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Target
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha
Ligand
BDBM13370
Substrate
biotinylated lamin B peptide substrate
Meas. Tech.
PFT IC50 Determination
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
10200±2600 nM
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 
Target
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
  
Inhibitor
Name:
BDBM13370
Synonyms:
(2S)-2-[(2R)-3-(4-hydroxy-2,5-dimethylphenyl)-2-[(2S)-2-[(2R)-2-formamido-3-sulfanylpropanamido]-3-methylbutanamido]propanamido]-4-(methylsulfanyl)butanoic acid | CAAX Analogue 13 | Compound XIII
Type:
Small organic molecule
Emp. Form.:
C25H38N4O7S2
Mol. Mass.:
570.722
SMILES:
CSCC[C@H](NC(=O)[C@@H](Cc1cc(C)c(O)cc1C)NC(=O)[C@@H](NC(=O)[C@H](CS)NC=O)C(C)C)C(O)=O |r|
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