| Reaction Details |
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 | Report a problem with these data |
| Target | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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| Ligand | BDBM238361 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | Human FTase Assay |
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| IC50 | 39000±4000 nM |
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| Citation |  Lethu, S; Bosc, D; Mouray, E; Grellier, P; Dubois, J New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis. J Enzyme Inhib Med Chem28:163-71 (2013) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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| Name: | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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| Synonyms: | Farnesyltransferase (FTase) | Protein Farnesyltransferase (PFT) | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyltransferase |
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| Type: | Protein Complex |
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| Mol. Mass.: | n/a |
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| Description: | To express recombinant enzyme in E. coli, the cloned human alpha and beta subunits were co-expressed from a plasmid, in which their expression was translationally coupled. |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Protein farnesyltransferase subunit beta |
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| Synonyms: | CAAX farnesyltransferase subunit alpha | CAAX farnesyltransferase subunit beta | FNTB | FNTB_HUMAN | FTase-alpha | FTase-beta | GGTase-I-alpha | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyl/geranylgeranyl transferase | Protein farnesyltransferase beta subunit | Protein farnesyltransferase subunit beta | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Ras proteins prenyltransferase subunit alpha | Ras proteins prenyltransferase subunit beta | Type I protein geranyl-geranyltransferase subunit alpha |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 48766.02 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Protein farnesyltransferase subunit beta |
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| Residue: | 437 |
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| Sequence: | MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
IVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQY
LYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPV
PGFEELKDETSAEPATD
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| Component 2 |
| Name: | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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| Synonyms: | CAAX farnesyltransferase alpha subunit | FNTA | FNTA_HUMAN | FTase-1-alpha | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Geranylgeranyl transferase type I | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyl/geranylgeranyl transferase | Protein farnesyltransferase | Protein farnesyltransferase subunit alpha | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha |
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| Type: | Enzyme |
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| Mol. Mass.: | 44392.46 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Recombinant human FTase. |
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| Residue: | 379 |
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| Sequence: | MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDS
PSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLR
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQR
YFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSTENDSPTNVQQ
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| BDBM238361 |
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| n/a |
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| Name | BDBM238361 |
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| Synonyms: | 3-(4-Methoxyphenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid (1j) |
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| Type | Small organic molecule |
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| Emp. Form. | C16H15NO3S2 |
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| Mol. Mass. | 333.425 |
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| SMILES | COc1ccc(cc1)-c1c(sc(SC(C)C)c1C#N)C(O)=O |
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| Structure | 
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