Reaction Details Report a problem with these data
Target
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM238373
Substrate
n/a
Meas. Tech.
Human FTase Assay
IC50
3300±200 nM
Citation
 Lethu, S; Bosc, D; Mouray, E; Grellier, P; Dubois, J New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis. J Enzyme Inhib Med Chem 28:163-71 (2013) [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:
BDBM238373
Synonyms:
3-(3-Biphenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid (1aa)
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
CC(C)Sc1sc(C(O)=O)c(c1C#N)-c1cccc(c1)-c1ccccc1
Structure:
Search PDB for entries with ligand similarity: