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Target
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM17326
Substrate
Ha-Ras-CVLS
Meas. Tech.
FTase Activity Assay
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
2.5±n/a nM
Citation
 Gwaltney, SL; O'Connor, SJ; Nelson, LT; Sullivan, GM; Imade, H; Wang, W; Hasvold, L; Li, Q; Cohen, J; Gu, WZ; Tahir, SK; Bauch, J; Marsh, K; Ng, SC; Frost, DJ; Zhang, H; Muchmore, S; Jakob, CG; Stoll, V; Hutchins, C; Rosenberg, SH; Sham, HL Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. Bioorg Med Chem Lett 13:1359-62 (2003) [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:
BDBM17326
Synonyms:
(2S)-2-[(1-{2-[benzyl(1,3-thiazol-5-ylmethyl)amino]acetyl}-5-(2-methylphenyl)-1,2,3,6-tetrahydropyridin-4-yl)formamido]-4-(methylsulfanyl)butanoic acid | methionine containing tetrahydropyridine, 8
Type:
Small organic molecule
Emp. Form.:
C31H36N4O4S2
Mol. Mass.:
592.772
SMILES:
CSCC[C@H](NC(=O)C1=C(CN(CC1)C(=O)CN(Cc1cncs1)Cc1ccccc1)c1ccccc1C)C(O)=O |r,t:8|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
GTPase HRas
Synonyms:
GTPase HRas, N-terminally processed | H-Ras | H-Ras-1 | HRAS | HRAS1 | Ha-Ras | His6-Ha-Ras-CVLS | RASH_HUMAN | 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:
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHQYREQIKRVKDSDDVPMVLVGNKCDLAARTVESRQAQDLARSYGIPYIETSAKTRQGVEDAFYTLVREIRQHKLRKLNPPDESGPGCMSCKCVLS