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Target
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM14453
Substrate
Ha-Ras-CVLS
Meas. Tech.
FTase Activity Assay
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
0.15±n/a nM
Citation
 Li, Q; Woods, KW; Wang, W; Lin, NH; Claiborne, A; Gu, WZ; Cohen, J; Stoll, VS; Hutchins, C; Frost, D; Rosenberg, SH; Sham, HL Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors. Bioorg Med Chem Lett 15:2033-9 (2005) [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:
BDBM14453
Synonyms:
1-({1-[(4-cyanophenyl)methyl]-1H-imidazol-5-yl}methyl)-5-(naphthalen-1-yl)-1H-indole-4-carbonitrile | indole analog 4d
Type:
Small organic molecule
Emp. Form.:
C31H21N5
Mol. Mass.:
463.5319
SMILES:
N#Cc1ccc(Cn2cncc2Cn2ccc3c(C#N)c(ccc23)-c2cccc3ccccc23)cc1
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