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Target
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM13310
Substrate
biotinylated lamin B peptide substrate
Meas. Tech.
PFT IC50 Determination
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
43±n/a nM
Citation
Glenn, MP; Chang, SY; Horney, C; Rivas, K; Yokoyama, K; Pusateri, EE; Fletcher, S; Cummings, CG; Buckner, FS; Pendyala, PR; Chakrabarti, D; Sebti, SM; Gelb, M; Van Voorhis, WC; Hamilton, AD Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites. J Med Chem 49:5710-27 (2006) [PubMed] Article
More Info.:
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:
BDBM13310
Synonyms:
N-(2-{(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino}ethyl)-1-methyl-N-(pyridin-2-ylmethyl)-1H-imidazole-4-sulfonamide | N-{2-[(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl}-1-methyl-N-(pyridin-2-ylmethyl)-1H-imidazole-4-sulfonamide | Sulfonamide 12aa
Type:
Small organic molecule
Emp. Form.:
C24H26N8O2S
Mol. Mass.:
490.581
SMILES:
Cn1cnc(c1)S(=O)(=O)N(CCN(Cc1cncn1C)c1ccc(cc1)C#N)Cc1ccccn1
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