecular adaptor activityProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
CAAX-protein geranylgeranyltransferase activityProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
protein farnesyltransferase activityProtein farnesyltransferase subunit betaHomo sapiens (human)
protein farnesyltransferase activityProtein farnesyltransferase subunit betaHomo sapiens (human)
protein bindingProtein farnesyltransferase subunit betaHomo sapiens (human)
zinc ion bindingProtein farnesyltransferase subunit betaHomo sapiens (human)
protein geranylgeranyltransferase activityGeranylgeranyl transferase type-1 subunit betaHomo sapiens (human)
CAAX-protein geranylgeranyltransferase activityGeranylgeranyl transferase type-1 subunit betaHomo sapiens (human)
protein bindingGeranylgeranyl transferase type-1 subunit betaHomo sapiens (human)
zinc ion bindingGeranylgeranyl transferase type-1 subunit betaHomo sapiens (human)
CAAX-protein geranylgeranyltransferase activityGeranylgeranyl transferase type-1 subunit betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
cytosolProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
plasma membraneProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
CAAX-protein geranylgeranyltransferase complexProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
microtubule associated complexProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
protein farnesyltransferase complexProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
cytoplasmProtein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)
cytosolProtein farnesyltransferase subunit betaHomo sapiens (human)
microtubule associated complexProtein farnesyltransferase subunit betaHomo sapiens (human)
protein farnesyltransferase complexProtein farnesyltransferase subunit betaHomo sapiens (human)
CAAX-protein geranylgeranyltransferase complexGeranylgeranyl transferase type-1 subunit betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID74648In vitro inhibition of [3H]GGPP incorporation into H-Ras-CVLL by Geranylgeranyl transferase type I1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.
AID72813In vitro inhibition of [3H]FPP incorporation into H-Ras-CVLS by Farnesyl transferase1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.
AID1371364Inhibition of GGTase1 (unknown origin) expressed in mouse NIH-3T3 cells transfected with k-Ras4B assessed as decrease in geranylgeranylation of k-Ras4B after 24 hrs by chemoluminescence assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.
AID1371365Inhibition of FTase (unknown origin) expressed in mouse NIH-3T3 cells cells transfected with human H-Ras assessed as decrease in farnesylation of H-Ras after 24 hrs by chemoluminescence assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.
AID233818Relative selectivity farnesyl (Ha-ras-CVLS) and geranylgeranyl (Ha-ras-CVLL) transferases as ratio of IC50s1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (25)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (4.00)18.2507
2000's17 (68.00)29.6817
2010's7 (28.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other24 (96.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]