Reaction Details |
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Target | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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Ligand | BDBM13373 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_70276 (CHEMBL681415) |
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IC50 | 25±n/a nM |
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Citation | Leonard, DM; Shuler, KR; Poulter, CJ; Eaton, SR; Sawyer, TK; Hodges, JC; Su, TZ; Scholten, JD; Gowan, RC; Sebolt-Leopold, JS; Doherty, AM Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase. J Med Chem40:192-200 (1997) [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 |
Synonyms: | Protein Farnesyltransferase (PFT) | Protein farnesyltransferase |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | Purified bovine brain FTase. |
Components: | This complex has 2 components. |
Component 1 |
Name: | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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 |
Type: | Enzyme |
Mol. Mass.: | 43827.38 |
Organism: | Bos taurus (bovine) |
Description: | The enzyme was purified from a bovine brain homogenate by sequential ammonium sulfate fractionation and affinity chromatography. |
Residue: | 375 |
Sequence: | MAAADGVGEAAQGGDPGQPEPPPPPQPHPPPPPPQPPQEEAAAASPIDDGFLSLDSPTYV
LYRDRPEWADIDPVPQNDGPNPVVQIIYSEKFQDVYDYFRAVLQRDERSERAFKLTRDAI
ELNAANYTVWHFRRVLLKSLQKDLHEEMNYISAIIEEQPKNYQVWHHRRVLVEWLRDPSQ
ELEFIADILTQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVI
SNTTGYNDRAILEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQP
SHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQ
SKHSTESDPPTNVQQ
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Component 2 |
Name: | Protein farnesyltransferase subunit beta |
Synonyms: | CAAX farnesyltransferase subunit beta | FNTB | FNTB_BOVIN | FTase-beta | Protein farnesyltransferase | Protein farnesyltransferase beta subunit | Protein farnesyltransferase subunit beta | RAS proteins prenyltransferase beta | Ras proteins prenyltransferase subunit beta |
Type: | Enzyme Subunit |
Mol. Mass.: | 48758.49 |
Organism: | Bos taurus (bovine) |
Description: | Protein farnesyltransferase subunit beta |
Residue: | 437 |
Sequence: | MASPSSFTYCCPPSSSPIWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
MVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDVINREKLLQY
LYSLKQPDGSFLMHDGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKKERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSRWMFHQQALQEYILMCCQCPTGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATMHFLQKPV
PGFEEHEDEASAEPATD
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BDBM13373 |
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n/a |
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Name | BDBM13373 |
Synonyms: | (2S)-2-[(2S)-2-[(2S)-2-[(2R)-2-amino-3-sulfanylpropanamido]-3-methylbutanamido]-3-phenylpropanamido]-4-(methylsulfanyl)butanoic acid | CHEMBL289302 | CHEMBL553980 | CVFM |
Type | Small organic molecule |
Emp. Form. | C22H34N4O5S2 |
Mol. Mass. | 498.659 |
SMILES | CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CS)C(C)C)C(O)=O |r| |
Structure |
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