General Information


DRAVP ID  DRAVPs021

Peptide Name   hACE2(21-55)F32K-A36E

Sequence  IEEQAKTFLDKⓀNHEⒺEDLFYQSSLASWNYNTNIT

Sequence Length  35

Original Sequence  IEEQAKTFLDKNHEEEDLFYQSSLASWNYNTNIT

Source  Synthetic Construct

Validation   Experimentally Validated



Activity Information


Target Organism  SARS-CoV-2

Assay  Inhibition assay

Activity 

  • [Ref.33651072]Virus:SARS-CoV-2:inhibition of SARS-CoV-2 Spike protein-hACE2 complex formation(IC50=28.4 μM).

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

Cytotoxicity  No cytotoxicity information found in the reference(s) presented

Binding Target  membrane

Mechanism  The stapled peptide inhibit the RBD-hACE2 complex formation, and hACE2 α1-helix-based peptidomimetics could potentially prevent SARS-CoV-2 from entering the human cells through hACE2 and thus inhibit subsequent viral replication.



Structure Information


Linear/Cyclic  Cyclic

N-terminal Modification  Free

C-terminal Modification  Free

Special Amino Acid and Stapling Position  Ⓚ (12) and Ⓔ (16) are corss-linked by lactam stapling.

Structure Description  ①6-13% α-helical content in 10 mM PBS at pH 7.4 and 298 K.②11-52% α-helical content in 10 mM PBS at pH 7.4 with 30% TFE at 298 K.

Stereochemistry  L



Literature Information


Literature 1

Title   Targeting SARS-CoV-2 spike protein by stapled hACE2 peptides.

Pubmed ID   33651072

Reference   Chem Commun (Camb). 2021 Apr 4;57(26):3283-3286.

Author   Maas MN , Hintzen JCJ , Löffler PMG , Mecinović J .

DOI   https://doi.org/10.1039/D0CC08387A