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TargetProtein farnesyltransferase
LigandBDBM13363
Substrate/Competitorbiotinylated lamin B peptide substrate
Meas. Tech.PFT IC50 Determination
pH7.5±n/a
Temperature310.15±n/a K
IC50 2500±1400 nM
Citation Santagada, VCaliendo, GSeverino, BLavecchia, APerissutti, EFiorino, FZampella, ASepe, VCalifano, DSantelli, GNovellino, E Synthesis, pharmacological evaluation, and molecular modeling studies of novel peptidic CAAX analogues as farnesyl-protein-transferase inhibitors. J Med Chem49:1882-90 (2006) [PubMed]  Article
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Protein farnesyltransferase
Name:Protein farnesyltransferase
Synonyms:CAAX farnesyltransferase alpha subunit | FTase-alpha | GGTase-I-alpha | Geranylgeranyl Transferase (GGTase-I) Chain A | Protein Farnesyltransferase (PFT) Chain A | 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:
MAAADGVGEAAQGGDPGQPEPPPPPQPHPPPPPPQPPQEEAAAASPIDDGFLSLDSPTYV
LYRDRPEWADIDPVPQNDGPNPVVQIIYSEKFQDVYDYFRAVLQRDERSERAFKLTRDAI
ELNAANYTVWHFRRVLLKSLQKDLHEEMNYISAIIEEQPKNYQVWHHRRVLVEWLRDPSQ
ELEFIADILTQDAKNYHAWQHRQWVIQEFKLWDNELQYVDQLLKEDVRNNSVWNQRYFVI
SNTTGYNDRAILEREVQYTLEMIKLVPHNESAWNYLKGILQDRGLSKYPNLLNQLLDLQP
SHSSPYLIAFLVDIYEDMLENQCDNKEDILNKALELCEILAKEKDTIRKEYWRYIGRSLQ
SKHSTESDPPTNVQQ
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BDBM13363
NameBDBM13363
Synonyms:(2S)-2-[(2S)-2-[(2S)-2-[(2R)-2-amino-3-sulfanylpropanamido]-3-methylbutanamido]-3-(4-hydroxy-2,5-dimethylphenyl)propanamido]-4-(methylsulfanyl)butanoic acid | CAAX Analogue 6 | Compound VI
TypeSmall organic molecule
Emp. Form.C24H38N4O6S2
Mol. Mass.542.712
SMILESCSCC[C@H](NC(=O)[C@H](Cc1cc(C)c(O)cc1C)NC(=O)[C@@H](NC(=O)[C@@H](N)CS)C(C)C)C(O)=O |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
biotinylated lamin B peptide 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:
biotin-YRASNRSCAIM