General Information

General Information

DRAVP ID DRAVPe00758

Peptide Name IN-1

Sequence WQCLTLTHRGFVLLTITVLR

Sequence Length 20

UniProt ID No entry found

Taxon ID None

Source Synthetic construct

Validation Experimentally Validated

Origin Information

Gene Name/ID Not Available

GenBank Not Available

Amino Acid position Not Available

Domain Accession ID Not Available

Nucleotide sequence ID Not Available

Molecular Type Not Available

Chromosomal Position Not Available

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