Reaction Details |
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Target | Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha |
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Ligand | BDBM14018 |
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Substrate/Competitor | K-Ras C-terminus |
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Meas. Tech. | In Vitro FTase Inhibition Assay |
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IC50 | <1±n/a nM |
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Citation | Bell, IM; Gallicchio, SN; Abrams, M; Beese, LS; Beshore, DC; Bhimnathwala, H; Bogusky, MJ; Buser, CA; Culberson, JC; Davide, J; Ellis-Hutchings, M; Fernandes, C; Gibbs, JB; Graham, SL; Hamilton, KA; Hartman, GD; Heimbrook, DC; Homnick, CF; Huber, HE; Huff, JR; Kassahun, K; Koblan, KS; Kohl, NE; Lobell, RB; Lynch, JJ; Robinson, R; Rodrigues, AD; Taylor, JS; Walsh, ES; Williams, TM; Zartman, CB 3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency. J Med Chem45:2388-409 (2002) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, 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: | Farnesyltransferase (FTase) | Protein Farnesyltransferase (PFT) | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyltransferase |
Type: | Protein Complex |
Mol. Mass.: | n/a |
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. |
Components: | This complex has 2 components. |
Component 1 |
Name: | Protein farnesyltransferase subunit beta |
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 |
Type: | Enzyme Subunit |
Mol. Mass.: | 48766.02 |
Organism: | Homo sapiens (Human) |
Description: | Protein farnesyltransferase subunit beta |
Residue: | 437 |
Sequence: | MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
IVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQY
LYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPV
PGFEELKDETSAEPATD
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Component 2 |
Name: | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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 |
Type: | Enzyme |
Mol. Mass.: | 44392.46 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant human FTase. |
Residue: | 379 |
Sequence: | MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDS
PSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLR
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQR
YFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSTENDSPTNVQQ
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BDBM14018 |
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K-Ras C-terminus |
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Name: | K-Ras C-terminus |
Synonyms: | K-Ras C-terminus containing PDCVIM |
Type: | Other Protein Type |
Mol. Mass.: | 358.43 |
Organism: | n/a |
Description: | [3H]farnesyl diphosphate (10-500 nM) as co-substrate. |
Residue: | 3 |
Sequence: | |