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Target
ATP-dependent RNA helicase RhlE
Ligand
BDBM31426
Substrate
biotinylated lamin B peptide substrate
Meas. Tech.
PfPFT IC50 Determination
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
70.0±n/a nM
Citation
 Hast, MA; Fletcher, S; Cummings, CG; Pusateri, EE; Blaskovich, MA; Rivas, K; Gelb, MH; Van Voorhis, WC; Sebti, SM; Hamilton, AD; Beese, LS Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase. Chem Biol 16:181-92 (2009) [PubMed]  Article 
Target
Name:
ATP-dependent RNA helicase RhlE
Synonyms:
Protein Farnesyltransferase (PFT) | Protein prenyltransferase, alpha subunit
Type:
Enzyme
Mol. Mass.:
54781.31
Organism:
Plasmodium falciparum (malaria parasite P. falciparum)
Description:
Q5E175
Residue:
500
Sequence:
MGFTSLGLSAPILKAVEEQGYSTPSPIQLQAIPAVIEGKDVMAAAQTGTGKTAGFTLPLLERLSNGPKRKFNQVRALVLTPTRELAAQVHESVEKYSKNLPLTSDVVFGGVKVNPQMQRLRRGVDVLVATPGRLLDLANQNAIKFDQLEILVLDEADRMLDMGFIHDIKKILAKLPKNRQNLLFSATFSDEIRQLAKGLVKDPVEISVAKRNTTAETVEQSVYVMDKGRKPKVLTKLIKDNDWKQVLVFSKTKHGANRLAKTLEEKGVSAAAIHGNKSQGARTKALANFKSGQVRVLVATDIAARGLDIEQLPQVINVDLPKVPEDYVHRIGRTGRAGATGKAISFVSEDEAKELFAIERLIQKVLPRHVLEGFEPVNKVPESKLDTRPIKPKKPKKPKAPRVEHKDGQRSGENRNGNKQGAKQGQKPATKRTPTNNPSGKKEGTDSDKKKRPFSGKPKTKGTGENRGNGSNFGKSKSTPKSDVKPRRQGPRPARKPKAN
  
Inhibitor
Name:
BDBM31426
Synonyms:
ethylenediamine scaffold, 10
Type:
Small organic molecule
Emp. Form.:
C40H48N6O6S
Mol. Mass.:
740.911
SMILES:
Cn1cncc1CN(CCN(CC1CCN(CC1)C(=O)OC(C)(C)C)S(=O)(=O)c1ccccc1-c1cccc(CCC(O)=O)c1)c1ccc(cc1)C#N
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