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TargetProtein Farnesyltransferase (PFT)
LigandBDBM13307
Substrate/CompetitorHa-Ras-CVLS
Meas. Tech.In Vitro PFT Activity Assay
pH7.7±n/a
Temperature303.15±n/a K
IC50 56±29 nM
Citation Hast MAFletcher SCummings CGPusateri EEBlaskovich MARivas KGelb MHVan Voorhis WCSebti SMHamilton ADBeese LS Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase. Chem Biol 16:181-92 (2009) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Protein Farnesyltransferase (PFT)
Name:Protein Farnesyltransferase (PFT)
Synonyms:Farnesyltransferase (FTase) | 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 farnesyl/geranylgeranyl transferase
Synonyms:CAAX farnesyltransferase subunit alpha | CAAX farnesyltransferase subunit beta | FTase-alpha | FTase-beta | GGTase-I-alpha | Protein Farnesyltransferase (PFT) Chain B | 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 farnesyl/geranylgeranyl transferase
Synonyms:CAAX farnesyltransferase alpha subunit | FTase-1-alpha | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Protein Farnesyltransferase (PFT) Chain A | 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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BDBM13307
NameBDBM13307
Synonyms:1-Methyl-1H-imidazole-4-sulfonic Acid Benzyl-{2-[(4-cyanophenyl)-(3-methyl-3H-imidazol-4-ylmethyl)amino]ethyl}amide | Chem Biol Compound 2 | N-benzyl-N-{2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl}-1-methyl-1H-imidazole-4-sulfonamide | Sulfonamide 12d
TypeSmall organic molecule
Emp. Form.C25H27N7O2S
Mol. Mass.489.593
SMILESCn1cnc(c1)S(=O)(=O)N(CCN(Cc1cncn1C)c1ccc(cc1)C#N)Cc1ccccc1
Structure
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Ha-Ras-CVLS
Name:Ha-Ras-CVLS
Synonyms:GTPase HRas | GTPase HRas, N-terminally processed | H-Ras | H-Ras-1 | Ha-Ras | His6-Ha-Ras-CVLS | Transforming protein p21 | Transforming protein p21/H-Ras-1 | Wild-type Ha-Ras | c-H-ras | p21ras
Type:Other Protein Type
Mol. Mass.:21293.37
Organism:Homo sapiens (human)
Description:P21 Ha-Ras was expressed and purified from E. coli. [3H]FPP (625 nM) as co-substrate.
Residue:189
Sequence:
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAG
QEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHQYREQIKRVKDSDDVPMVLVGNKCDL
AARTVESRQAQDLARSYGIPYIETSAKTRQGVEDAFYTLVREIRQHKLRKLNPPDESGPG
CMSCKCVLS
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