Page last updated: 2024-11-11

ggti 298

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Description

GGTI 298: inhibits geranylgeranyltransferase-I; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9811606
CHEMBL ID282748
CHEBI ID124997
SCHEMBL ID4283635
MeSH IDM0268390

Synonyms (32)

Synonym
bdbm50076138
2-[4-((r)-2-amino-3-mercapto-propylamino)-2-naphthalen-1-yl-benzoylamino]-4-methyl-pentanoic acid (s)-methyl ester
(2s)-methyl 2-(4-((r)-2-amino-3-mercaptopropylamino)-2-(naphthalen-1-yl)benzamido)-4-methylpentanoate
(s)-2-[4-((r)-2-amino-3-mercapto-propylamino)-2-naphthalen-1-yl-benzoylamino]-4-methyl-pentanoic acid methyl ester
ggti 298
NCGC00165800-01
ggti-298 ,
(s)-methyl 2-(4-((r)-2-amino-3-mercaptopropylamino)-2-(naphthalen-1-yl)benzamido)-4-methylpentanoate
CHEBI:124997
CHEMBL282748 ,
180977-44-0
BRD-K19669037-019-01-3
SCHEMBL4283635
Q27215330
(2s)-2-[[[4-[[(2r)-2-amino-3-mercaptopropyl]amino]-2-(1-naphthalenyl)phenyl]-oxomethyl]amino]-4-methylpentanoic acid methyl ester
HY-100876
CS-6098
ggti298
(s)-methyl 2-(4-(((r)-2-amino-3-mercaptopropyl)amino)-2-(naphthalen-1-yl)benzamido)-4-methylpentanoate
AKOS032945065
BCP24854
EX-A2390
unii-ela97v8q7p
l-leucine, n-[4-[[(2r)-2-amino-3-mercaptopropyl]amino]-2-(1-naphthalenyl)benzoyl]-, methyl ester
l-leucine, n-(4-((2-amino-3-mercaptopropyl)amino)-2-(1-naphthalenyl)benzoyl)-, methyl ester, (r)-
ELA97V8Q7P ,
l-leucine, n-(4-(((2r)-2-amino-3-mercaptopropyl)amino)-2-(1-naphthalenyl)benzoyl)-, methyl ester
methyl (2s)-2-[[4-[[(2r)-2-amino-3-sulfanylpropyl]amino]-2-naphthalen-1-ylbenzoyl]amino]-4-methylpentanoate
(s)-methyl2-(4-(((r)-2-amino-3-mercaptopropyl)amino)-2-(naphthalen-1-yl)benzamido)-4-methylpentanoate
A935063
methyl n-[4-{[(2r)-2-amino-3-sulfanylpropyl]amino}-2-(1-naphthyl)benzoyl]-l-leucinate
AC-36053
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
leucine derivativeAn amino acid derivative resulting from reaction of leucine at the amino group or the carboxy group, or from the replacement of any hydrogen of leucine by a heteroatom. The definition normally excludes peptides containing leucine residues.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency1.41250.004023.8416100.0000AID485290
phosphopantetheinyl transferaseBacillus subtilisPotency15.84890.141337.9142100.0000AID1490
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency8.91250.354828.065989.1251AID504847
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorHomo sapiens (human)IC50 (µMol)20.00000.00020.75218.0140AID132512
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)IC50 (µMol)0.05400.00050.471610.0000AID74784
Geranylgeranyl transferase type-1 subunit betaHomo sapiens (human)IC50 (µMol)0.05400.00732.364210.0000AID74784
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaMus musculus (house mouse)IC50 (µMol)20.00001.00001.00001.0000AID132512
Protein farnesyltransferase subunit betaMus musculus (house mouse)IC50 (µMol)20.00001.00001.00001.0000AID132512
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (27)

Processvia Protein(s)Taxonomy
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
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)
protein geranylgeranylationGeranylgeranyl transferase type-1 subunit betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
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 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 (14)

Processvia Protein(s)Taxonomy
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
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)
CAAX-protein geranylgeranyltransferase complexGeranylgeranyl transferase type-1 subunit betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID500997Inhibition of RabGGTase in african green monkey COS7 cells assessed as Rab prenylation by Western blot analysis2009Nature chemical biology, Apr, Volume: 5, Issue:4
Analysis of the eukaryotic prenylome by isoprenoid affinity tagging.
AID132514In vivo inhibition of geranylgeranylation based on the inhibition of Rap1A processing.1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.
AID74784Inhibition binding constant Geranylgeranyl transferase type I2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?
AID575994Antimalarial activity against Plasmodium berghei NK65 infected in human HepG2 cells after 48 hrs by RT-PCR2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Lipophilic bisphosphonates are potent inhibitors of Plasmodium liver-stage growth.
AID164445In vitro inhibition of [3H]GGPP incorporation into H-Ras-CVLL by Geranylgeranyl transferase type I (Not determined)1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.
AID576009Antiplasmodial activity against Plasmodium berghei NK65 infected in 12 wk old C57BL/6 mouse assessed as prepatent period at 5 mg/kg, ip administered once daily via a regimen of day 2, 1 pre-infection, on the day of infection followed by day 1 and 2 postin2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Lipophilic bisphosphonates are potent inhibitors of Plasmodium liver-stage growth.
AID500996Inhibition of FTase in african green monkey COS7 cells assessed as protein prenylation at 15 uM by Western blot analysis2009Nature chemical biology, Apr, Volume: 5, Issue:4
Analysis of the eukaryotic prenylome by isoprenoid affinity tagging.
AID132512In vivo for inhibition of farnesylation based on the inhibition of H-Ras processing.1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.
AID500995Inhibition of GGTase-1 in african green monkey COS7 cells assessed as protein prenylation at >5 uM by Western blot analysis2009Nature chemical biology, Apr, Volume: 5, Issue:4
Analysis of the eukaryotic prenylome by isoprenoid affinity tagging.
AID233815Relative selectivity for H-Ras farnesylation and Rap1A geranylgeranylation as ratio of IC50s1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.
AID72815In vitro inhibition of [3H]FPP incorporation into H-Ras-CVLS by Farnesyl transferase (Not determined)1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.
AID576226Antiplasmodial activity against 3000 Plasmodium berghei NK65 liver stage sporozoites infected in 12 wk old C57BL/6 mouse assessed as delay in prepatent period at 5 mg/kg, ip administered once daily via a regimen of day 2, 1 pre-infection, on the day of in2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Lipophilic bisphosphonates are potent inhibitors of Plasmodium liver-stage growth.
AID575995Cytotoxicity against human HepG2 cells after 22 hrs2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Lipophilic bisphosphonates are potent inhibitors of Plasmodium liver-stage growth.
AID576007Antiplasmodial activity against Plasmodium berghei NK65 infected in 14 wk old C57BL/6 mouse assessed as prepatent period at 5 mg/kg, ip administered once daily via a regimen of day 2, 1 pre-infection, on the day of infection followed by day 1 and 2 postin2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Lipophilic bisphosphonates are potent inhibitors of Plasmodium liver-stage growth.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (68)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's14 (20.59)18.2507
2000's32 (47.06)29.6817
2010's21 (30.88)24.3611
2020's1 (1.47)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 24.85

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index24.85 (24.57)
Research Supply Index4.28 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index29.12 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (24.85)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (1.41%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other70 (98.59%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]