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Target
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM13335
Substrate
biotinylated lamin B peptide substrate
Meas. Tech.
PfPFT and Rat PFT IC50 Determination
IC50
5±n/a nM
Citation
 Nallan, L; Bauer, KD; Bendale, P; Rivas, K; Yokoyama, K; Horney, CP; Pendyala, PR; Floyd, D; Lombardo, LJ; Williams, DK; Hamilton, A; Sebti, S; Windsor, WT; Weber, PC; Buckner, FS; Chakrabarti, D; Gelb, MH; Van Voorhis, WC Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. J Med Chem 48:3704-13 (2005) [PubMed]  Article 
Target
Name:
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Synonyms:
CAAX farnesyltransferase alpha subunit | FNTA_RAT | FTase-alpha | Fnta | GGTase-I-alpha | Protein farnesyltransferase | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha | Type I protein geranyl-geranyltransferase alpha subunit | geranylgeranyltransferase type-I
Type:
Enzyme
Mol. Mass.:
44030.14
Organism:
Rattus norvegicus (rat)
Description:
Recombinant rat enzyme.
Residue:
377
Sequence:
MAATEGVGESAPGGEPGQPEQPPPPPPPPPAQQPQEEEMAAEAGEAAASPMDDGFLSLDSPTYVLYRDRAEWADIDPVPQNDGPSPVVQIIYSEKFRDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLRSLQKDLQEEMNYIIAIIEEQPKNYQVWHHRRVLVEWLKDPSQELEFIADILNQDAKNYHAWQHRQWVIQEFRLWDNELQYVDQLLKEDVRNNSVWNQRHFVISNTTGYSDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSRYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSRESDIPASV
  
Inhibitor
Name:
BDBM13335
Synonyms:
N-tert-Butyl-2-[[6-cyano-1-(3-methyl-3H-imidazol-4-yl-methyl)-1,2,3,4-tetrahydroquinolin-3-yl]-(1-methyl-1H-imidazole-2-sulfonyl)amino]acetamide | N-tert-butyl-2-({6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl}(1-methyl-1H-imidazole-2-)sulfonamido)acetamide | tetrahydroquinoline (THQ)-based inhibitor 4q
Type:
Small organic molecule
Emp. Form.:
C25H32N8O3S
Mol. Mass.:
524.638
SMILES:
Cn1cncc1CN1CC(Cc2cc(ccc12)C#N)N(CC(=O)NC(C)(C)C)S(=O)(=O)c1nccn1C
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated lamin B peptide substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1715.01
Organism:
n/a
Description:
A human lamin-B carboxy-terminus sequence peptide (biotin-YRASNRSCAIM) is 3H-farnesylated at the cysteine residue when processed by farnesyltransferase.
Residue:
15
Sequence:
ITINYRASNRSCAIM