General Information


DRAVP ID  DRAVPe01980

Peptide Name   LEDGF/p75 (355-377)

Sequence  IHAEIKNSLKIDNLDVNRCIEAL

Sequence Length  23

UniProt ID  O75475 

Source  Synthetic construct



Activity Information


Target Organism  HIV

Assay  IN enzymatic assay

Activity 

  • [Ref.18331842]Human immunodeficiency virus (HIV): Inhibition of integrase activity (3' end processing)(IC50=165±28 µM); inhibition of integrase activity(strand transfer)(IC50=153±28 µM).

Hemolytic Activity  No hemolysis information or data found in the reference(s) presented in this entry

Cytotoxicity 

  • No cytotoxicity information or data found in the reference(s) presented in this entry

Binding Target  Integrase

Mechanism  The LEDGF/p75 peptide modestly inhibited IN catalysis and was dependent on IN–DNA assembly. The peptide was also effective at disrupting LEDGF/p75–IN complex formation.



Structure Information


PDB ID  None

Predicted Structure Download  No predicted structure available

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  Free

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C113H193N33O36S

Absent amino acids  FGMPQTWY

Common amino acids  I

Mass  2622.03

Pl  5.48

Basic residues  4

Acidic residues  4

Hydrophobic residues  10

Net charge  0

Boman Index  -4168

Hydrophobicity  -4.78

Aliphatic Index  140

Half Life 

  •     Mammalian:20 hour
  •     Yeast:30 min
  •     E.coli:>10 hour

Extinction Coefficient cystines  0

Absorbance 280nm  0

Polar residues  5



Literature Information


Literature 1

Title   Inhibitory profile of a LEDGF/p75 peptide against HIV-1 integrase: insight into integrase-DNA complex formation and catalysis.

Pubmed ID   18331842

Reference   FEBS Lett. 2008 Apr 30;582(10):1425-30.

Author   Al-Mawsawi LQ, Christ F, Dayam R, Debyser Z, Neamati N.

DOI   10.1016/j.febslet.2008.02.076