DRAVP ID  DRAVPe00058

Peptide Name   4286(derived from DNA-polymerase domain of HIV-1 RT (20-mers))

Sequence  KILEPFRKQNPDIVIYQYMD

Sequence Length  20

UniProt ID  No entry found

Source  Synthetic construct(derived from HIV-1 Reverse Transcriptase)

Target Organism  HIV

Assay  Dot-blot assay

Activity 

• [Ref.15790559]HIV-1:Inhibition of 3′-processing catalyzed by integrase(IC50=4.8 µM);inhibition of strand transfer catalyzed by integrase(IC50=4.5 µM);inhibition of disintegration catalyzed by integrase(IC50=9.4 µM);
• HIV-1:the level of peptide binding to HIV integrase is high.

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  Two viral encoded enzymes(reverse transcriptase and integrase) play central roles in the early stages of the replication of retroviruses and retrotransposons.The peptide derived from the RT DNA polymerase domain inhibits all three integrase-associated activities (3′-end processing, strand transfer, and disintegration) and inhibit virus replication.

PDB ID  None

Predicted Structure Download  DRAVPe00058

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  Free

Other Modification  None

Stereochemistry  L

Literature 1

Title   Peptides derived from the reverse transcriptase of human immunodeficiency virus type 1 as novel inhibitors of the viral integrase.

Pubmed ID   15790559

Reference   J Biol Chem. 2005 Jun 10;280(23):21987-96.

Author   Oz Gleenberg I, Avidan O, Goldgur Y, Herschhorn A, Hizi A.

DOI   10.1074/jbc.M414679200