DRAVP ID  DRAVPs001

Peptide Name   RQ-02

Sequence  DISGINASVVNI8KEIDRLXEVAKNLNESLIDLQELG(K*) 

Sequence Length  37

Original Sequence  DISGINASVVNIQKEIDRLNEVAKNLNESLIDLQELG

Source  Synthetic Construct

Validation   Experimentally Validated

Target Organism  SARS-CoV-2, Ebola, Nipah

Assay  AlphaScreen binding assay

Activity 

• [Ref.38177138]SARS-CoV:IC50=4.5 × 10-8,PV:IC50=1.9 × 10-8 against Wuhan-hu-1 strain,IC50=4.2 × 10-8 against B.1 D614G strain,IC50=2.6 × 10-8 against PV B.1.1.7 strain,IC50=2.4 × 10-8 against PV B.1.135 strain,IC50= against PV 5.3 × 10-9 B.1.1.529.4/5 strain.

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  RQ-01, which exhibits lownanomolar potency across all SARS-CoV-2 strains tested to date.Compared to previously reported HR2-based constructs that weretested in small animals16,20, RQ-01 exhibits markedly improved peptidestability and solubility, enhanced potency and breadth of antiviralactivity, and fully on-resin chemical synthesis, including the lipidationstep, thereby streamlining synthesis and purification for facile itera-tion, lead selection, and upscale. The local tissue persistence of nasallyadministered compound showcases the desirable pharmacologicproperties of stapled lipopeptides, with RQ-01 protecting hamstersfrom SARS-CoV-2-induced weight loss and pulmonary damage

Linear/Cyclic  Cyclic

N-terminal Modification  Acetylation

C-terminal Modification  Free

Special Amino Acid and Stapling Position  Staple location is D and it is choleaterol with peg length is 8

Structure Description  Not Available

Stereochemistry  L

Literature 1

Title   A stapled lipopeptide platform for preventing and treating highly pathogenic viruses of pandemic potential

Pubmed ID   38177138

Reference   Nature communications, 15(1), 274.

Author   Godes, M., Moyer, B. M., Owen, C. D., DaSilva-Jardine, P., Neuberg, D. S., Bowen, R. A., Davey, R. A., & Walensky, L. D. (2024).

DOI   10.1038/s41467-023-44361-1