2022
DOI: 10.3390/molecules27072070
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Structure/Function Analysis of Truncated Amino-Terminal ACE2 Peptide Analogs That Bind to SARS-CoV-2 Spike Glycoprotein

Abstract: The global burden of the SARS-CoV-2 pandemic is thought to result from a high viral transmission rate. Here, we consider mechanisms that influence host cell–virus binding between the SARS-CoV-2 spike glycoprotein (SPG) and the human angiotensin-converting enzyme 2 (ACE2) with a series of peptides designed to mimic key ACE2 hot spots through adopting a helical conformation analogous to the N-terminal α1 helix of ACE2, the region experimentally shown to bind to the SARS-CoV-2 receptor-binding domain (RBD). The a… Show more

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Cited by 3 publications
(2 citation statements)
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References 78 publications
(102 reference statements)
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“…Compared to unmodified L163, the L163 analogs exhibited enhanced stability against pH, plasma, and trypsin degradation. Furthermore, Mackin et al 76 conducted structural and functional analysis of ACE2 peptide analogs targeting the spike glycoprotein of SARS‐CoV‐2. They found that among the N‐terminal modifications of the peptide, succinimide acylation exhibited stronger binding affinity compared to the native ACE2 peptide.…”
Section: Modification Of Peptides and Pasmentioning
confidence: 99%
“…Compared to unmodified L163, the L163 analogs exhibited enhanced stability against pH, plasma, and trypsin degradation. Furthermore, Mackin et al 76 conducted structural and functional analysis of ACE2 peptide analogs targeting the spike glycoprotein of SARS‐CoV‐2. They found that among the N‐terminal modifications of the peptide, succinimide acylation exhibited stronger binding affinity compared to the native ACE2 peptide.…”
Section: Modification Of Peptides and Pasmentioning
confidence: 99%
“…Targeting ACE2 was considered the obvious first-choice target for prophylactic and therapeutic interventions aiming to block virus accessibility to respiratory cells early on in infection [97,98]. Several strategies have been evaluated in vitro and in vivo with varied success, including decoy or soluble ACE2 molecules, pseudoligands with a high ACE2 affinity and blocking antibodies [67,99,100].…”
Section: Ace2 and Tmprss2 As Candidate Targets For Antiviral Therapymentioning
confidence: 99%