| Reaction Details |
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 | Report a problem with these data |
| Target | Geranylgeranyl transferase type-1 subunit beta [A2V]/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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| Ligand | BDBM14713 |
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| Substrate/Competitor | Ha-Ras-CVLL |
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| Meas. Tech. | In Vitro FTase/GGTase-1 Inhibition Assay |
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| pH | 7.7±n/a |
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| Temperature | 303.15±n/a K |
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| IC50 | 8.24±0.97 nM |
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| Citation |  Peterson, YK; Kelly, P; Weinbaum, CA; Casey, PJ A novel protein geranylgeranyltransferase-I inhibitor with high potency, selectivity, and cellular activity. J Biol Chem281:12445-50 (2006) [PubMed] Article |
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| More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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| Geranylgeranyl transferase type-1 subunit beta [A2V]/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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| Name: | Geranylgeranyl transferase type-1 subunit beta [A2V]/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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| Synonyms: | Geranylgeranyl Transferase (GGTase-I) |
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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: | Geranylgeranyl transferase type-1 subunit beta [A2V] |
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| Synonyms: | GGTase-I-beta | Geranylgeranyl Transferase (GGTase-I) Chain B | Geranylgeranyl transferase type-1 subunit beta | PGGT1B | PGTB1_HUMAN |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 42397.89 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Geranylgeranyl transferase type-1 subunit beta. |
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| Residue: | 377 |
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| Sequence: | MVATEDERLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDM
LDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKAPGTAHPYDSG
HIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASC
ICYMLNNWSGMDMKKAITYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVF
SEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILS
TQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLLDLHQS
WKTKDSKQCSENVHIST
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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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| BDBM14713 |
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| Ha-Ras-CVLL |
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| Name: | Ha-Ras-CVLL |
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| Synonyms: | H-Ras Mutant (S189L) | Ha-Ras Mutant (S189L) | Ras-CVLL |
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| Type: | Other Protein Type |
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| Mol. Mass.: | 21319.45 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Protein was expressed and purified from E. coli.
[3H]-geranylgeranylpyrophosphate (525 nM) as co-substrate. |
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| Residue: | 189 |
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| Sequence: | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAG
QEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHQYREQIKRVKDSDDVPMVLVGNKCDL
AARTVESRQAQDLARSYGIPYIETSAKTRQGVEDAFYTLVREIRQHKLRKLNPPDESGPG
CMSCKCVLL
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