DRAVP ID  DRAVPe00071

Peptide Name   4321(derived from the RNase H domain of HIV-1 RT (20-mes)),64(derived from the HIV-1 HXB2 Pol region of the viral genome)

Sequence  ELVNQIIEQLIKKEKVYLAW

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=6.9 µM);inhibition of strand transfer catalyzed by integrase(IC50=5 µM);inhibition of disintegration catalyzed by integrase(IC50>100 µM);
• HIV-1:the level of peptide binding to HIV integrase is high.
• [Ref.16879966]HIV:inhibition of 3′-processing catalyzed by wild-type integrase(IC50=15±2 µM);inhibition of strand transfer catalyzed by wild-type integrase(IC50=14±4 µM);inhibition of 3′-processing catalyzed by soluble mutant integrase(IC50=113±11 µM);inhibition of strand transfer catalyzed by soluble mutant integrase(IC50=83±5 µM);inhibition of 3′-processing catalyzed by C130S integrase(IC50=136±5 µM);inhibition of strand transfer catalyzed by C130S integrase(IC50=7±1 µM);inhibition of 3′-processing catalyzed by C130S integrase(IC50=45 µM);inhibition of strand transfer catalyzed by C130A integrase(IC50=15 µM).
• NOTE:soluble mutant,C130S,C130S integrase are mutant IN.

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 RNase H domain of HIV-1 RT inhibits integrase-associated activities (3′-end processing and strand transfer) and inhibit virus replication.

PDB ID  None

Predicted Structure Download  DRAVPe00071

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

Literature 2

Title   Inhibition of HIV-1 integrase activity by synthetic peptides derived from the HIV-1 HXB2 Pol region of the viral genome.

Pubmed ID   16879966

Reference   Bioorg Med Chem Lett. 2006 Oct 1;16(19):5199-202.

Author   Zawahir Z, Neamati N.

DOI   10.1016/j.bmcl.2006.07.022