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TargetProtein Farnesyltransferase (PFT)
LigandBDBM13307
Substrate/Competitorn/a
Meas. Tech.ChEBML_665227
IC50 56±n/a nM
Citation Fletcher SKeaney EPCummings CGBlaskovich MAHast MAGlenn MPChang SYBucher CJFloyd RJKatt WPGelb MHVan Voorhis WCBeese LSSebti SMHamilton AD Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents. J Med Chem 53:6867-88 (2010) [PubMed]  Article
More Info.:Get all data from this article,  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
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
n/a