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TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
LigandBDBM50080744
Substrate/Competitorn/a
Meas. Tech.ChEMBL_70270 (CHEMBL681409)
IC50 0.8±n/a nM
Citation O'Connor, SJBarr, KJWang, LSorensen, BKTasker, ASSham, HNg, SCCohen, JDevine, ECherian, SSaeed, BZhang, HLee, JYWarner, RTahir, SKovar, PEwing, PAlder, JMitten, MLeal, JMarsh, KBauch, JHoffman, DJSebti, SMRosenberg, SH Second-generation peptidomimetic inhibitors of protein farnesyltransferase demonstrating improved cellular potency and significant in vivo efficacy. J Med Chem42:3701-10 (1999) [PubMed]  Article
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Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Name:Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Synonyms:Protein Farnesyltransferase (PFT) | 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/geranylgeranyltransferase type-1 subunit alpha
Synonyms:CAAX farnesyltransferase alpha subunit | FNTA | FNTA_BOVIN | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyltransferase | 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 subunit beta
Synonyms:CAAX farnesyltransferase subunit beta | FNTB | FNTB_BOVIN | FTase-beta | Protein farnesyltransferase | 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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BDBM50080744
n/a
NameBDBM50080744
Synonyms:(S)-2-({5-[(Benzyl-pyrazin-2-yl-amino)-methyl]-2'-methyl-biphenyl-2-carbonyl}-amino)-4-methylsulfanyl-butyric acid | CHEMBL122882
TypeSmall organic molecule
Emp. Form.C31H32N4O3S
Mol. Mass.540.676
SMILESCSCC[C@H](NC(=O)c1ccc(CN(Cc2ccccc2)c2cnccn2)cc1-c1ccccc1C)C(O)=O
Structure
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