| Reaction Details |
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 | Report a problem with these data |
| Target | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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| Ligand | BDBM13365 |
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| Substrate/Competitor | biotinylated lamin B peptide substrate |
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| Meas. Tech. | PFT IC50 Determination |
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| pH | 7.5±n/a |
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| Temperature | 310.15±n/a K |
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| IC50 | 4300±2100 nM |
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| Citation |  Santagada, V; Caliendo, G; Severino, B; Lavecchia, A; Perissutti, E; Fiorino, F; Zampella, A; Sepe, V; Califano, D; Santelli, G; Novellino, E Synthesis, pharmacological evaluation, and molecular modeling studies of novel peptidic CAAX analogues as farnesyl-protein-transferase inhibitors. J Med Chem49:1882-90 (2006) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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| Name: | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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| Synonyms: | CAAX farnesyltransferase alpha subunit | FNTA | FNTA_BOVIN | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyltransferase | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha | Type I protein geranyl-geranyltransferase alpha subunit |
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| Type: | Enzyme |
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| Mol. Mass.: | 43827.38 |
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| Organism: | Bos taurus (bovine) |
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| Description: | The enzyme was purified from a bovine brain homogenate by sequential ammonium sulfate fractionation and affinity chromatography. |
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| Residue: | 375 |
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| Sequence: | MAAADGVGEAAQGGDPGQPEPPPPPQPHPPPPPPQPPQEEAAAASPIDDGFLSLDSPTYV
LYRDRPEWADIDPVPQNDGPNPVVQIIYSEKFQDVYDYFRAVLQRDERSERAFKLTRDAI
ELNAANYTVWHFRRVLLKSLQKDLHEEMNYISAIIEEQPKNYQVWHHRRVLVEWLRDPSQ
ELEFIADILTQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVI
SNTTGYNDRAILEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQP
SHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQ
SKHSTESDPPTNVQQ
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| BDBM13365 |
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| biotinylated lamin B peptide substrate |
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| Name: | biotinylated lamin B peptide substrate |
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| Synonyms: | n/a |
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| Type: | Peptide |
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| Mol. Mass.: | 1715.01 |
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| Organism: | n/a |
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| Description: | A human lamin-B carboxy-terminus sequence peptide (biotin-YRASNRSCAIM) is 3H-farnesylated at the cysteine residue when processed by farnesyltransferase. |
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| Residue: | 15 |
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| Sequence: | |
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