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TargetProtein Farnesyltransferase (PFT)
LigandBDBM14423
Substrate/CompetitorHa-Ras-CVLS
Meas. Tech.FTase Activity Assay
pH7.5±n/a
Temperature310.15±n/a K
IC50 0.5±n/a nM
Citation Li QLi TWoods KWGu WZCohen JStoll VSGalicia THutchins CFrost DRosenberg SHSham HL Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity. Bioorg Med Chem Lett 15:2918-22 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Protein Farnesyltransferase (PFT)
Name:Protein Farnesyltransferase (PFT)
Synonyms:Protein farnesyltransferase
Type:Protein Complex
Mol. Mass.:n/a
Description:Purified bovine brain FTase.
Components:This complex has 2 components.
Component 1
Name:Protein farnesyltransferase
Synonyms:CAAX farnesyltransferase alpha subunit | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha | Type I protein geranyl-geranyltransferase alpha subunit
Type:Enzyme
Mol. Mass.:43827.38
Organism:Bos taurus (bovine)
Description:The enzyme was purified from a bovine brain homogenate by sequential ammonium sulfate fractionation and affinity chromatography.
Residue:375
Sequence:
MAAADGVGEAAQGGDPGQPEPPPPPQPHPPPPPPQPPQEEAAAASPIDDGFLSLDSPTYV
LYRDRPEWADIDPVPQNDGPNPVVQIIYSEKFQDVYDYFRAVLQRDERSERAFKLTRDAI
ELNAANYTVWHFRRVLLKSLQKDLHEEMNYISAIIEEQPKNYQVWHHRRVLVEWLRDPSQ
ELEFIADILTQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVI
SNTTGYNDRAILEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQP
SHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQ
SKHSTESDPPTNVQQ
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Component 2
Name:Protein farnesyltransferase
Synonyms:CAAX farnesyltransferase subunit beta | FTase-beta | Protein farnesyltransferase beta subunit | Protein farnesyltransferase subunit beta | RAS proteins prenyltransferase beta | Ras proteins prenyltransferase subunit beta
Type:Enzyme Subunit
Mol. Mass.:48758.49
Organism:Bos taurus (bovine)
Description:Protein farnesyltransferase subunit beta
Residue:437
Sequence:
MASPSSFTYCCPPSSSPIWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS
SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ
MVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDVINREKLLQY
LYSLKQPDGSFLMHDGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG
GVPGMEAHGGYTFCGLAALVILKKERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY
SFWQAGLLPLLHRALHAQGDPALSMSRWMFHQQALQEYILMCCQCPTGGLLDKPGKSRDF
YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATMHFLQKPV
PGFEEHEDEASAEPATD
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BDBM14423
Ha-Ras-CVLS
Name:GTPase HRas
Synonyms:GTPase HRas, N-terminally processed | H-Ras | H-Ras-1 | HRAS1 | 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:P01112
Residue:189
Sequence:
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAG
QEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHQYREQIKRVKDSDDVPMVLVGNKCDL
AARTVESRQAQDLARSYGIPYIETSAKTRQGVEDAFYTLVREIRQHKLRKLNPPDESGPG
CMSCKCVLS
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