General Information


DRAVP ID  DRAVPs023

Peptide Name   CAI Stapled (Peptide 1)

Sequence  ITFEDLLDYYGP

Sequence Length  12

Original Sequence  ITFEDLLDYYGP

Source  Synthetic Construct

Validation   Experimentally Validated



Activity Information


Target Organism  HIV-1

Assay  Multi-Cycle Infection Assay

Activity 

  • [Ref:24613163]HIV-1:IC50=>135μM in MT-2 cells, IC50=>135μM in TZM-b1 cells.

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

Cytotoxicity 

  • [Ref:24613163]HIV-1:CC50=>135µM in MT-2 cells,CC50=>135µM in TZM b1 cells

Binding Target  Capsid CTD and gp120

Mechanism  CAI peptide binds to the C-terminal domain of HIV capsid protein as well as envelop glycoprotein gp120 with low micromolar binding affinities, and as a result, inhibits both the HIV-1 virus entry and the virus assembly.



Structure Information


Linear/Cyclic  Cyclic

N-terminal Modification  Free

C-terminal Modification  Free

Special Amino Acid and Stapling Position  Biphenyl staple (i+7)

Structure Description  Not Available

Stereochemistry  L



Literature Information


Literature 1

Title   Design of antiviral stapled peptides containing a biphenyl cross-linker

Pubmed ID   24613163

Reference   Bioorg Med Chem Lett. 2014 Apr 1;24(7):1748-51.

Author   Muppidi A, Zhang H, Curreli F, Li N, Debnath AK, Lin Q.

DOI   10.1016/j.bmcl.2014.02.038