Neutralizing SARS-CoV-2 by dimeric side chain-to-side chain cross-linked ACE2 peptide mimetics.

Zhang, Yan-Ni; Zhang, Yuwei; Su, Shan; Zhu, Han-Ying; Xu, Wei; Wang, Lu; Wu, Meng; Chen, Kai; Yu, Fei-Qiang; Xi, Tong-Kuai; Zhou, Qin; Xie, You-Hua; Qin, Ximing; Ge, Honghua; Lu, Lu; Qing, Jie; Fang, Ge-Min

Zhang, Yan-Ni; Zhang, Yuwei; Su, Shan; Zhu, Han-Ying; Xu, Wei; Wang, Lu; Wu, Meng; Chen, Kai; Yu, Fei-Qiang; Xi, Tong-Kuai; Zhou, Qin; Xie, You-Hua; Qin, Ximing; Ge, Honghua; Lu, Lu; Qing, Jie; Fang, Ge-Min.

Zhang YN; Department of Health Sciences, Institutes of Physical Science and Information Technology, Anhui University, Hefei 230601, P. R. China. fanggm@ahu.edu.cn.
Zhang Y; National Traditional Chinese Medicine Clinical Research Base, The Affiliated Traditional Chinese Medicine Hospital of Southwest Medical University, Luzhou, 646000, P. R. China. qing282420@163.com.
Su S; Key Laboratory of Medical Molecular Virology (MOE/NHC/CAMS), School of Basic Medical Sciences and Biosafety Level 3 Laboratory, Shanghai Institute of Infectious Disease and Biosecurity, Fudan University, Shanghai 200032, P. R. China. lul@fudan.edu.cn.
Zhu HY; Department of Health Sciences, Institutes of Physical Science and Information Technology, Anhui University, Hefei 230601, P. R. China. fanggm@ahu.edu.cn.
Xu W; Key Laboratory of Medical Molecular Virology (MOE/NHC/CAMS), School of Basic Medical Sciences and Biosafety Level 3 Laboratory, Shanghai Institute of Infectious Disease and Biosecurity, Fudan University, Shanghai 200032, P. R. China. lul@fudan.edu.cn.
Wang L; National Traditional Chinese Medicine Clinical Research Base, The Affiliated Traditional Chinese Medicine Hospital of Southwest Medical University, Luzhou, 646000, P. R. China. qing282420@163.com.
Wu M; Department of Health Sciences, Institutes of Physical Science and Information Technology, Anhui University, Hefei 230601, P. R. China. fanggm@ahu.edu.cn.
Chen K; Department of Health Sciences, Institutes of Physical Science and Information Technology, Anhui University, Hefei 230601, P. R. China. fanggm@ahu.edu.cn.
Yu FQ; Department of Health Sciences, Institutes of Physical Science and Information Technology, Anhui University, Hefei 230601, P. R. China. fanggm@ahu.edu.cn.
Xi TK; Department of Health Sciences, Institutes of Physical Science and Information Technology, Anhui University, Hefei 230601, P. R. China. fanggm@ahu.edu.cn.
Zhou Q; Department of Health Sciences, Institutes of Physical Science and Information Technology, Anhui University, Hefei 230601, P. R. China. fanggm@ahu.edu.cn.
Xie YH; Key Laboratory of Medical Molecular Virology (MOE/NHC/CAMS), School of Basic Medical Sciences and Biosafety Level 3 Laboratory, Shanghai Institute of Infectious Disease and Biosecurity, Fudan University, Shanghai 200032, P. R. China. lul@fudan.edu.cn.
Qin X; Department of Health Sciences, Institutes of Physical Science and Information Technology, Anhui University, Hefei 230601, P. R. China. fanggm@ahu.edu.cn.
Ge H; Department of Health Sciences, Institutes of Physical Science and Information Technology, Anhui University, Hefei 230601, P. R. China. fanggm@ahu.edu.cn.
Lu L; Key Laboratory of Medical Molecular Virology (MOE/NHC/CAMS), School of Basic Medical Sciences and Biosafety Level 3 Laboratory, Shanghai Institute of Infectious Disease and Biosecurity, Fudan University, Shanghai 200032, P. R. China. lul@fudan.edu.cn.
Qing J; National Traditional Chinese Medicine Clinical Research Base, The Affiliated Traditional Chinese Medicine Hospital of Southwest Medical University, Luzhou, 646000, P. R. China. qing282420@163.com.
Fang GM; Department of Health Sciences, Institutes of Physical Science and Information Technology, Anhui University, Hefei 230601, P. R. China. fanggm@ahu.edu.cn.

Chem Commun (Camb) ; 58(11): 1804-1807, 2022 Feb 03.

Artículo en Inglés | MEDLINE | ID: covidwho-1639537

ABSTRACT

ABSTRACT

We present the finding of a dimeric ACE2 peptide mimetic designed through side chain cross-linking and covalent dimerization. It has a binding affinity of 16 nM for the SARS-CoV-2 spike RBD, and effectively inhibits the SARS-CoV-2 pseudovirus in Huh7-hACE2 cells with an IC50 of 190 nM and neutralizes the authentic SARS-CoV-2 in Caco2 cells with an IC50 of 2.4 µM. Our study should provide a new insight for the optimization of peptide-based anti-SARS-CoV-2 inhibitors.

Asunto(s)

Antivirales/farmacología; Fragmentos de Péptidos/farmacología; Peptidomiméticos/farmacología; SARS-CoV-2/efectos de los fármacos; Secuencia de Aminoácidos; Enzima Convertidora de Angiotensina 2/química; Antivirales/síntesis química; Antivirales/metabolismo; Línea Celular Tumoral; Humanos; Pruebas de Sensibilidad Microbiana; Fragmentos de Péptidos/síntesis química; Fragmentos de Péptidos/metabolismo; Peptidomiméticos/síntesis química; Peptidomiméticos/metabolismo; Unión Proteica; Dominios Proteicos; Glicoproteína de la Espiga del Coronavirus/química; Glicoproteína de la Espiga del Coronavirus/metabolismo

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Texto completo: Disponible Colección: Bases de datos internacionales Base de datos: MEDLINE Asunto principal: Antivirales / Fragmentos de Péptidos / Peptidomiméticos / SARS-CoV-2 Tipo de estudio: Ensayo controlado aleatorizado Límite: Humanos Idioma: Inglés Revista: Chem Commun (Camb) Asunto de la revista: Química Año: 2022 Tipo del documento: Artículo

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