General Information

General Information

DRAVP ID DRAVPe00758

Peptide Name IN-1

Sequence WQCLTLTHRGFVLLTITVLR

Sequence Length 20

UniProt ID No entry found

Source Synthetic construct

Activity Information

Target Organism HIV

Assay MAGI assay

Activity

[Ref.18201721]HIV-1:Inhibition of 3′-processing catalyzed by integrase(IC50=38 µM);inhibition of strand transfer catalyzed by integrase(IC50=12 µM).
[Ref.19850483]HIV-1:inhibition of integrase catalytic activity(77% inhibition at 62.5μM);inhibition of virus replication in TZM-bl cells(70% inhibition at 62.5μM);inhibition of intergration(63% inhibition at 62.5μM).

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

Cytotoxicity

[Ref.18201721]No cytotixic against HeLa cells and H9 T-lymphocyte cultured cells up to ~62.5 μM.

Binding Target Integrase

Mechanism The peptide can inhibit integrase and thus inhibit virus replication.

Structure Information

PDB ID None

Predicted Structure Download DRAVPe00758

Linear/Cyclic Linear

N-terminal Modification Free

C-terminal Modification Free

Other Modification None

Stereochemistry L

Physicochemical Information

Formula C110H180N30O26S

Absent amino acids ADEKMNPSY

Common amino acids L

Mass 2370.88

Pl 10.35

Basic residues 3

Acidic residues 0

Hydrophobic residues 10

Net charge 3

Boman Index -519

Hydrophobicity 87

Aliphatic Index 146

Half Life

Mammalian:2.8 hour
Yeast:3 min
E.coli:2 min

Extinction Coefficient cystines 5500

Absorbance 280nm 289.47

Polar residues 6

Literature Information

Literature 1

Title Correlation between shiftide activity and HIV-1 integrase inhibition by a peptide selected from a combinatorial library.

Pubmed ID 18201721

Reference J Mol Biol. 2008 Feb 29;376(4):971-82.

Author Armon-Omer A, Levin A, Hayouka Z, Butz K, Hoppe-Seyler F, Loya S, Hizi A, Friedler A, Loyter A.

DOI 10.1016/j.jmb.2007.11.095

Literature 2

Title Peptide inhibitors of HIV-1 integrase: from mechanistic studies to improved lead compounds.

Pubmed ID 19850483

Reference Bioorg Med Chem. 2009 Nov 15;17(22):7635-42.

Author Maes M, Levin A, Hayouka Z, Shalev DE, Loyter A, Friedler A.

DOI 10.1016/j.bmc.2009.09.053