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Target
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50080743
Substrate
n/a
Meas. Tech.
ChEMBL_70270 (CHEMBL681409)
IC50
0.4±n/a nM
Citation
 O'Connor, SJ; Barr, KJ; Wang, L; Sorensen, BK; Tasker, AS; Sham, H; Ng, SC; Cohen, J; Devine, E; Cherian, S; Saeed, B; Zhang, H; Lee, JY; Warner, R; Tahir, S; Kovar, P; Ewing, P; Alder, J; Mitten, M; Leal, J; Marsh, K; Bauch, J; Hoffman, DJ; Sebti, SM; Rosenberg, SH Second-generation peptidomimetic inhibitors of protein farnesyltransferase demonstrating improved cellular potency and significant in vivo efficacy. J Med Chem 42:3701-10 (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:
BDBM50080743
Synonyms:
(S)-2-({5-[(Benzyl-thiazol-5-ylmethyl-amino)-methyl]-2'-methyl-biphenyl-2-carbonyl}-amino)-4-methylsulfanyl-butyric acid | CHEMBL121921
Type:
Small organic molecule
Emp. Form.:
C31H33N3O3S2
Mol. Mass.:
559.742
SMILES:
CSCC[C@H](NC(=O)c1ccc(CN(Cc2cncs2)Cc2ccccc2)cc1-c1ccccc1C)C(O)=O
Structure:
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