Review
Pharmacology & Pharmacy
Chuanfeng Liu, Lide Hu, Guanyu Dong, Ying Zhang, Edeildo Ferreira da Silva-Junior, Xinyong Liu, Luis Menendez- Arias, Peng Zhan
Summary: Influenza is a respiratory infection caused by influenza viruses, resulting in millions of severe cases and deaths each year. The frequent mutations and resistance to antiviral drugs make it necessary to develop efficient drugs against different strains of influenza. This review summarizes strategies for discovering and developing antiviral agents targeting multiple strains of influenza, including drug design based on structure, mechanism, multivalent interaction, and repurposing.
ACTA PHARMACEUTICA SINICA B
(2023)
Article
Microbiology
Kin Kui Lai, James B. B. Munro, Guoli Shi, Saliha Majdoul, Alex A. A. Compton, Alan Rein
Summary: Serine incorporator 5 (Ser5) is a host antiviral factor against HIV-1, gammaretroviruses, and Influenza A virus (IAV). It inhibits virus-cell fusion by interacting with HA proteins and destabilizing the pre-fusion conformation of IAV HA. This study provides insights into the antiviral mechanism of Ser5.
Review
Biochemistry & Molecular Biology
Dahai Yu, Linlin Wang, Ye Wang
Summary: This literature review explores the use of computer-aided drug design (CADD) in the development of anti-influenza drugs. It describes the general process of CADD and highlights the viral proteins that can be targeted for anti-influenza therapy. The review also provides examples of drug screening using the CADD approach and discusses the limitations and future directions of CADD strategies in anti-influenza drug discovery.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Biochemistry & Molecular Biology
Facundo N. Gallo, Ana G. Enderle, Lucas A. Pardo, Emilse S. Leal, Mariela Bollini
Summary: Dengue virus is a major challenge in public health, and there is currently no effective antiviral treatment. Control strategies focused on vector control have been unsuccessful, and the virus has become endemic in over 100 countries. This review provides an overview of potential antiviral agents that target the entry of the virus into host cells, discussing their development and evaluation.
CURRENT MEDICINAL CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Charlotte Bach, Julie Lucifora, Marion Delphin, Laura Heydmann, Margaux J. Heuschkel, Caroline Pons, Kaku Goto, Els Scheers, Catherine Schuster, David Durantel, Frederik Pauwels, Thomas F. Baumert, Eloi R. Verrier
Summary: Chronic hepatitis D, caused by super-infection of hepatitis B virus (HBV)-infected hepatocytes with hepatitis D virus (HDV), is the most aggressive form of chronic viral hepatitis. Further improvement in therapy is needed to address the unmet medical need, which requires a more detailed characterization of virus-host interactions for the identification of novel therapeutic targets.
ANTIVIRAL RESEARCH
(2023)
Review
Pharmacology & Pharmacy
Wenteng Chen, Jiaan Shao, Zhimin Ying, Yushen Du, Yongping Yu
Summary: This review summarizes the technologies and medicinal chemistry strategies for the development of PB2 inhibitors as a potential target for combating influenza virus, and provides insights for the fight against drug resistance.
DRUG DISCOVERY TODAY
(2022)
Article
Virology
Louisa E. Wallace, Erik de Vries, Frank J. M. van Kuppeveld, Cornelis A. M. de Haan
Summary: This study systematically analyzed the role of sialoglycan-cleaving neuraminidase (NA) in viral entry in relation to sialoglycan-binding hemagglutinin (HA) receptor-binding preference, the receptor repertoire displayed on cells, and the presence of mucus decoy receptors. It was found that the dependency on NA activity for influenza A virus (IAV) entry largely depends on HA, with a2-6 sialoglycan-binding viruses being more inhibited by NA inhibitor than a2-3 sialoglycan-preferring viruses. The results indicate that the receptor-binding properties of HA in combination with the receptor repertoire present on cells determine the dependency of IAV on NA activity for entry.
JOURNAL OF VIROLOGY
(2023)
Review
Pharmacology & Pharmacy
Lingxin Hou, Ying Zhang, Han Ju, Srinivasulu Cherukupalli, Ruifang Jia, Jian Zhang, Bing Huang, Arianna Loregian, Xinyong Liu, Peng Zhan
Summary: Influenza is a global acute respiratory infectious disease caused by the influenza virus, leading to significant social and economic losses. The viral ribonucleoprotein complex (vRNP) plays a crucial role in the life cycle of influenza viruses and serves as an attractive target for discovering new anti-influenza drugs. Several drug candidates, including baloxavir, have entered clinical trials, with baloxavir already being marketed in Japan and the United States.
ACTA PHARMACEUTICA SINICA B
(2022)
Review
Pharmacology & Pharmacy
Lisa Belfiore, Behnaz Aghaei, Andrew M. K. Law, Jeremy C. Dobrowolski, Lyndon J. Raftery, Angie D. Tjandra, Christine Yee, Alberto Piloni, Alexander Volkerling, Cameron J. Ferris, Martin Engel
Summary: 3D cell models are considered more accurate in predicting the efficacy of drug responses and are seen as more physiologically representative tools for in vitro modeling of in vivo tissues. In the future, 3D cell models will continue to play an important role in drug discovery applications.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Jiwei Zhang, Chuanfeng Liu, Ruifang Jia, Xujie Zhang, Jian Zhang, Chiara Bertagnin, Anna Bonomini, Laura Guizzo, Yuanmin Jiang, Huinan Jia, Shuzhen Jia, Xiuli Ma, Arianna Loregian, Bing Huang, Peng Zhan, Xinyong Liu
Summary: Introducing structurally diverse benzyl side chains at the C5-NH2 position of oseltamivir improves its binding affinity with neuraminidase and anti-influenza activity. We designed and synthesized novel oseltamivir derivatives with different N-heterocycle substituents that induce opening of the 150-loop of group-2 neuraminidases. Compound 6k showed broad-spectrum activity against wild-type neuraminidases and enhanced activity against H3N2 compared to oseltamivir carboxylate and zanamivir.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Virology
Aleksandr Ianevski, Rouan Yao, Eva Zusinaite, Hilde Lysvand, Valentyn Oksenych, Tanel Tenson, Magnar Bjoras, Denis Kainov
Summary: The study suggests that commonly prescribed drugs can affect host responses to FLUAV infection, potentially contributing to increased morbidity and mortality among patients with influenza virus infections.
Article
Biochemistry & Molecular Biology
Elisa Franzi, Gregory Mathez, Soraya Dinant, Charlotte Deloizy, Laurent Kaiser, Caroline Tapparel, Ronan Le Goffic, Valeria Cagno
Summary: Influenza virus is a major cause of respiratory infections worldwide, and finding alternative antiviral strategies is necessary despite the availability of vaccines and antiviral drugs. This study identifies non-steroidal estrogens as potent inhibitors of influenza virus by interacting with the hemagglutinin protein to prevent viral entry.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Liang Shao, Yangqing Su, Yuan Zhang, Fan Yang, Jihong Zhang, Tao Tang, Fei Yu
Summary: The influenza pandemic is a global public health challenge, especially for vulnerable and immunocompromised individuals. Designing effective drugs to inhibit the highly infectious and genetically variable influenza virus is difficult. However, previous studies have shown that oleanolic acid (OA) and its derivatives can block interactions between the virus and host cells, making them potential antiviral agents. In this study, a series of OA nonamers were synthesized and evaluated for their antiviral activities. Compound 15 was found to have the highest potency, comparable to the antiviral drug oseltamivir, and demonstrated activity against both influenza A and B viruses. Mechanistic experiments revealed that the OA nonamers effectively target the influenza HA protein. This study demonstrates the effectiveness of a multivalent structure-activity binding strategy for designing influenza virus inhibitors.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Xia Yang, Hailiang Sun, Zhening Zhang, Weixin Ou, Fengxiang Xu, Ling Luo, Yahong Liu, Weisan Chen, Jianxin Chen
Summary: Influenza A virus (IAV) infections pose a serious threat to public health and there is an urgent need for novel anti-IAV medications. This study reveals that ginsenoside rk1 (G-rk1) and G-rg5, derived from panax ginseng, exhibit significant antiviral effects against different IAV subtypes both in vitro and in vivo. G-rk1 specifically blocks IAV binding to sialic acid and interacts with HA1, making it a potential approach for preventing and treating IAV infections.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biotechnology & Applied Microbiology
Longlong Si, Quan Shen, Jing Li, Li Chen, Jinying Shen, Xue Xiao, Haiqing Bai, Tang Feng, Adam Yongxin Ye, Le Li, Chunhe Zhang, Zhen Li, Ping Wang, Crystal Yuri Oh, Atiq Nurani, Siwen Niu, Chengxin Zhang, Xiaoqiong Wei, Wanqiong Yuan, Hao Liao, Xiaojie Huang, Ning Wang, Wen-xia Tian, Hongwei Tian, Li Li, Xiaoheng Liu, Roberto Plebani
Summary: The study describes the generation of a live attenuated influenza A virus vaccine using PROTAC technology to degrade viral proteins via the host cell's ubiquitin-proteasome system. The vaccine showed highly attenuated and immune responses against both homologous and heterologous virus challenges in mouse and ferret models.
NATURE BIOTECHNOLOGY
(2022)
Article
Immunology
Hany Khalil, Amira Abd ElHady, Khaled A. Elawdan, Dalia Mohamed, Doaa D. Mohamed, Ahmed I. Abd El Maksoud, Farha A. El-Chennawi, Bhgat EI-Fikiy, Ibrahim H. El-Sayed
Summary: Autophagy is a cellular process that maintains cell survival and energy sources, and is associated with the development of many human diseases. Controlling autophagy levels can effectively combat these diseases and the ongoing coronavirus epidemic.
IMMUNOLOGICAL INVESTIGATIONS
(2022)
Article
Biology
Dalia Elebeedy, Ingy Badawy, Ayman Abo Elmaaty, Moustafa M. Saleh, Ahmed Kandeil, Aml Ghanem, Omnia Kutkat, Radwan Alnajjar, Ahmed Abd El Maksoud, Ahmed A. Al-karmalawy
Summary: This study evaluated the antiviral activities of six plant constituents against H1N1 virus, with Tanshinone IIA showing the most promising inhibitory activity and Salvianolic acid B demonstrating high affinities towards the surface glycoproteins of influenza A virus in in silico molecular docking.
COMPUTERS IN BIOLOGY AND MEDICINE
(2022)
Article
Chemistry, Physical
Tamer El Malah, Hanaa Farag, Bahaa A. Hemdan, Randa E. Abdel Mageid, Mohamad T. Abdelrahman, May A. El-Manawaty, Hany F. Nour
Summary: Antibiotic resistance poses a severe threat to humanity, prompting researchers to synthesize a series of isatin-1,2,3-triazole hybrids and evaluate their antimicrobial activity. The most active derivative displayed stronger activity against Gram-negative bacteria and showed potential for binding to specific enzymes via various interactions.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
Katren F. Khella, Ahmed I. Abd El Maksoud, Amr Hassan, Shaimaa E. Abdel-Ghany, Rafaat M. Elsanhoty, Mohammed Abdullah Aladhadh, Mohamed A. Abdel-Hakeem
Summary: This study introduces a promising formula, CA-BSA-NPs, for treating breast and colon cancer, which has good drug loading capacity and release rate, and exhibits high antitumor activity.
Article
Chemistry, Physical
Tamer El Malah, Mohamed Hegab, Hassan M. Awad, Mohamad T. Abdelrahman, Farouk M. E. Abdel-Megeid, Ahmed H. Shamroukh, Randa E. Abdel Mageid, Hany F. Nour
Summary: A new series of benzothiazole-1,2,3-triazole compounds were synthesized and tested for their antibacterial and antifungal activities. One derivative showed high antibacterial activity against Escherichia coli, most compounds exhibited remarkable inhibitory effects against Pseudomonas aeruginosa, while another derivative displayed high activity against Candida albicans. Several derivatives also showed high antioxidant activity.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Organic
Tamer El Malah, Hanaa Farag, Hanem Mohamed Awad, Mohamad Taha Abdelrahman, Ahmed Hussien Shamroukh
Summary: A novel series of 1-substituent-4-(3,4-dimethoxyphenyl)-1H-1,2,3-triazole hybrids were efficiently synthesized via CuAAC reactions. The synthesized compounds were confirmed for their structure and evaluated for cytotoxicity and anticancer activity. Compound 15 showed higher activity against HCT116 and can be considered as a potential candidate for further biological evaluation.
POLYCYCLIC AROMATIC COMPOUNDS
(2023)
Review
Chemistry, Organic
Tamer El Malah, Randa Abdel E. Mageid, Ahmed H. Shamroukh
Summary: The current review mainly focused on the synthetic methods of pyrido[2,3-d]pyrimidine derivatives and their reactions with important pharmaceutical and biological activities.
CURRENT ORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Gad Elsayed Mohamed Salem, Shaimaa M. Azzam, Mona A. F. Nasser, Tamer El Malah, Hanan M. Abd El-Latief, Rizwan Hasan Khan, Suchana Chavanich, Hend Mohamed Anwar
Summary: This study focuses on evaluating the anti-inflammatory and antioxidant effects of Bacterial Protease (BP) and 4,4'-(2,5-dimethoxy-1,4-phenylene) bis (1-(3-ethoxy phenyl)-1H-1,2,3-triazole) (DPET) in treating early-stage liver fibrosis induced by thioacetamide (TAA). The results showed that treatment with BP can improve the severe effects of TAA on the liver, restore tissue architecture, and have the potential to alleviate liver fibrosis.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Microbiology
Sherry A. Guirgis, Khalil A. El-Halfawy, Mai Alalem, Hany Khalil
Summary: This study investigates DNA methylation changes in human lung epithelial cells during L. pneumophila infection and the inhibitory effects of methylation inhibitor agents on L. pneumophila replication. The results showed that L. pneumophila infection induces methylation activity in the promoter regions of TET genes, leading to decreased expression levels. Treatment with 5-AZA or EGCG significantly reduced bacterial reproduction and inhibited methionine synthase expression.
JOURNAL OF MEDICAL MICROBIOLOGY
(2023)
Article
Chemistry, Physical
Tamer El Malah, Hany F. Nour, Tawfik A. Khattab, Saber Ibrahim, Ahmad M. Labeeb
Summary: Triazole bent-core mesogens with symmetrical bent-shaped of two 1,2,3-triazole ring arms were synthesized and characterized. The thermal stability and mesomorphic phase transitions of these novel mesogens were studied, showing a wide temperature range. Different substituents on the bentcore were investigated, resulting in compact supramolecular structures formed by self-assembly. The synthesis, characterization, and polymorphism of the bent-core mesogens were demonstrated, using click chemistry to introduce various substituents. The liquid crystalline performance and morphological characteristics were analyzed, showing the potential for tunable transition temperature and mesophases by selecting lateral structures.
JOURNAL OF MOLECULAR LIQUIDS
(2023)
Article
Chemistry, Organic
Tamer El Malah, Hanaa Farag, Mohamed A. Abdelati, Mohamed I. Hegab
Summary: A series of new 1,2,3-triazole-acetophenone hybrid systems were synthesized through a click reaction and characterized. It was found that compound 9 exhibited higher chemical reactivity compared to the other compounds, while compounds 8, 10, 11, 12, and 13 showed the highest stability and the lowest reactivity.
POLYCYCLIC AROMATIC COMPOUNDS
(2023)
Article
Virology
Mai Alalem, Emad Dabous, Ahmed M. Awad, Nedaa Alalem, Adel A. Guirgis, Samir El-Masry, Hany Khalil
Summary: Research has revealed the significant role of miR-141 in influenza virus infection, where it regulates virus replication by modulating the interferon signaling pathway. The downregulation of several genes, including MxA, STAT3, IFI27, and LAMP3, by miR-141 affects the expression of antiviral genes induced by interferon and IL-6 signaling. This study is of great importance in understanding the immune response mechanisms during influenza virus infection.
Article
Oncology
Amira Abd El-Hady, Farha A. El-Chennawi, Bahgat El-Fikiy, Ibrahim H. El-Sayed, Hany Khalil
Summary: This experimental study investigated the anticancer properties of interferon-gamma, rapamycin, and vitamin B17 in hepatocellular carcinoma and stem cells. Vitamin B17 showed competitive inhibition on cancer cell proliferation compared to Sorafenib, while exerting different effects on stem cells. Vitamin B17 selectively regulated the expression of Raf-1 and autophagy-related LC3B in cancer cells, indicating its effectiveness in cancer treatment.
MIDDLE EAST JOURNAL OF CANCER
(2023)
Article
Chemistry, Multidisciplinary
Noha Abdellatif Ibrahim, Hend Mohamed Anwar, Asmaa M. Moghazy, Tamer El Malah, Waleed Mahmoud Ragab, Rania Awad Hassan Abd El-Aal, Neveen A. Saleh, Doaa Ebrahim Eldosoki
Summary: This study investigated the destructive changes of DENA in liver and colon and the possible therapeutic effects of DOX, MDP, and LAB against DENA-induced dysplasia in liver and colon.
EGYPTIAN JOURNAL OF CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Adeniyi T. Adewumi, Ahmed Elrashedy, Opeyemi S. Soremekun, Mary B. Ajadi, Mahmoud E. S. Soliman
Summary: This study investigated the structural features and dynamics of the Ag85C protein in Mycobacterium tuberculosis, and identified potential targets for antitubercular drugs. The findings have important implications for the design of novel compounds with potent anti-TB activity.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)