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Target
Geranylgeranyl transferase type-1 subunit beta [A2V]/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM14434
Substrate
PGGT I peptide substrate
Meas. Tech.
GGTase-1 Scintillation Proximity Assay
pH
7.5±n/a
Temperature
295.15±n/a K
Comments
40% inhibition uM.
Citation
 End, DW; Smets, G; Todd, AV; Applegate, TL; Fuery, CJ; Angibaud, P; Venet, M; Sanz, G; Poignet, H; Skrzat, S; Devine, A; Wouters, W; Bowden, C Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. Cancer Res 61:131-7 (2001) [PubMed] 
Target
Name:
Geranylgeranyl transferase type-1 subunit beta [A2V]/Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
Geranylgeranyl Transferase (GGTase-I)
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:
Geranylgeranyl transferase type-1 subunit beta [A2V]
Synonyms:
GGTase-I-beta | Geranylgeranyl Transferase (GGTase-I) Chain B | Geranylgeranyl transferase type-1 subunit beta | PGGT1B | PGTB1_HUMAN
Type:
Enzyme Subunit
Mol. Mass.:
42397.89
Organism:
Homo sapiens (Human)
Description:
Geranylgeranyl transferase type-1 subunit beta.
Residue:
377
Sequence:
MVATEDERLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDMLDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKAPGTAHPYDSGHIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASCICYMLNNWSGMDMKKAITYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVFSEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILSTQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLLDLHQSWKTKDSKQCSENVHIST
  
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:
BDBM14434
Synonyms:
6-[amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-1,2-dihydroquinolin-2-one | 6-[amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2(1H)-one | R-115777 | R-115777 | Zarnestra | Racemic mixture | Tipifarnib | Zarnestra
Type:
Small organic molecule
Emp. Form.:
C27H22Cl2N4O
Mol. Mass.:
489.396
SMILES:
Cn1cncc1C(N)(c1ccc(Cl)cc1)c1ccc2n(C)c(=O)cc(-c3cccc(Cl)c3)c2c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PGGT I peptide substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1696.97
Organism:
n/a
Description:
n/a
Residue:
15
Sequence:
ITINYRASNRSCAIL