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

Marijn N. Maas; Jordi C. J. Hintzen; Philipp M. G. Löffler; Jasmin Mecinović

doi:10.1039/D0CC08387A

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

Marijn N. Maas, Jordi C. J. Hintzen, Philipp M. G. Löffler, Jasmin Mecinović^*

^*Corresponding author for this work

Department of Physics, Chemistry and Pharmacy

Research output: Contribution to journal › Journal article › Research › peer-review

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Abstract

SARS-CoV-2 Spike protein RBD interacts with the hACE2 receptor to
initiate cell entry and infection. We set out to develop lactam-based i,
i + 4 stapled hACE2 peptides targeting SARS-CoV-2. In vitro screening
demonstrates the inhibition of the Spike protein RBD-hACE2 complex
formation by the hACE221-55A36K-F40E stapled peptide (IC50: 3.6 lM,
Kd: 2.1 lM), suggesting that hACE2 peptidomimetics could form the
basis for the development of anti-COVID-19 therapeutics.

Original language	English
Journal	Chemical Communications
Volume	57
Issue number	26
Pages (from-to)	3283-3286
ISSN	1359-7345
DOIs	https://doi.org/10.1039/D0CC08387A
Publication status	Published - 2021

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10.1039/D0CC08387ALicence: CC BY

Open Access VersionFinal published version, 2.56 MBLicence: CC BY

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title = "Targeting SARS-CoV-2 spike protein by stapled hACE2 peptides",

abstract = "SARS-CoV-2 Spike protein RBD interacts with the hACE2 receptor toinitiate cell entry and infection. We set out to develop lactam-based i,i + 4 stapled hACE2 peptides targeting SARS-CoV-2. In vitro screeningdemonstrates the inhibition of the Spike protein RBD-hACE2 complexformation by the hACE221-55A36K-F40E stapled peptide (IC50: 3.6 lM,Kd: 2.1 lM), suggesting that hACE2 peptidomimetics could form thebasis for the development of anti-COVID-19 therapeutics.",

author = "Maas, {Marijn N.} and Hintzen, {Jordi C. J.} and L{\"o}ffler, {Philipp M. G.} and Jasmin Mecinovi{\'c}",

year = "2021",

doi = "10.1039/D0CC08387A",

language = "English",

volume = "57",

pages = "3283--3286",

journal = "Chemical Communications",

issn = "1359-7345",

publisher = "Royal Society of Chemistry",

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TY - JOUR

T1 - Targeting SARS-CoV-2 spike protein by stapled hACE2 peptides

AU - Maas, Marijn N.

AU - Hintzen, Jordi C. J.

AU - Löffler, Philipp M. G.

AU - Mecinović, Jasmin

PY - 2021

Y1 - 2021

N2 - SARS-CoV-2 Spike protein RBD interacts with the hACE2 receptor toinitiate cell entry and infection. We set out to develop lactam-based i,i + 4 stapled hACE2 peptides targeting SARS-CoV-2. In vitro screeningdemonstrates the inhibition of the Spike protein RBD-hACE2 complexformation by the hACE221-55A36K-F40E stapled peptide (IC50: 3.6 lM,Kd: 2.1 lM), suggesting that hACE2 peptidomimetics could form thebasis for the development of anti-COVID-19 therapeutics.

AB - SARS-CoV-2 Spike protein RBD interacts with the hACE2 receptor toinitiate cell entry and infection. We set out to develop lactam-based i,i + 4 stapled hACE2 peptides targeting SARS-CoV-2. In vitro screeningdemonstrates the inhibition of the Spike protein RBD-hACE2 complexformation by the hACE221-55A36K-F40E stapled peptide (IC50: 3.6 lM,Kd: 2.1 lM), suggesting that hACE2 peptidomimetics could form thebasis for the development of anti-COVID-19 therapeutics.

U2 - 10.1039/D0CC08387A

DO - 10.1039/D0CC08387A

M3 - Journal article

VL - 57

SP - 3283

EP - 3286

JO - Chemical Communications

JF - Chemical Communications

SN - 1359-7345

IS - 26

ER -

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

Abstract

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