General Information


DRAVP ID  DRAVPe00020

Peptide Name   NL6-L5A

Sequence  TAYFALKLAGRW

Sequence Length  12

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=115±21 µM);inhibition of strand transfer catalyzed by integrase(IC50=51±7 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  DRAVPe00020

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  Free

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C68H101N17O15

Absent amino acids  CDEHIMNPQSV

Common amino acids  A

Mass  1396.65

Pl  9.99

Basic residues  2

Acidic residues  0

Hydrophobic residues  7

Net charge  2

Boman Index  -166

Hydrophobicity  34.17

Aliphatic Index  90

Half Life 

  •     Mammalian:7.2 hour
  •     Yeast:>20 hour
  •     E.coli:>10 hour

Extinction Coefficient cystines  6990

Absorbance 280nm  635.45

Polar residues  3



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