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Target
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50079786
Substrate
n/a
Meas. Tech.
ChEMBL_70277 (CHEMBL681416)
IC50
20±n/a nM
Citation
 O'Connell, CE; Ackermann, K; Rowell, CA; Garcia, AM; Lewis, MD; Schwartz, CE Synthesis and evaluation of hydroxyproline-derived isoprenyltransferase inhibitors. Bioorg Med Chem Lett 9:2095-100 (1999) [PubMed]  Article 
Target
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:
MAAADGVGEAAQGGDPGQPEPPPPPQPHPPPPPPQPPQEEAAAASPIDDGFLSLDSPTYVLYRDRPEWADIDPVPQNDGPNPVVQIIYSEKFQDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYISAIIEEQPKNYQVWHHRRVLVEWLRDPSQELEFIADILTQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVISNTTGYNDRAILEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSTESDPPTNVQQ
  
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:
MASPSSFTYCCPPSSSPIWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFSSYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQMVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDVINREKLLQYLYSLKQPDGSFLMHDGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIGGVPGMEAHGGYTFCGLAALVILKKERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCYSFWQAGLLPLLHRALHAQGDPALSMSRWMFHQQALQEYILMCCQCPTGGLLDKPGKSRDFYHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATMHFLQKPVPGFEEHEDEASAEPATD
  
Inhibitor
Name:
BDBM50079786
Synonyms:
2-[1-[5-amino-6-sulfanyl-(5R)-hexyl]-4-phenoxy-(2S,4S)-tetrahydro-1H-2-pyrrolylcarboxamido]-4-methylsulfanyl-(2S)-butanoic acid with di( TFA) | CHEMBL303509
Type:
Small organic molecule
Emp. Form.:
C22H35N3O4S2
Mol. Mass.:
469.661
SMILES:
CSCC[C@H](NC(=O)[C@@H]1C[C@@H](CN1CCCC[C@@H](N)CS)Oc1ccccc1)C(O)=O
Structure:
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