DRAVP ID  DRAVPs028

Peptide Name   5

Sequence  ISF c'ELADYYC'ESGS 

Sequence Length  14

Original Sequence  ISFCELADYYCESGS

Source  Synthetic Construct

Validation   Experimentally Validated

Target Organism  HIV-1

Assay  Multi-Cycle Infection Assay

Activity 

• [Ref:24613163]HIV:IC50=4.1 ± 0.3μM in MT-2 cells, IC50=1.4 ± 0.2μM in TZM-b1 cells.

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

Cytotoxicity 

• [Ref:24613163]HIV:CC50=~26µM in MT-2 cells,CC50=>52µM in TZM b1 cells

Binding Target  Capsid CTD and gp125

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.

Linear/Cyclic  Cyclic

N-terminal Modification  Free

C-terminal Modification  Free

Special Amino Acid and Stapling Position  c' and C' denote the Bph-linked D-cysteine and L-cysteine, respectively.

Structure Description  Not Available

Stereochemistry  L

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