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Literature summary for 2.5.1.59 extracted from

  • Peterson, Y.K.; Wang, X.S.; Casey, P.J.; Tropsha, A.
    Discovery of geranylgeranyltransferase-I inhibitors with novel scaffolds by the means of quantitative structure-activity relationship modeling, virtual screening, and experimental validation (2009), J. Med. Chem., 52, 4210-4220.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
recombinant mammalian enzyme expressed in Sf9 cells Mammalia

Inhibitors

Inhibitors Comment Organism Structure
3-chloro-N-[2-oxo-2-[2-[[1-phenyl-3-(4-propoxyphenyl)pyrazol-4-yl]methylidene]hydrazinyl]ethyl]benzamide GGTI-DU.Sig1, PubChem CID 3311883, inhibitor of protein geranylgeranyltransferase type I Mammalia
4-[[([5-[(4-ethylphenoxy)methyl]-4-(1-phenylethyl)-4H-pyrazol-3-yl]sulfanyl)acetyl]amino]benzamide inhibitor identified using quantitative structure-activity realtionship models and virtual screening of chemicals. confirmation of predicted data by experiment Rattus norvegicus
4-[[2-[[5-(2-methoxyphenyl)-4-phenethyl-1,2,4-triazol-3-yl]sulfanyl]acetyl]amino]benzamide GGTI-DU.En1, PubChem CID 2118978, inhibitor of protein geranylgeranyltransferase type I Mammalia
4-[[2-[[5-[(4-ethylphenoxy)methyl]-4-(1-phenylethyl)-1,2,4-triazol-3-yl]sulfanyl]acetyl]amino]benzamide GGTI-DU.En2, PubChem CID 3455185, inhibitor of protein geranylgeranyltransferase type I, no or little activity against protein farnesyltransferase Mammalia
additional information inhibitors pose a potential treatment for inflammation, multiple sclerosis, atherosclerosis, and other diseases, 47 potential inhibitors with a predicted IC50 greater than 5.50 microM are identified by the use of quantitative structure-activity relationship models and in vitro tests with 7 of them Mammalia
N-(2,5-dichlorophenyl)-N'-[[3-(4-methylphenyl)-1-phenylpyrazol-4-yl]methylideneamino]oxamide GGTI-DU.Sig2, PubChem CID 4277701, inhibitor of protein geranylgeranyltransferase type I Mammalia
N-benzyl-2-[(2-chlorobenzyl)[[5-(4-methylphenyl)-2H-tetrazol-2-yl]acetyl]amino]butanamide inhibitor identified using quantitative structure-activity realtionship models and virtual screening of chemicals. confirmation of predicted data by experiment Rattus norvegicus
N-benzyl-2-[(2-chlorophenyl)methyl-[2-[5-(4-methylphenyl)tetrazol-2-yl]acetyl]amino]butanamide GGTI-DU.As2, PubChem CID 3180738, inhibitor of protein geranylgeranyltransferase type I, no or little activity against protein farnesyltransferase Mammalia
N-[(E)-1-(benzylcarbamoyl)-2-[5-(3,4-dichlorophenyl)furan-2-yl]ethenyl]-4-methylbenzamide inhibitor identified using quantitative structure-activity realtionship models and virtual screening of chemicals. confirmation of predicted data by experiment Rattus norvegicus
N-[2-(benzylamino)-2-oxoethyl]-2-[5-(4-chlorophenyl)tetrazol-2-yl]-N-(4-propan-2-ylphenyl)acetamide GGTI-DU.As1, PubChem CID 3180720, inhibitor of protein geranylgeranyltransferase type I Mammalia
N-[3-(benzylamino)-1-[5-(3,4-dichlorophenyl)furan-2-yl]-3-oxoprop-1-en-2-yl]-4-methylbenzamide GGTI-DU.Sig3, PubChem CID 5143450, inhibitor of protein geranylgeranyltransferase type I, no or little activity against protein farnesyltransferase Mammalia

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
geranylgeranyl diphosphate + Ras-CVLL Mammalia tritium labelled geranylgeranyl diphosphate for enzyme assay, His-tagged geranylgeranyl diphosphate S-geranylgeranyl-Ras-CVLL + diphosphate
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Organism

Organism UniProt Comment Textmining
Mammalia
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-
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Rattus norvegicus
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Purification (Commentary)

Purification (Comment) Organism
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Mammalia

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
geranylgeranyl diphosphate + Ras-CVLL tritium labelled geranylgeranyl diphosphate for enzyme assay, His-tagged geranylgeranyl diphosphate Mammalia S-geranylgeranyl-Ras-CVLL + diphosphate
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Synonyms

Synonyms Comment Organism
mammalian GGTase-I
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Mammalia
protein geranylgeranyltransferase type I
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Mammalia

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.008
-
30°C Rattus norvegicus 4-[[([5-[(4-ethylphenoxy)methyl]-4-(1-phenylethyl)-4H-pyrazol-3-yl]sulfanyl)acetyl]amino]benzamide
0.035
-
30°C Rattus norvegicus N-benzyl-2-[(2-chlorobenzyl)[[5-(4-methylphenyl)-2H-tetrazol-2-yl]acetyl]amino]butanamide
0.043
-
30°C Rattus norvegicus N-[(E)-1-(benzylcarbamoyl)-2-[5-(3,4-dichlorophenyl)furan-2-yl]ethenyl]-4-methylbenzamide