Article
Pharmacology & Pharmacy
Siew Pheng Lim
Summary: Despite the availability of vaccines and therapeutics, continuous genetic alterations in the SARS-CoV-2 virus pose a persistent threat, especially to immunocompromised and elderly individuals. The virus enters host cells via the interaction of its spike protein (S protein) with different receptors on the cell surface, such as angiotensin-converting enzyme 2 (ACE2). This review discusses therapeutic approaches to block the interaction between SARS-CoV-2 and host cell receptors, as well as the identification of auxiliary entry receptors.
ANTIVIRAL RESEARCH
(2023)
Article
Biology
Ming-Feng He, Jian-Hui Liang, Yan-Ni Shen, Jin-Wen Zhang, Ying Liu, Kuang-Yang Yang, Li-Chu Liu, Junyi Wang, Qian Xie, Chun Hu, Xun Song, Yan Wang
Summary: Glycyrrhizin, an active ingredient in the extract of Glycyrrhizae Radix et Rhizoma, inhibits the entry of SARS-CoV-2 into cells by targeting ACE2.
Article
Biotechnology & Applied Microbiology
Qizhong Lu, Zongliang Zhang, Hexian Li, Kunhong Zhong, Qin Zhao, Zeng Wang, Zhiguo Wu, Donghui Yang, Shuang Sun, Nian Yang, Meijun Zheng, Qiang Chen, Cheng Long, Wenhao Guo, Hui Yang, Chunlai Nie, Aiping Tong
Summary: This study identified four specific nanobodies with antiviral activity against SARS-CoV-2 spike protein, with the heterodimer nanobody Nb91-Nb3-hFc showing the strongest RBD-binding affinity and neutralizing ability. The use of a naive VHH library could be a potential resource for rapid acquisition of antiviral nanobodies, with Nb91-Nb3-hFc showing potential as a therapeutic agent for COVID-19 treatment.
JOURNAL OF NANOBIOTECHNOLOGY
(2021)
Article
Pharmacology & Pharmacy
Khushwant S. Bhullar, Manal A. Nael, Khaled M. Elokely, Steven J. Drews, Jianping Wu
Summary: Two analogs of the bioactive tripeptide IRW, A9 and A14, were found to lower the interaction between SARS-CoV-2 spike protein and ACE2 in vitro. These peptide analogs showed potential as seed candidates for inhibiting SARS-CoV-2 host cell binding through cellular and computational evaluations.
Article
Biochemistry & Molecular Biology
Lei Xie, Sai Shi, Lin Cheng, Binghong Xu, Sen Ma, Jie Liu, Xilin Wu, Yaxin Wang, Sheng Ye
Summary: The continued evolution of SARS-CoV-2 has led to the emergence of variants that are partially resistant to vaccines and antiviral drugs. This study identifies an association between the evolutionary trend of these variants and increased electrostatic interactions between viral spike proteins and ACE2. Virtual screening and experimental assays reveal the antiviral activity of Dauricine, a Traditional Chinese medicine, against different strains of the virus.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Biochemistry & Molecular Biology
Yu Hu, Kefang Liu, Pu Han, Zepeng Xu, Anqi Zheng, Xiaoqian Pan, Yunfei Jia, Chao Su, Lingfeng Tang, Lili Wu, Bin Bai, Xin Zhao, Di Tian, Zhihai Chen, Jianxun Qi, Qihui Wang, George F. Gao
Summary: Bat-origin RshSTT182 and RshSTT200 coronaviruses from Rhinolophus shameli in Southeast Asia (Cambodia) have 92.6% whole-genome identity with SARS-CoV-2 and share identical receptor-binding domains (RBDs). The study determined the structure of the RshSTT182/200 RBD in complex with human angiotensin-converting enzyme 2 (hACE2) and identified key residues influencing receptor binding. RshSTT182 pseudovirus could enter cells by utilizing human, fox, and Rhinolophus affinis ACE2 receptors, and SARS-CoV-2 induces cross-neutralizing antibodies against RshSTT182 pseudovirus.
Article
Biochemistry & Molecular Biology
Shailendra Mani, Anupamjeet Kaur, Kamini Jakhar, Geetika Kumari, Sudipta Sonar, Amit Kumar, Sudesna Das, Santosh Kumar, Vijay Kumar, Rakesh Kundu, Anil Kumar Pandey, Umesh Prasad Singh, Tanmay Majumdar
Summary: Highly mutated SARS-CoV-2 plays a crucial role in causing COVID-19. The spike protein's receptor binding domain (RBD) can interact with human dipeptidyl peptidase 4 (DPP4) to facilitate virus entry, in addition to the usual ACE2-RBD binding route. By using DPP4 inhibitors, such as sitagliptin and linagliptin, to inhibit the catalytic activity of DPP4, the growth of various SARS-CoV-2 variants can be impeded. However, these drugs do not affect the enzymatic activity of PLpro and Mpro. This study suggests that selectively blocking the interaction between RBD and both DPP4 and ACE2 by sitagliptin and linagliptin could be a potential strategy to prevent viral replication.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Microbiology
Ting Wang, Jie Xu, Beibei Wang, Yulian Wang, Wei Zhao, Bin Xiang, Yuhua Xue, Quan Yuan, Yiqiang Wang
Summary: This study identified two peptides using PhD methodology that have the potential to interfere with the interaction between S protein and ACE2. These peptides showed inhibitory effects on the binding of S protein to ACE2 at high concentrations, suggesting their potential as therapeutic agents for blocking the attachment of SARS-CoV-2 virus to host cells.
FRONTIERS IN MICROBIOLOGY
(2022)
Article
Multidisciplinary Sciences
Bo Yang, Yuanyuan Jia, Yumin Meng, Ying Xue, Kefang Liu, Yan Li, Shichao Liu, Xiaoxiong Li, Kaige Cui, Lina Shang, Tianyou Cheng, Zhichao Zhang, Yingxiang Hou, Xiaozhu Yang, Hong Yan, Liqiang Duan, Zhou Tong, Changxin Wu, Zhida Liu, Shan Gao, Shu Zhuo, Weijin Huang, George Fu Gao, Jianxun Qi, Guijun Shang
Summary: This study reveals the critical role of SNX27 in regulating ACE2 receptor homeostasis by preventing the entry of ACE2/virus complex into lysosome/late endosome through its interaction with the retromer complex. This mechanism serves as a countermeasure against invasion by ACE2 receptor-utilizing SARS coronaviruses.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Article
Critical Care Medicine
Lingbing Zhang, Yandan Zhang, Xia Qin, Xuejun Jiang, Jun Zhang, Lejiao Mao, Ziqi Jiang, Yu Jiang, Gang Liu, Jingfu Qiu, Chengzhi Chen, Feng Qiu, Zhen Zou
Summary: This study demonstrates that rACE2 plays a protective role against SARS-CoV-2 spike RBD protein-aggravated LPS-induced ALI in an animal model and illustrates the potential mechanism involving the ACE2-AngII-AT(1)R-NOX1/2 axis in SARS-CoV-2-induced ALI.
Article
Biochemistry & Molecular Biology
Abdullah Hoter, Hassan Y. Naim
Summary: Infection of mammalian cells by SARS-CoV-2 coronavirus requires primary interaction between the receptor binding domain (RBD) of the viral spike protein and the host cell surface receptor angiotensin-converting enzyme 2 (ACE2) glycoprotein. Mutations in the RBD, such as L452R and E484Q, have been found in the Indian B.1.617 variant and may result in evasion of the host immune response and enhanced interaction with ACE2.
FRONTIERS IN MOLECULAR BIOSCIENCES
(2022)
Article
Multidisciplinary Sciences
Arun Bahadur Gurung, Mohammad Ajmal Ali, Joongku Lee, Mohammad Abul Farah, Khalid Mashay Al-Anazi, Fahad Al-Hemaid, Hiba Sami
Summary: This study investigated the impact of mutations in the spike protein of the SARS-CoV-2 virus on its binding affinity to the ACE2 receptor. The findings suggest that these mutations increase the binding affinity, potentially leading to higher virulence and infectivity of emerging variants. The study provides insights for designing therapeutics targeting the interface between the spike protein and ACE2 receptor.
JOURNAL OF KING SAUD UNIVERSITY SCIENCE
(2022)
Article
Medicine, Research & Experimental
Changzhi Li, Hongjuan Zhou, Lingling Guo, Dehuan Xie, Huiping He, Hong Zhang, Yixiu Liu, Lixia Peng, Lisheng Zheng, Wenhua Lu, Yan Mei, Zhijie Liu, Jie Huang, Mingdian Wang, Ditian Shu, Liuyan Ding, Yanhong Lang, Feifei Luo, Jing Wang, Bijun Huang, Peng Huang, Song Gao, Jindong Chen, Chao-Nan Qian
Summary: This study established an anti-coronavirus drug screening platform and identified three potential compounds with anti-coronavirus activity. TS-984 showed strong inhibitory effects and has the potential to be developed into an effective anti-coronavirus drug.
JOURNAL OF TRANSLATIONAL MEDICINE
(2022)
Article
Immunology
Thi Nhu Mai Tran, Bruce Pearson May, Trong Thuan Ung, Mai Khoi Nguyen, Thi Thuy Trang Nguyen, Van Long Dinh, Chinh Chung Doan, The Vinh Tran, Hiep Khong, Thi Thanh Truc Nguyen, Hoang Quoc Huy Hua, Viet Anh Nguyen, Tan Phat Ha, Dang Luu Phan, Truong An Nguyen, Thi Ngoc Bui, Tieu My Tu, Thi Theo Nguyen, Thi Thuy Hang Le, Thi Lan Dong, Trong Hieu Huynh, Phien Huong Ho, Nguyen Thanh Thao Le, Cong Thao Truong, Hoang Phi Pham, Cong Y. Luong, Minh Ngoc Cao, Duy Khanh Nguyen, Thi Thanh Le, Duc Cuong Vuong, Le Khanh Hang Nguyen, Minh Si Do
Summary: The development of the SARS-CoV-2 vaccine candidate Nanocovax, based on recombinant protein production of the S protein, induced high levels of specific IgG antibodies and provided protection against upper respiratory tract infection in animal models, demonstrating safety and efficacy.
FRONTIERS IN IMMUNOLOGY
(2021)
Article
Environmental Sciences
Xiaoning Wang, Chuanxi Yang, Yangyang Sun, Xin Sui, Tong Zhu, Qian Wang, Shuai Wang, Jun Yang, Weijie Yang, Fengying Liu, Minmin Zhang, Yongan Wang, Yuan Luo
Summary: The study used computational simulation to clarify the binding mechanism between SARS-CoV-2 virus and human cells, and investigated and classified anti-viral drugs based on interactions and binding energy of compounds. The results provide valuable information for future screening of anti-viral drugs.
ENVIRONMENT INTERNATIONAL
(2021)
Article
Cardiac & Cardiovascular Systems
Laura P. M. H. de Rooij, Lisa M. Becker, Laure Anne Teuwen, Bram Boeckx, Sander Jansen, Simon Feys, Stijn Verleden, Laurens Liesenborghs, Anna K. Stalder, Sasha Libbrecht, Tina Van Buyten, Gino Philips, Abhishek Subramanian, Sebastien J. Dumas, Elda Meta, Mila Borri, Liliana Sokol, Amelie Dendooven, Anh Co K. Truong, Jan Gunst, Pierre Van Mol, Jasmin D. Haslbauer, Katerina Rohlenova, Thomas Menter, Robbert Boudewijns, Vincent Geldhof, Stefan Vinckier, Jacob Amersfoort, Wim Wuyts, Dirk Van Raemdonck, Werner Jacobs, Laurens J. Ceulemans, Birgit Weynand, Bernard Thienpont, Martin Lammens, Mark Kuehnel, Guy Eelen, Mieke Dewerchin, Luc Schoonjans, Danny Jonigk, Jo van Dorpe, Alexandar Tzankov, Els Wauters, Massimiliano Mazzone, Johan Neyts, Joost Wauters, Diether Lambrechts, Peter Carmeliet
Summary: This study provides new insights into the abundance, expression patterns, and interactomes of endothelial cell (EC) subtypes in COVID-19 and idiopathic pulmonary fibrosis (IPF). The findings suggest the importance of ECs in the pathophysiology of both conditions and may contribute to future investigations into the progression and treatment of COVID-19 and IPF.
CARDIOVASCULAR RESEARCH
(2023)
Article
Chemistry, Medicinal
Martina Salerno, Carmine Varricchio, Federica Bevilacqua, Dirk Jochmans, Johan Neyts, Andrea Brancale, Salvatore Ferla, Marcella Bassetto
Summary: Different viruses, such as enterovirus 71, rely on the host enzyme METTL3 to complete their cytoplasmic life cycle stages. By modulating the activity of this enzyme, it is possible to interfere with a broad range of viral infections. In this study, a series of nucleoside analogues were designed as inhibitors of human METTL3 to target multiple viral infections. Through molecular docking studies and synthesis, several novel and potent inhibitors of enterovirus 71 were identified.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Physical
Az-Eddine El Mansouri, Saida Lachhab, Ali Oubella, Mehdi Ahmad, Johan Neyts, Dirk Jochmans, Winston Chiu, Laura Vangeel, Steven De Jonghe, Hamid Morjani, Mustapha Ait Ali, Mohamed Zahouily, Yogesh S. Sanghvi, Hassan B. Lazrek
Summary: Analogous to pyrimidine and 1,3,4-oxadiazole, the newly synthesized pyrimidine-1,3,4-oxadiazole conjugated hybrid molecules exhibited potential anticancer activity. Specifically, compound 5e demonstrated significant growth inhibition against various cancer cell lines and induced apoptosis through caspase activation and cell-cycle arrest.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Shenghua Gao, Letian Song, Hongtao Xu, Antonios Fikatas, Merel Oeyen, Steven De Jonghe, Fabao Zhao, Lanlan Jing, Dirk Jochmans, Laura Vangeel, Yusen Cheng, Dongwei Kang, Johan Neyts, Piet Herdewijn, Dominique Schols, Peng Zhan, Xinyong Liu
Summary: DF-47 and DF-51 were identified as effective inhibitors of SARS-CoV-2/DENV polymerase through RdRp inhibition screening and in vitro antiviral study. In silico simulation revealed stable binding modes between DF-47/DF-51 and SARS-CoV-2/DENV RdRp, including chelating with Mg2+ near the polymerase active site. These polyphenols have the potential to be developed into broad-spectrum, non-nucleoside RdRp inhibitors with a new scaffold.
Correction
Multidisciplinary Sciences
Emiel Michiels, Kenny Roose, Rodrigo Gallardo, Ladan Khodaparast, Laleh Khodaparast, Rob van der Kant, Maxime Siemons, Bert Houben, Meine Ramakers, Hannah Wilkinson, Patricia Guerreiro, Nikolaos Louros, Suzanne J. F. Kaptein, Lorena Itati Ibanez, Anouk Smet, Pieter Baatsen, Shu Liu, Ina Vorberg, Guy Bormans, Johan Neyts, Xavier Saelens, Frederic Rousseau, Joost Schymkowitz
NATURE COMMUNICATIONS
(2023)
Article
Multidisciplinary Sciences
Rana Abdelnabi, Dirk Jochmans, Kim Donckers, Bettina Trueeb, Nadine Ebert, Birgit Weynand, Volker Thiel, Johan Neyts
Summary: The SARS-CoV-2 main protease (3CLpro) is an important target for COVID-19 treatment. A drug-resistant virus (3CLpro(res)) that is cross-resistant with nirmatrelvir has been identified. The 3CLpro(res) virus can replicate efficiently and be transmitted in Syrian hamsters, but nirmatrelvir still exhibits some antiviral activity against this virus.
NATURE COMMUNICATIONS
(2023)
Article
Multidisciplinary Sciences
Sheli R. Radoshitzky, Patrick Iversen, Xianghan Lu, Jing Zou, Suzanne J. F. Kaptein, Kelly S. Stuthman, Sean A. Van Tongeren, Jesse Steffens, Ruoyu Gong, Hoa Truong, Annapurna A. Sapre, Huiling Yang, Xiaodong Xie, Jia Jun Chia, Zhijuan J. Song, Stacey M. Leventhal, Josolyn Chan, Alex Shornikov, Xin Zhang, David Cowfer, Helen Yu, Travis Warren, Tomas Cihlar, Danielle P. Porter, Johan Neyts, Pei-Yong Shi, Jay Wells, John P. Bilello, Joy Y. Feng
Summary: Remdesivir is an antiviral drug that can inhibit the infection of multiple RNA viruses, including dengue, yellow fever, Zika viruses, and Ebola virus. However, it is not effective against influenza viruses and hepatitis B, C, and E viruses.
SCIENTIFIC REPORTS
(2023)
Article
Plant Sciences
Ngoc-Thao-Hien Le, Steven De Jonghe, Kristien Erven, Johan Neyts, Christophe Pannecouque, Tom Vermeyen, Wouter A. Herrebout, Luc Pieters, Emmy Tuenter
Summary: Scadoxus multiflorus is traditionally used for respiratory problems and this study investigated its alkaloidal composition. A previously undescribed alkaloid and fourteen known ones were identified. Some of the alkaloids exhibited weak antiviral activity against SARS-CoV-2, highlighting the potential of S. multiflorus as a source for anti-SARS-CoV-2 Amaryllidaceae alkaloid scaffolds.
PHYTOCHEMISTRY LETTERS
(2023)
Article
Multidisciplinary Sciences
Dhammika Leshan, Aye Mya Sithu Shein, Cameron Hurst, Peter N. Monk, Parichart Hongsing, Phatthranit Phattharapornjaroen, William Graham Fox Ditcham, Puey Ounjai, Thammakorn Saethang, Naphat Chantaravisoot, Pattama Wapeesittipan, Sirirat Luk-in, Sasipen Sae-Joo, Sumanee Nilgate, Ubolrat Rirerm, Chanikan Tanasatitchai, Naris Kueakulpattana, Matchima Laowansiri, Tingting Liao, Rosalyn Kupwiwat, Rojrit Rojanathanes, Natharin Ngamwongsatit, Somkanya Tungsanga, Asada Leelahavanichkul, Naveen Kumar Devanga Ragupathi, Vishnu Nayak Badavath, S. M. Ali Hosseini, Talerngsak Kanjanabuch, Nattiya Hirankarn, Robin James Storer, Longzhu Cui, Mohan Amarasiri, Hitoshi Ishikawa, Paul G. Higgins, Stephen M. Stick, Anthony Kicic, Tanittha Chatsuwan, Shuichi Abe
Summary: The novel aztreonam-Ca-EDTA or ceftazidime-avibactam-Ca-EDTA combinations show favorable efficacy and safety in treating carbapenemase-positive Klebsiella pneumoniae (CPKp) infections.
Article
Plant Sciences
Ngoc-Thao-Hien Le, Steven De Jonghe, Kristien Erven, Johan Neyts, Christophe Pannecouque, Tom Vermeyen, Wouter A. Herrebout, Luc Pieters, Emmy Tuenter
Summary: A new alkaloid, along with 17 known alkaloids, was isolated and identified from Pancratium maritimum using advanced probabilistic methods and spectroscopic techniques. Assessment of their anti-SARS-CoV-2 activity and cytotoxicity revealed several compounds with weak antiviral potency at non-toxic concentrations, while some compounds showed cytotoxicity.
PHYTOCHEMISTRY LETTERS
(2023)
Meeting Abstract
Gastroenterology & Hepatology
Zhenzhen Shi, Xin Zhang, Niels Cremers, Johan Neyts, Harel Dahari, Suzanne Kaptein
JOURNAL OF HEPATOLOGY
(2023)
Meeting Abstract
Gastroenterology & Hepatology
Kalliopi Pervolaraki, Jean-Christophe Vanherck, Charlene Marcadet, Lieven Verhoye, Amse De Meyer, Madina Rasulova, Heyrhyoung Lyoo, Jasmine Paulissen, Hendrik Jan Thibaut, Kristof De Vos, Patrick Chaltin, Johan Neyts, Pieter Annaert, Philip Meuleman, Arnaud Marchand, Matthias Versele, Stan van de Graaf
JOURNAL OF HEPATOLOGY
(2023)