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Target
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM13321
Substrate
biotinylated lamin B peptide substrate
Meas. Tech.
PfPFT and Rat PFT IC50 Determination
IC50
0.8±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:
BDBM13321
Synonyms:
1-Methyl-1H-imidazole-4-sulfonic Acid (2-Bromoallyl)-[6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]amide | N-(2-bromoprop-2-en-1-yl)-N-{6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl}-1-methyl-1H-imidazole-4-sulfonamide | tetrahydroquinoline (THQ)-based inhibitor 4c
Type:
Small organic molecule
Emp. Form.:
C22H24BrN7O2S
Mol. Mass.:
530.441
SMILES:
Cn1cnc(c1)S(=O)(=O)N(CC(Br)=C)C1CN(Cc2cncn2C)c2ccc(cc2C1)C#N
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