[Webinar] How to better optimize an oncology drug discovery program
Register for this webinar discussing how conventional and innovative integrated technological skills should be incorporated into an oncology program.
Read more Authors:
Philippe Karoyan, Vincent Vieillard, Luis Gómez-Morales, Estelle Odile, Amélie Guihot, Charles-Edouard Luyt, Alexis Denis, Pascal Grondin & Olivier Lequin
Abstract:
In light of the recent accumulated knowledge on SARS-CoV-2 and its mode of human cells invasion, the binding of viral spike glycoprotein to human Angiotensin Converting Enzyme 2 (hACE2) receptor plays a central role in cell entry. We designed a series of peptides mimicking the N-terminal helix of hACE2 protein which contains most of the contacting residues at the binding site, exhibiting a high helical folding propensity in aqueous solution. Our best peptide-mimics are able to block SARS-CoV-2 human pulmonary cell infection with an inhibitory concentration (IC50) in the nanomolar range upon binding to the virus spike protein with high affinity. These first-in-class blocking peptide mimics represent powerful tools that might be used in prophylactic and therapeutic approaches to fight the coronavirus disease 2019 (COVID-19).
Ref: Communications Biology volume 4, Article number: 197 (2021)