Article
Chemistry, Medicinal
Artem Cherkasov, Olivia Garland, Anh-Tien Ton, Shoeib Moradi, Jason R. Smith, Suzana Kovacic, Kurtis Ng, Mohit Pandey, Fuqiang Ban, Jaeyong Lee, Marija Vuckovic, Liam J. Worrall, Robert N. Young, Ralph Pantophlet, Natalie C. J. Strynadka
Summary: The rapid spread of SARS-CoV-2 has led to the development of direct-acting antiviral agents (DAAs). Through virtual screening and pharmacophore filtering, prospective noncovalent PLpro inhibitors with desirable inhibitory activities have been identified. These findings could serve as diverse templates for the development of effective noncovalent PLpro inhibitors.
JOURNAL OF CHEMICAL INFORMATION AND MODELING
(2023)
Article
Chemistry, Multidisciplinary
Yong Cheng, Raina M. Borum, Alex E. Clark, Zhicheng Jin, Colman Moore, Pavla Fajtova, Anthony J. O'Donoghue, Aaron F. Carlin, Jesse Jokerst
Summary: Researchers have developed a dual-color probe for the simultaneous detection of the main protease (MPpro) and papain-like protease (PLpro) of SARS-CoV-2. This probe produces fluorescence from two different fluorophores, which can be used for rapid screening of antiviral inhibitors.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Immunology
Xiang-Hong Ran, Jia-Wu Zhu, Ya-Yun Chen, Run-Ze Ni, Dan Mu
Summary: This study reveals that the papain-like protease of newly emerged SARS-CoV-2 can suppress interferon production and signaling through multiple mechanisms. It targets key components of the signaling pathway and provides insights into the pathogenesis of SARS-CoV-2 and potential antiviral therapies for COVID-19.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Lingyu Li, Liyan Ma, Yue Hu, Xiaoxue Li, Meng Yu, Hai Shang, Zhongmei Zou
Summary: This study discovered natural biflavones as potent inhibitors of SARS-CoV-2 PLpro by investigating the national compound library of traditional Chinese medicines, revealing their inhibitory effects on viral replication and immune evasion processes. Further evaluation included structure-activity relationship elucidation and molecular docking investigation to understand the mechanism of action.
Article
Chemistry, Multidisciplinary
Xin Chen, Ke Chen, Zhaoyong Zhang, Peilan Wei, Lu Zhang, Yunxia Xu, Qili Lun, Yanhong Ma, Fang Wu, Ying Zhang, Yanqun Wang, Jincun Zhao, Yaoqi Zhou, Jian Zhan, Wei Xu
Summary: The PLpro enzyme of SARS-CoV-2 plays a crucial role in virus replication and host immune regulation, making it a potential target for antiviral drugs. In this study, a derivative of chloroxine was found to disrupt the interaction between PLpro and ISG15, showing antiviral effects against SARS-CoV-2 variants.
Article
Biochemistry & Molecular Biology
Daoqun Li, Junwen Luan, Leiliang Zhang
Summary: The study identified potential inhibitors of the SARS-CoV-2 papain-like protease using an in silico molecular docking approach, with Neobavaisoflavone showing the highest binding energy. These compounds may be promising candidates for therapeutic intervention against COVID-19 by targeting crucial catalytic residues of the protease.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2021)
Article
Chemistry, Multidisciplinary
Hangchen Hu, Qian Wang, Haixia Su, Qiang Shao, Wenfeng Zhao, Guofeng Chen, Minjun Li, Yechun Xu
Summary: This study discovered two activators of SARS-CoV-2 PLpro and identified a unique allosteric and covalent regulatory site. These findings provide insights into the allosteric modulation of SARS-CoV-2 PLpro and offer a potential target for allosteric inhibitors design.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Biochemistry & Molecular Biology
Wandong Liu, Juan Wang, Suyun Wang, Kairui Yue, Yu Hu, Xiaochun Liu, Lihao Wang, Shengbiao Wan, Ximing Xu
Summary: This study identifies potential dual-target antiviral drugs by developing inhibitors against PLpro and Mpro proteins in SARS-CoV-2. Compound 6c and 7e showed excellent PLpro inhibition and potent antiviral activities in infected cells. These findings suggest that they are promising candidates for further drug development.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Chia-Chuan Cho, Shuhua G. Li, Tyler J. Lalonde, Kai S. Yang, Ge Yu, Yuchen Qiao, Shiqing Xu, Wenshe Ray Liu
Summary: SARS-CoV-2 encodes PLPro which not only suppresses host immune responses but also serves as a potential therapeutic target. Experimental screening identified several inhibitors with strong inhibitory effects on PLPro, among which SJB2-043 exhibits unique characteristics that warrant further investigation.
Article
Biochemistry & Molecular Biology
Yasir Mohamud, Yuan Chao Xue, Huitao Liu, Chen Seng Ng, Amirhossein Bahreyni, Eric Jan, Honglin Luo
Summary: The study revealed a new mechanism by which PLpro of betacoronaviruses induces viral pathogenesis by targeting cellular autophagy, indicating the significant role of autophagy regulation in virus infection. Viral-encoded proteases target ULK1 protein, disrupting autophagy and promoting viral replication, highlighting the potential for ULK1 as a target for therapeutic interventions against beta-coronaviruses.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2021)
Article
Engineering, Environmental
Qizhi Liang, Yue Huang, Minghui Wang, Deqi Kuang, Jiahua Yang, Yongxiang Yi, Hai Shi, Jinlong Li, Jie Yang, Genxi Li
Summary: In this study, an electrochemical biosensor was developed for the detection of SARS-CoV-2 using its papain-like cysteine protease (PLpro), as well as for screening protease inhibitors against the virus. The biosensor allows sensitive and specific detection of SARS-CoV-2 PLpro in complex real environments and has been tested with patient samples to demonstrate its practical application capability. Additionally, rapid screening of inhibitors against SARS-CoV-2 PLpro can also be achieved, highlighting the potential of this electrochemical biosensor in COVID-19 combat and drug development.
CHEMICAL ENGINEERING JOURNAL
(2023)
Article
Microbiology
GuanQun Liu, Jung-Hyun Lee, Zachary M. Parker, Dhiraj Acharya, Jessica J. Chiang, Michiel van Gent, William Riedl, Meredith E. Davis-Gardner, Effi Wies, Cindy Chiang, Michaela U. Gack
Summary: Conjugation of ISG15 plays a crucial role in activating the RIG-I-like receptor MDA5 and triggering antiviral responses, while SARS-CoV-2 suppresses MDA5 activation through direct de-ISGylation to evade innate immunity.
NATURE MICROBIOLOGY
(2021)
Article
Pharmacology & Pharmacy
Xiaoyan Tian, Quanfeng Zhao, Xiaohong Chen, Zhe Peng, Xiaodan Tan, Qin Wang, Lin Chen, Yang Yang
Summary: Hit 2, a novel and highly potent PLpro inhibitor, was identified through a combined screening approach of structure-based pharmacophore modeling and molecular docking. It showed excellent inhibitory activities against PLpro, with an IC50 value about 4 times higher than that of the positive control. Molecular dynamics simulations confirmed the stability of the binding of these hit compounds to the active site of PLpro.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Marjorie C. L. C. Freire, Gabriela D. Noske, Natalia V. Bitencourt, Paulo R. S. Sanches, Norival A. Santos-Filho, Victor O. Gawriljuk, Eduardo P. de Souza, Victor H. R. Nogueira, Mariana O. de Godoy, Aline M. Nakamura, Rafaela S. Fernandes, Andre S. Godoy, Maria A. Juliano, Bianca M. Peres, Cecilia G. Barbosa, Carolina B. Moraes, Lucio H. G. Freitas-Junior, Eduardo M. Cilli, Rafael V. C. Guido, Glaucius Oliva
Summary: This study reported on antiviral peptides and their derivatives against SARS-CoV-2, showing strong inhibitory activities with low cytotoxicity. These peptides inhibited viral enzyme activities, indicating that they are promising prototypes for the discovery and development of new drugs against SARS-CoV-2.
Review
Chemistry, Medicinal
C. S. Brian Chia, Siew Pheng Lim
Summary: This literature review discusses the patents of coronavirus PLpro inhibitors, providing an overview of the inhibitors that have generated commercial interest, particularly among drug companies.
Article
Environmental Sciences
ZabnAllah M. Alaizeri, Hisham A. Alhadlaq, Saad Aldawood, Mohd Javed Akhtar, Maqusood Ahamed
Summary: This study examined the effect of silver doping on the photocatalytic and anticancer activity of indium oxide nanoparticles. The results showed that silver doping enhances the crystallinity, photocatalytic activity, and anticancer efficacy of indium oxide nanoparticles.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2023)
Article
Multidisciplinary Sciences
Rashid Lateef, Marhaba, Payal Mandal, Kausar M. Ansari, Mohd Javed Akhtar, Maqusood Ahamed
Summary: CuO-rGO nanocomposites have attracted great attention due to their exceptional physicochemical properties. However, their effects on human and environmental health are not well understood. This study investigated the cytotoxicity and apoptosis response of CuO-rGO in normal rat kidney cells. The results showed that CuO-rGO induced cytotoxicity, generation of reactive oxygen species, and apoptosis. Further research is needed to elucidate the potential mechanisms of CuO-rGO toxicity at the molecular level.
JOURNAL OF KING SAUD UNIVERSITY SCIENCE
(2023)
Article
Multidisciplinary Sciences
Maqusood Ahamed, Mohd Javed Akhtar, M. A. Majeed Khan, Hisham A. Alhadlaq
Summary: Due to their exceptional properties, copper oxide nanoparticles (CuO NPs) are widely used in various fields. However, they are toxic to living organisms and no effective method is available to mitigate their health hazards. This study investigates the cytoprotective mechanism of protocatechuic acid (PCA) against CuO NPs toxicity in liver cells. The results show that pre-treatment with PCA can effectively mitigate the cytotoxicity and oxidative stress induced by CuO NPs.
JOURNAL OF KING SAUD UNIVERSITY SCIENCE
(2023)
Article
Multidisciplinary Sciences
Mohd Javed Akhtar, Maqusood Ahamed, Hisham Alhadlaq
Summary: Pt-coated Au nanoparticles exhibited higher uptake and cytotoxicity in human breast cancer cells compared to non-cancerous cells. The nanoparticles induced oxidative stress and loss of mitochondrial membrane potential. These findings suggest the potential of Pt-Au nanoparticles as a promising option for cancer therapy.
JOURNAL OF KING SAUD UNIVERSITY SCIENCE
(2023)
Article
Oncology
Imran Ahmad, Saurabh Pal, Ranjana Singh, Khursheed Ahmad, Nilanjan Dey, Aditi Srivastava, Rumana Ahmad, Muath Suliman, Mohammad Y. Alshahrani, Md. Abul Barkat, Sahabjada Siddiqui
Summary: This study investigates the anticancer potential and underlying mechanism of moricin peptide-induced cell death in triple negative cancer cells. In silico analysis predicts the anticancer potential of moricin, while molecular docking reveals a strong binding interaction between moricin and signaling proteins. In vitro studies demonstrate that moricin exposure leads to dose dependent inhibition of cell viability and caspase-dependent cell death.
CANCER CELL INTERNATIONAL
(2023)
Article
Environmental Sciences
Mohd Javed Akhtar, Maqusood Ahamed, Hisham Alhadlaq
Summary: A review of recent literature suggests that bismuth oxide nanoparticles (Bi2O3 NPs) show appreciable response in cells with epithelial origin only at concentrations above 40-50 μg/mL. However, in human endothelial cells (HUVE cell line), the toxicological profile of Bi2O3 NPs showed much steeper cytotoxicity, with 50% cytotoxicity observed at a much lower concentration of 6.7 μg/mL. The study also found that Bi2O3 NPs induced reactive oxygen species (ROS), lipid peroxidation (LPO), and depletion of intracellular antioxidant glutathione (GSH) in HUVE cells.
Article
Biotechnology & Applied Microbiology
Saheb Ali, Kattakgoundar Govindaraj Sudha, Natesan Thirumalaivasan, Maqusood Ahamed, Saravanan Pandiaraj, Vijayarangan Devi Rajeswari, Yamini Vinayagam, Muthu Thiruvengadam, Rajakumar Govindasamy
Summary: This study focused on the synthesis of magnesium oxide (MgO) nanoparticles (NPs) using Abrus precatorius L. bark extract through the green chemistry method. Characterization techniques such as XRD, FTIR, SEM, TEM, and UV-visible analysis were used to confirm the synthesis of MgO NPs. The synthesized MgO NPs exhibited small particle size and specific surface area. The study also assessed the efficacy of MgO NPs in dye degradation, antioxidant activity, and toxicity using zebrafish embryos and human melanoma cancer cells (A375).
BIOENGINEERING-BASEL
(2023)
Correction
Oncology
Imran Ahmad, Saurabh Pal, Ranjana Singh, Khursheed Ahmad, Nilanjan Dey, Aditi Srivastava, Rumana Ahmad, Muath Suliman, Mohammad Y. Alshahrani, Md. Abul Barkat, Sahabjada Siddiqui
CANCER CELL INTERNATIONAL
(2023)
Article
Multidisciplinary Sciences
Maqusood Ahamed, Mohd Javed Akhtar, Hisham A. Alhadlaq
Summary: The study investigates the combined effects of NiO NPs and BaP in human liver cells and rat hepatocytes, revealing that the co-exposure induces synergistic toxicity and oxidative stress mediated by free oxygen radicals. Further research on risk assessment in an appropriate in vivo model is warranted.
JOURNAL OF KING SAUD UNIVERSITY SCIENCE
(2023)
Article
Multidisciplinary Sciences
Maqusood Ahamed, Mohd Javed Akhtar, M. A. Majeed Khan
Summary: This study describes a method for manufacturing MgO nanoparticles using garlic extract to minimize environmental impact. The results show that these nanoparticles exhibit high effectiveness against various microorganisms and cancer cells.
JOURNAL OF KING SAUD UNIVERSITY SCIENCE
(2023)
Article
Multidisciplinary Sciences
Mohd Javed Akhtar, Maqusood Ahamed, Hisham Alhadlaq
Summary: This study compares the effects of two types of cobalt-based nanoparticles on lung cells and finds that cobalt nanoparticles are more toxic to cells than cobalt-iron oxide nanoparticles, possibly due to the higher release of Co2+ ions by cobalt nanoparticles. Additionally, the study suggests that CalceinAM alone is insufficient to assess the toxicity of cobalt-based nanoparticles, and other methods should be used for further confirmation.
JOURNAL OF KING SAUD UNIVERSITY SCIENCE
(2024)
Article
Chemistry, Multidisciplinary
ZabnAllah M. Alaizeri, Hisham A. Alhadlaq, Saad Aldawood, Mohd Javed Akhtar, Maqusood Ahamed
Summary: Graphene derivatives and metal oxide-based nanocomposites (NCs) are investigated for various applications. This study demonstrates that the integration of rGO and Bi2O3 enhances photocatalytic and anticancer efficacy, and the prepared Bi2O3-WO3/rGO NCs exhibit improved activity.
Article
Materials Science, Multidisciplinary
Maqusood Ahamed, Mohd Javed Akhtar, M. A. Majeed Khan
Summary: In this study, we synthesized Acacia nilotica (L.) fruit extract-green produced ZrO2/RGO nanocomposites (NCs) and investigated their anticancer properties. The results showed that ZrO2/RGO NCs were more effective than pure ZrO2 NPs in inhibiting the growth of different human cancer cells (A549, HepG2, and MCF7), while also exhibiting greater cytocompatibility in normal cell lines (IMR90 and MCF10A). Mechanistic evidence suggested that the anticancer response of ZrO2/RGO NCs was attributed to the production of intracellular reactive oxygen species and the reduction of glutathione, leading to oxidative stress.
MATERIALS TODAY COMMUNICATIONS
(2023)
Article
Chemistry, Multidisciplinary
Sitah Alanazi, ZabnAllah M. Alaizeri, Rashid Lateef, Nawal Madkhali, Abdullah Alharbi, Maqusood Ahamed
Summary: This study investigates the anticancer potential of Zn-doped SnO2 nanoparticles (NPs) and demonstrates that Zn doping enhances the anticancer efficacy of SnO2 NPs. The physicochemical properties of the NPs are characterized using various techniques, revealing changes in the crystalline size and band gap energy after Zn doping. In vitro studies show that Zn-doped SnO2 NPs exhibit increased anticancer activity in breast cancer cells.
APPLIED SCIENCES-BASEL
(2023)
Article
Multidisciplinary Sciences
Rashid Lateef, Israr Ahmad, Abbas Ali Mahdi, Pavan Rajanahalli, Mohd Javed Akhtar, Maqusood Ahamed
Summary: Recent research has found that metal oxide nanoparticles may pose a threat to the health of pregnant individuals and developing fetuses. This study aimed to investigate the preventative effects of solanesol on the harmful effects caused by copper oxide (CuO) and nickel oxide (NiO) nanoparticles in human placental cells. The results showed that solanesol significantly alleviated the cytotoxicity and apoptosis induced by the nanoparticles. Further research is needed to explore the pharmacological potential of solanesol against nanoparticle-generated pregnancy problems.
JOURNAL OF KING SAUD UNIVERSITY SCIENCE
(2023)