General Information

General Information

DRAVP ID DRAVPe00068

Peptide Name 4318(derived from the RNase H domain of HIV-1 RT (20-mes)),65(derived from the HIV-1 HXB2 Pol region of the viral genome)

Sequence LQDSGLEVNIVTDSQYALGI

Sequence Length 20

UniProt ID No entry found

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

Activity Information

Target Organism HIV

Assay Dot-blot assay

Activity

[Ref.16879966]HIV:inhibition of 3′-processing catalyzed by wild-type integrase(IC50=11±1 µM);inhibition of strand transfer catalyzed by wild-type integrase(IC50=2±1 µM);inhibition of 3′-processing catalyzed by soluble mutant integrase(IC50>167 µM);inhibition of strand transfer catalyzed by soluble mutant integrase(IC50=36±14 µM);inhibition of 3′-processing catalyzed by C130S integrase(IC50=18±3 µM);inhibition of strand transfer catalyzed by C130S integrase(IC50=4±1 µM);inhibition of 3′-processing catalyzed by C130S integrase(IC50>167 µM);inhibition of strand transfer catalyzed by C130A integrase(IC50=20 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.

Structure Information

PDB ID None

Predicted Structure Download DRAVPe00068

Linear/Cyclic Linear

N-terminal Modification Free

C-terminal Modification Free

Other Modification None

Stereochemistry L

Physicochemical Information

Formula C93H151N23O34

Absent amino acids CFHKMPRW

Common amino acids L

Mass 2135.36

Pl 3.49

Basic residues 0

Acidic residues 3

Hydrophobic residues 8

Net charge -3

Boman Index -1511

Hydrophobicity 26

Aliphatic Index 131.5

Half Life

Mammalian:5.5 hour
Yeast:3 min
E.coli:2 min

Extinction Coefficient cystines 1490

Absorbance 280nm 78.42

Polar residues 7

Literature Information

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