General Information


DRAVP ID  DRAVPe00027

Peptide Name   NL9-C2A

Sequence  AAWWAGIKQEF

Sequence Length  11

UniProt ID  No entry found

Source  Synthetic construct(derived from HIV-1 integrase)



Activity Information


Target Organism  HIV

Assay  Integrase Assay

Activity 

  • [Ref.16854053]HIV-1:Inhibition of 3′-processing catalyzed by integrase(IC50=277±47 µM);inhibition of strand transfer catalyzed by integrase(IC50=311±19 µM).

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  HIV-1 integrase (IN) is essential for viral replication. Following reverse transcription of the RNA into DNA by HIV-1 reverse transcriptase, IN integrates the viral DNA into the host genome.The peptide could inbibit integrase(By inhibiting the two steps of IN catalysis: 3′-processing and strand transfer).



Structure Information


PDB ID  None

Predicted Structure Download  DRAVPe00027

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  Free

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C64H87N15O15

Absent amino acids  CDHLMNPRSTVY

Common amino acids  A

Mass  1306.49

Pl  6.05

Basic residues  1

Acidic residues  1

Hydrophobic residues  7

Net charge  0

Boman Index  103

Hydrophobicity  -3.64

Aliphatic Index  62.73

Half Life 

  •     Mammalian:4.4 hour
  •     Yeast:>20 hour
  •     E.coli:>10 hour

Extinction Coefficient cystines  11000

Absorbance 280nm  1100

Polar residues  1



Literature Information


Literature 1

Title   Sequence-based design and discovery of peptide inhibitors of HIV-1 integrase: insight into the binding mode of the enzyme.

Pubmed ID   16854053

Reference   J Med Chem. 2006 Jul 27;49(15):4477-86.

Author   Li HY, Zawahir Z, Song LD, Long YQ, Neamati N.

DOI   10.1021/jm060307u