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TargetProtein Farnesyltransferase (PFT)
LigandBDBM50130365
Substrate/Competitorn/a
Meas. Tech.ChEMBL_70431
IC50 0.19±n/a nM
Citation deSolms SJCiccarone TMMacTough SCShaw AWBuser CAEllis-Hutchings MFernandes CHamilton KAHuber HEKohl NELobell RBRobinson RGTsou NNWalsh ESGraham SLBeese LSTaylor JS Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents. J Med Chem 46:2973-84 (2003) [PubMed]  Article
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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BDBM50130365
n/a
NameBDBM50130365
Synonyms:4-[1-Amino-1-(3-methyl-3H-imidazol-4-yl)-ethyl]-2-{3-[1-methyl-2-oxo-3-(3,3,3-trifluoro-propyl)-azepan-3-yl]-phenoxy}-benzonitrile | CHEMBL316673
TypeSmall organic molecule
Emp. Form.C29H32F3N5O2
Mol. Mass.539.5919
SMILESCN1CCCC[C@@](CCC(F)(F)F)(c2cccc(Oc3cc(ccc3C#N)[C@](C)(N)c3cncn3C)c2)C1=O
Structure
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