Target

Ligand

Substrate

Meas. Tech.

PFT IC50 Determination

pH

7.5±n/a

Temperature

310.15±n/a K

Citation

 Santagada, V; Caliendo, G; Severino, B; Lavecchia, A; Perissutti, E; Fiorino, F; Zampella, A; Sepe, V; Califano, D; Santelli, G; Novellino, E Synthesis, pharmacological evaluation, and molecular modeling studies of novel peptidic CAAX analogues as farnesyl-protein-transferase inhibitors. J Med Chem 49:1882-90 (2006) [PubMed]  Article Copy BDB DOI

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Name:

Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha

Synonyms:

CAAX farnesyltransferase alpha subunit | FNTA | FNTA_BOVIN | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Protein Farnesyltransferase (PFT) Chain A | Protein farnesyltransferase | Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit | Ras proteins prenyltransferase alpha | Type I protein geranyl-geranyltransferase alpha subunit

Type:

Enzyme

Mol. Mass.:

43827.38

Organism:

Bos taurus (bovine)

Description:

The enzyme was purified from a bovine brain homogenate by sequential ammonium sulfate fractionation and affinity chromatography.

Residue:

375

Sequence:

MAAADGVGEAAQGGDPGQPEPPPPPQPHPPPPPPQPPQEEAAAASPIDDGFLSLDSPTYVLYRDRPEWADIDPVPQNDGPNPVVQIIYSEKFQDVYDYFRAVLQRDERSERAFKLTRDAIELNAANYTVWHFRRVLLKSLQKDLHEEMNYISAIIEEQPKNYQVWHHRRVLVEWLRDPSQELEFIADILTQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVISNTTGYNDRAILEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQPSHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQSKHSTESDPPTNVQQ

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Blast E-value cutoff:

Name:

BDBM13371

Synonyms:

CAAX Analogue 14 | Compound XIV | methyl (2S)-2-[(2S)-2-[(2S)-2-[(2R)-2-amino-3-sulfanylpropanamido]-3-methylbutanamido]-3-(4-hydroxy-2,3-dimethylphenyl)propanamido]-4-(methylsulfanyl)butanoate

Type:

Small organic molecule

Emp. Form.:

C25H40N4O6S2

Mol. Mass.:

556.738

SMILES:

COC(=O)[C@H](CCSC)NC(=O)[C@H](Cc1ccc(O)c(C)c1C)NC(=O)[C@@H](NC(=O)[C@@H](N)CS)C(C)C |r|

Structure:

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Similarity to this molecule at least:

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