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TargetProtein Farnesyltransferase (PFT)
LigandBDBM50126326
Substrate/Competitorn/a
Meas. Tech.ChEBML_69990
IC50 0.500000±n/a nM
Citation Gwaltney SLO'Connor SJNelson LTSullivan GMImade HWang WHasvold LLi QCohen JGu WZTahir SKBauch JMarsh KNg SCFrost DJZhang HMuchmore SJakob CGStoll VHutchins CRosenberg SHSham HL Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency. Bioorg Med Chem Lett 13:1363-6 (2003) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Protein Farnesyltransferase (PFT)
Name:Protein Farnesyltransferase (PFT)
Synonyms:Farnesyltransferase (FTase) | 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 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:Geranylgeranyl transferase type I
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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BDBM50126326
n/a
NameBDBM50126326
Synonyms:1-[(4-Cyano-phenyl)-(3-methyl-3H-imidazol-4-yl)-methyl]-5-naphthalen-1-yl-1,2,3,6-tetrahydro-pyridine-4-carbonitrile | CHEMBL30118
TypeSmall organic molecule
Emp. Form.C28H23N5
Mol. Mass.429.5157
SMILESCn1cncc1C(N1CCC(C#N)=C(C1)c1cccc2ccccc12)c1ccc(cc1)C#N |c:13|
Structure
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