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Target
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50115924
Substrate
n/a
Meas. Tech.
ChEBML_69836
IC50
63±n/a nM
Citation
 Tucker, TJ; Abrams, MT; Buser, CA; Davide, JP; Ellis-Hutchings, M; Fernandes, C; Gibbs, JB; Graham, SL; Hartman, GD; Huber, HE; Liu, D; Lobell, RB; Lumma, WC; Robinson, RG; Sisko, JT; Smith, AM The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases. Bioorg Med Chem Lett 12:2027-30 (2002) [PubMed]  Article 
Target
Name:
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Farnesyltransferase (FTase) | Protein farnesyltransferase | Protein Farnesyltransferase (PFT) | Protein Farnesyltransferase (PFT) Chain B
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
To express recombinant enzyme in E. coli, the cloned human alpha and beta subunits were co-expressed from a plasmid, in which their expression was translationally coupled.
Components:
This complex has 2 components.
Component 1
Name:
Protein farnesyltransferase subunit beta
Synonyms:
Protein Farnesyltransferase (PFT) Chain B | Protein farnesyltransferase subunit beta | CAAX farnesyltransferase subunit beta | CAAX farnesyltransferase subunit alpha | Ras proteins prenyltransferase subunit alpha | Type I protein geranyl-geranyltransferase subunit alpha | FTase-beta | GGTase-I-alpha | Ras proteins prenyltransferase subunit beta | Protein farnesyltransferase beta subunit | FTase-alpha | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | FNTB_HUMAN | FNTB | Protein farnesyl/geranylgeranyl transferase
Type:
Enzyme Subunit
Mol. Mass.:
48766.02
Organism:
Human
Description:
Protein farnesyltransferase subunit beta
Residue:
437
Sequence:
MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFSSYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQIVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQYLYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIGGVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCYSFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDFYHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPVPGFEELKDETSAEPATD
  
Component 2
Name:
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Protein Farnesyltransferase (PFT) Chain A | GGTase-I-alpha | FTase-alpha | FTase-1-alpha | Protein farnesyltransferase | Ras proteins prenyltransferase alpha | CAAX farnesyltransferase alpha subunit | Protein farnesyltransferase subunit alpha | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Geranylgeranyl Transferase (GGTase-I) Chain A | FNTA_HUMAN | FNTA | Geranylgeranyl transferase type I | Protein farnesyl/geranylgeranyl transferase
Type:
Enzyme
Mol. Mass.:
44392.46
Organism:
Human
Description:
Recombinant human FTase.
Residue:
379
Sequence:
MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDSPSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLRDPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSTENDSPTNVQQ
  
Inhibitor
Name:
BDBM50115924
Synonyms:
4-[3-(4-Cyano-benzyl)-3H-imidazol-4-ylmethyl]-piperazine-1-carboxylic acid 2-methyl-benzyl ester | CHEMBL304449
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
Cc1ccccc1COC(=O)N1CCN(Cc2cncn2Cc2ccc(cc2)C#N)CC1
Structure:
Search PDB for entries with ligand similarity: