Reaction Details |
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Target | Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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Ligand | BDBM13314 |
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Substrate/Competitor | biotinylated lamin B peptide substrate |
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Meas. Tech. | PFT IC50 Determination |
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pH | 7.5±n/a |
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Temperature | 310.15±n/a K |
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IC50 | 180±n/a nM |
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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 Chem49:5710-27 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha |
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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: | MAATEGVGESAPGGEPGQPEQPPPPPPPPPAQQPQEEEMAAEAGEAAASPMDDGFLSLDS
PTYVLYRDRAEWADIDPVPQNDGPSPVVQIIYSEKFRDVYDYFRAVLQRDERSERAFKLT
RDAIELNAANYTVWHFRRVLLRSLQKDLQEEMNYIIAIIEEQPKNYQVWHHRRVLVEWLK
DPSQELEFIADILNQDAKNYHAWQHRQWVIQEFRLWDNELQYVDQLLKEDVRNNSVWNQR
HFVISNTTGYSDRAVLEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSRYPNLLNQLL
DLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIG
RSLQSKHSRESDIPASV
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BDBM13314 |
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biotinylated lamin B peptide substrate |
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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: | |