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Target
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM50134315
Substrate
n/a
Meas. Tech.
ChEBML_70452
IC50
80000±n/a nM
Citation
 Vigushin, DM; Brooke, G; Willows, D; Coombes, RC; Moody, CJ Pyrazino[1,2-a]indole-1,4-diones, simple analogues of gliotoxin, as selective inhibitors of geranylgeranyltransferase I. Bioorg Med Chem Lett 13:3661-3 (2003) [PubMed]  Article 
Target
Name:
Protein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Farnesyltransferase (FTase) | Protein Farnesyltransferase (PFT) | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyltransferase
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:
CAAX farnesyltransferase subunit alpha | CAAX farnesyltransferase subunit beta | FNTB | FNTB_HUMAN | FTase-alpha | FTase-beta | GGTase-I-alpha | Protein Farnesyltransferase (PFT) Chain B | Protein farnesyl/geranylgeranyl transferase | Protein farnesyltransferase beta subunit | Protein farnesyltransferase subunit beta | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha | Ras proteins prenyltransferase subunit alpha | Ras proteins prenyltransferase subunit beta | Type I protein geranyl-geranyltransferase subunit alpha
Type:
Enzyme Subunit
Mol. Mass.:
48766.02
Organism:
Homo sapiens (Human)
Description:
Protein farnesyltransferase subunit beta
Residue:
437
Sequence:
MASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFSSYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQIVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQYLYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIGGVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCYSFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDFYHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPVPGFEELKDETSAEPATD
  
Component 2
Name:
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
CAAX farnesyltransferase alpha subunit | FNTA | FNTA_HUMAN | FTase-1-alpha | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Geranylgeranyl transferase type I | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyl/geranylgeranyl transferase | Protein farnesyltransferase | Protein farnesyltransferase subunit alpha | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha
Type:
Enzyme
Mol. Mass.:
44392.46
Organism:
Homo sapiens (Human)
Description:
Recombinant human FTase.
Residue:
379
Sequence:
MAATEGVGEAAQGGEPGQPAQPPPQPHPPPPQQQHKEEMAAEAGEAVASPMDDGFVSLDSPSYVLYRDRAEWADIDPVPQNDGPNPVVQIIYSDKFRDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYITAIIEEQPKNYQVWHHRRVLVEWLRDPSQELEFIADILNQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVISNTTGYNDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSTENDSPTNVQQ
  
Inhibitor
Name:
BDBM50134315
Synonyms:
7-hydroxy-11-hydroxymethyl-12-methyl-14,15-dithia-9,12-diazatetracyclo[9.2.2.01,9.03,8]pentadeca-3,5-diene-10,13-dione | CHEMBL331627 | GLIOTOXIN
Type:
Small organic molecule
Emp. Form.:
C13H14N2O4S2
Mol. Mass.:
326.391
SMILES:
CN1C(=O)[C@]23CC4=CC=C[C@H](O)[C@H]4N2C(=O)[C@@]1(CO)SS3 |r,c:8,t:6,THB:12:13:1.2:19.20,15:14:1.2:19.20|
Structure:
Search PDB for entries with ligand similarity: