“Molecular Masks” for ACE2 to Effectively and Safely Block SARS-CoV-2 Virus Entry |
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| Authors: | Satya Prakash Shukla Kwang Bog Cho Vineeta Rustagi Xiang Gao Xinping Fu Shaun Xiaoliu Zhang Bin Guo D. Gomika Udugamasooriya |
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| Affiliation: | 1.Department of Pharmacological & Pharmaceutical Sciences, University of Houston, 4849 Calhoun Rd, Houston, TX 77204-5037, USA; (S.P.S.); (K.B.C.); (V.R.); (X.G.);2.Department of Biology and Biochemistry, University of Houston, 3455 Cullen Blvd, Houston, TX 77204-5037, USA; (X.F.); (S.X.Z.);3.MD Anderson Cancer Center, Department of Cancer Systems Imaging, 1881 East Road, Houston, TX 77030-4009, USA |
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| Abstract: | Coronavirus Disease 2019 (COVID-19) remains a global health crisis, despite the development and success of vaccines in certain countries. Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the virus that causes COVID-19, uses its spike protein to bind to the human cell surface receptor angiotensin-converting enzyme 2 (ACE2), which allows the virus to enter the human body. Using our unique cell screening technology, we identified two ACE2-binding peptoid compounds and developed dimeric derivatives (ACE2P1D1 and ACE2P2D1) that effectively blocked spike protein-ACE2 interaction, resulting in the inhibition of SARS-CoV-2 pseudovirus entry into human cells. ACE2P1D1 and ACE2P2D1 also blocked infection by a D614G mutant pseudovirus. More importantly, these compounds do not decrease ACE2 expression nor its enzyme activity (which is important in normal blood pressure regulation), suggesting safe applicability in humans |
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| Keywords: | SARS-CoV-2 ACE2 receptor peptoids |
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