Article
Chemistry, Medicinal
Yejin Jang, Jinhe Han, Xiaoli Li, Hyunjin Shin, Won-Jea Cho, Meehyein Kim
Summary: Influenza viruses are major pathogens causing respiratory infections in humans. A newly discovered isoquinolone compound showed potential in inhibiting influenza A and B viruses, but exhibited cytotoxic effects. Through chemical optimization, compound 21 was developed with improved antiviral activity and reduced cytotoxicity.
Article
Medicine, Research & Experimental
Won-Kyung Cho, Jin Yeul Ma
Summary: Epimedium koreanum Nakai (EKN) has shown significant inhibitory effects on influenza A virus infection by directly blocking viral attachment and having a virucidal effect. It can potentially be developed as a natural viral inhibitor against influenza virus infection.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Chemistry, Medicinal
Hui-Xian Wang, Mao-Sen Zeng, Yi Ye, Jin-Yuan Liu, Pei-Ping Xu
Summary: Puerarin, a major isoflavone compound from Pueraria lobata root, exhibits various properties including anti-inflammatory, antioxidant, and antiviral effects. It shows inhibitory activity against H1N1 influenza virus by blocking viral NP transport and newly formed virus particle release. In vivo studies demonstrate its potential as a treatment for influenza virus infection, with effective antiviral activity and reduced inflammation in the lungs.
PHYTOTHERAPY RESEARCH
(2021)
Article
Medicine, Research & Experimental
Yong-Hyun Joo, Yeong-Geun Lee, Younghyun Lim, Hoyeon Jeon, In-Gu Lee, Yong -Bin Cho, So-Hee Hong, Eui Ho Kim, Soon Ho Choi, Jung-Woong Kim, Se Chan Kang, Young-Jin Seo
Summary: This study investigated the anti-influenza A virus (IAV) activity of an aqueous mixture of Agrimonia pilosa and Galla rhois extracts (APRG64). The results showed that APRG64 significantly reduced IAV-induced cytopathic effect, viral protein transcription/expression, and infectious viral particle production. The main component responsible for the anti-IAV activity was identified as apigenin. APRG64 and apigenin inhibited virus attachment, entry, and polymerase activity. Intranasal or oral administration of APRG64 reduced viral loads and protected mice from IAV-induced mortality by reducing viral RNA levels and pro-inflammatory cytokine expression in the lungs.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Biochemistry & Molecular Biology
Na Jiang, Liqiu Quan, Yan Zhou, Yungyi Cheng, Hongmei Li, Xuanqin Chen, Rongtao Li, Dan Liu
Summary: This study found that TP derivatives have antiviral activity and anti-inflammatory effects against influenza A virus by inhibiting viral replication and regulating immune response. They could be potential candidates for antiviral drugs.
BIOORGANIC CHEMISTRY
(2022)
Article
Nutrition & Dietetics
Ayaka Nakashima, Yuka Horio, Kengo Suzuki, Yuji Isegawa
Summary: Euglena extract has shown strong inhibitory effects against various strains of influenza virus, including drug-resistant strains. It may work by activating host cell defense mechanisms rather than directly targeting the virus. Additionally, minerals in the extract, mainly zinc, were found to be involved in its antiviral activity.
Article
Biochemistry & Molecular Biology
Irina Smirnova, Anastasiya Petrova, Gul'nara Giniyatullina, Anna Smirnova, Alexandrina Volobueva, Julia Pavlyukova, Vladimir Zarubaev, Tran Van Loc, Thao Tran Thi Phoung, Vu Thi Bich Hau, Nguyen Thi Thu Thuy, Myint Myint Khine, Oxana Kazakova
Summary: A series of sixteen A-ring modified oleanonic acid derivatives were synthesized and screened for antiviral activity against influenza and dengue viruses. Two compounds showed high potency against both viruses.
Article
Biochemistry & Molecular Biology
Esra Tatar, Seda Yaldiz, Necla Kulabas, Evelien Vanderlinden, Lieve Naesens, Ilkay Kucukguzel
Summary: The study investigates a series of novel 1,3,4-thiadiazole derivatives as potential inhibitors of influenza A virus, with two compounds showing promising antiviral activity. These compounds selectively inhibit influenza A virus during the entry process. In silico studies suggest these active compounds could be good candidates for oral administration without apparent toxicity concerns.
CHEMICAL BIOLOGY & DRUG DESIGN
(2022)
Article
Virology
Mengwei Li, Yuxu Wang, Jing Jin, Jie Dou, Qinglong Guo, Xue Ke, Changlin Zhou, Min Guo
Summary: The study reveals that honeysuckle acids and flavonoids extracts are the major antiviral active components, showing inhibitory effects against influenza viruses. Honeysuckle extracts have a broad-spectrum inhibitory effect on the neuraminidase of influenza viruses.
Article
Virology
Rashid Manzoor, Nao Eguchi, Reiko Yoshida, Hiroichi Ozaki, Tatsunari Kondoh, Kosuke Okuya, Hiroko Miyamoto, Ayato Takada
Summary: Protective immunity against influenza A viruses mainly relies on antibodies to hemagglutinin (HA), but the conserved M2 protein has been studied as a vaccine antigen for cross-protective immunity. This study reveals that an M2-specific antibody can interfere with the HA-M2 association, providing a novel mechanism for the antiviral activity of M2-specific antibodies.
JOURNAL OF VIROLOGY
(2021)
Review
Virology
Mostafa Javanian, Mohammad Barary, Sam Ghebrehewet, Veerendra Koppolu, VeneelaKrishnaRekha Vasigala, Soheil Ebrahimpour
Summary: Influenza is an acute viral respiratory infection that affects all age groups and is associated with high mortality. Vaccination is the most effective method for prevention, but antiviral drugs are also available for treatment.
JOURNAL OF MEDICAL VIROLOGY
(2021)
Article
Plant Sciences
Yong-Hyun Joo, Yeong-Geun Lee, Younghyun Lim, Hoyeon Jeon, Eui Ho Kim, Joongyeon Choi, Woojae Hong, Hyelin Jeon, Michael Ahrweiler, Hyunggun Kim, Se Chang Kang, Young-Jin Seo
Summary: The study found that the extract of Elaeocarpus sylvestris has strong antiviral activity against influenza A virus infection, which could lead to the development of new plant-based medicine to treat influenza virus infection.
Article
Biochemistry & Molecular Biology
Antoine Guillon, Deborah Brea-Diakite, Adeline Cezard, Alan Wacquiez, Thomas Baranek, Jerome Bourgeais, Frederic Picou, Virginie Vasseur, Lea Meyer, Christophe Chevalier, Adrien Auvet, Jose M. Carballido, Lydie Nadal Desbarats, Florent Dingli, Andrei Turtoi, Audrey Le Gouellec, Florence Fauvelle, Amelie Donchet, Thibaut Crepin, Pieter S. Hiemstra, Christophe Paget, Damarys Loew, Olivier Herault, Nadia Naffakh, Ronan Le Goffic, Mustapha Si-Tahar
Summary: Research has shown that influenza virus infection causes significant changes in lung metabolism, leading to the accumulation of succinate in respiratory fluids. Succinate exhibits powerful antiviral activity by inhibiting influenza virus replication and reducing metabolic disruptions and inflammatory responses. Administering succinate intranasally to mice reduces viral loads in the lungs and improves survival rates. The antiviral mechanism involves succinylation of viral nucleoproteins, which alters their interactions with viral RNA.
Article
Nanoscience & Nanotechnology
Indrani Das Jana, Partha Kumbhakar, Saptarshi Banerjee, Chinmayee Chowde Gowda, Nandita Kedia, Saikat Kumar Kuila, Susanta Banerjee, Narayan Chandra Das, Amit Kumar Das, Indranil Manna, Chandra Sekhar Tiwary, Arindam Mondal
Summary: Researchers have identified copper-graphene (Cu-Gr) nanocomposite as a material with strong antiviral activity against influenza virus. The unique metal oxide-embedded graphene sheet architecture can inactivate virus particles within 30 minutes and interfere with their entry into host cells, reducing viral gene expression and transmission rate. The nanocomposite can be potentially applied as a highly transparent coating on various surfaces to minimize respiratory virus infections.
ACS APPLIED NANO MATERIALS
(2021)
Article
Chemistry, Medicinal
Yongzhuang Ge, Chaofeng Zhang, Ying Qu, Lixia Ding, Xinbo Zhang, Zhongmou Zhang, Chengyun Jin, Xiao-Na Wang, Zhenya Wang
Summary: Through the synthesis of a series of naphthalene derivatives, it was found that 2-aminonaphthalene 4d has anti-influenza virus activity and can inhibit H1N1 and H3N2 subtypes. It has the best effect in the early stages of virus replication, reducing virus replication, inhibiting virus-induced inflammation response, and cell death. Therefore, 2-aminonaphthalene 4d is a potential drug for the treatment of influenza A virus infection.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Milan Kumar Mandal, Swagatika Ghosh, Lieve Naesens, Hans Raj Bhat, Udaya Pratap Singh
Summary: The study involved the synthesis of novel compounds with significant antimicrobial and antiviral activities, particularly showing strong inhibitory effects against bacteria and fungi, as well as considerable antiviral activity against various viruses. The findings suggest potential for the development of compounds with dual antimicrobial and antiviral properties.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Esra Tatar, Seda Yaldiz, Necla Kulabas, Evelien Vanderlinden, Lieve Naesens, Ilkay Kucukguzel
Summary: The study investigates a series of novel 1,3,4-thiadiazole derivatives as potential inhibitors of influenza A virus, with two compounds showing promising antiviral activity. These compounds selectively inhibit influenza A virus during the entry process. In silico studies suggest these active compounds could be good candidates for oral administration without apparent toxicity concerns.
CHEMICAL BIOLOGY & DRUG DESIGN
(2022)
Article
Immunology
Nathalie Vanderheijden, Annelies Stevaert, Jiexiong Xie, Xiaolei Ren, Cyril Barbezange, Sam Noppen, Isabelle Desombere, Bruno Verhasselt, Peter Geldhof, Nick Vereecke, Veerle Stroobants, Dayoung Oh, Merijn Vanhee, Lieve M. J. Naesens, Hans J. Nauwynck
Summary: Broadly protective therapeutic antibodies are urgently needed to combat SARS-CoV-2 variants. Researchers have found that antibodies formed during coronavirus infection can target multiple coronaviruses. These antibodies can bind to both alpha- and betacoronaviruses, but their neutralizing activity against SARS-CoV-2 is weak. However, they may still play a role in influencing the severity of coronavirus infection and disease through Fc-mediated effector functions.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Microbiology
Laura Seldeslachts, Cato Jacobs, Birger Tielemans, Eliane Vanhoffelen, Lauren Van der Sloten, Stephanie Humblet-Baron, Lieve Naesens, Katrien Lagrou, Erik Verbeken, Joost Wauters, Greetje Vande Velde
Summary: The study found that baloxavir marboxil has a therapeutic effect on influenza-associated pulmonary aspergillosis, improving body weight, survival, and viral clearance in a mouse model. It also reduces lung lesions and fungal burden, suggesting that baloxavir marboxil can mitigate severe influenza and decrease the risk of lethal invasive Aspergillus superinfection.
Article
Chemistry, Medicinal
Gokce Cihan-Ustundag, Cigdem Acar, Lieve Naesens, Gonca Erkose-Genc, Dilek Satana
Summary: We synthesized a novel series of hybrid spirothiazolidinone derivatives and evaluated their antiviral and antitubercular activities. Some of these compounds showed specific antiviral activity against the influenza A/H3N2 virus, with the most active compound being 3a with an antiviral EC50 value of 5.2μM. In addition, some compounds also exhibited inhibitory activity against Mycobacterium tuberculosis.
ARCHIV DER PHARMAZIE
(2022)
Article
Microbiology
Annelies Stevaert, Ria Van Berwaer, Cato Mestdagh, Julie Vandeput, Els Vanstreels, Valerie Raeymaekers, Manon Laporte, Lieve Naesens
Summary: The S2' motif in the SARS-CoV-2 spike protein plays a crucial role in spike activation, with TMPRSS2 showing more tolerance to variations than TMPRSS13. This insight will help in estimating the impact of S2' motif changes in new variants.
Article
Pharmacology & Pharmacy
Bert Vanmechelen, Joren Stroobants, Winston Chiu, Lieve Naesens, Joost Schepers, Kurt Vermeire, Piet Maes
Summary: This study successfully achieved biological containment of Marburg virus, demonstrating its feasibility for other filoviruses. By using genetic engineering and specific cell lines, the virus can be handled safely in lower biosafety settings.
ANTIVIRAL RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Miklos Bege, Alexandra Kiss, Ilona Bereczki, Jan Hodek, Lenke Polyak, Gabor Szeman-Nagy, Lieve Naesens, Jan Weber, Aniko Borbas
Summary: In this study, d-arabinofuranosyl-pyrimidine and -purine nucleoside analogues containing alkylthio-, acetylthio- or 1-thiosugar substituents at the C2' position were synthesized by photoinitiated, radical-mediated hydrothiolation reactions. Some of these compounds exhibited selective cytotoxicity against tumor cells and also showed antiviral activity against SARS-CoV-2 and/or HCoV-229E.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Multidisciplinary Sciences
Ilona Bereczki, Vladimir Vimberg, Eszter Lorincz, Henrietta Papp, Lajos Nagy, Sandor Keki, Gyula Batta, Ana Mitrovic, Janko Kos, Aron Zsigmond, Istvan Hajdu, Zsolt Lorincz, David Bajusz, Laszlo Petri, Jan Hodek, Ferenc Jakab, Gyorgy M. Keseru, Jan Weber, Lieve Naesens, Pal Herczegh, Aniko Borbas
Summary: Patients infected with SARS-CoV-2 are at risk of co-infection with Gram-positive bacteria, which greatly affects their prognosis. Antimicrobial drugs with dual antiviral and antibacterial activity would be valuable in this context. The researchers synthesized and evaluated seven derivatives of teicoplanin, a glycopeptide antibiotic, with hydrophobic or superbasic side chains. Except for one derivative, all teicoplanin derivatives effectively inhibited SARS-CoV-2 replication in VeroE6 cells. Some of these derivatives also showed activity against HCoV-229E, a human coronavirus, in human Calu-3 cells. The study revealed that the teicoplanin derivatives efficiently prevented the entry of SARS-CoV-2 into cells through both endosomal and surface entry routes. Moreover, these derivatives exhibited good to excellent activity against Gram-positive bacteria resistant to glycopeptide antibiotics.
SCIENTIFIC REPORTS
(2022)
Article
Chemistry, Medicinal
Sonia De Castro, Annelies Stevaert, Miguel Maldonado, Adrien Delpal, Julie Vandeput, Benjamin Van Loy, Cecilia Eydoux, Jean-Claude Guillemot, Etienne Decroly, Federico Gago, Bruno Canard, Maria-Jose Camarasa, Sonsoles Velazquez, Lieve Naesens
Summary: There is a need for novel antiviral concepts to control SARS-CoV-2 infection. A class of 1,4,4-trisubstituted piperidines have shown promising anti-coronavirus activity. Several analogues were synthesized and evaluated, and four molecules demonstrated micromolar activity against SARS-CoV-2. These compounds were found to inhibit the main protease (M-pro) of SARS-CoV-2, suggesting they could serve as non-covalent inhibitors for further development.
Article
Chemistry, Medicinal
Cagla Begum Apaydin, Ozge Soylu-Eter, Pinar Eraslan-Elma, Nurten Ozsoy, Nilgun Karali
Summary: In this study, a series of 1-benzyl-2-indolinone compounds were designed, synthesized, and evaluated for their inhibitory effects on acetylcholinesterase and butyrylcholinesterase. Several compounds showed superior potency and selectivity against acetylcholinesterase compared with donepezil. Molecular dynamics simulations suggested the preferred binding of these compounds at allosteric binding pocket 4 of the enzyme.
FUTURE MEDICINAL CHEMISTRY
(2022)
Article
Virology
Annelies Stevaert, Elisabetta Groaz, Lieve Naesens
Summary: The COVID-19 pandemic has accelerated the development of nucleoside analogs for treating respiratory virus infections. Remdesivir is the first authorized compound, and three other nucleoside analogs are in the pipeline. This article summarizes the current knowledge on their clinical efficacy and mentions trials for influenza and respiratory syncytial virus. Furthermore, it outlines how nucleoside analogs interact with respiratory virus polymerases to cause lethal virus mutagenesis or disturbance of viral RNA synthesis.
CURRENT OPINION IN VIROLOGY
(2022)
Article
Pharmacology & Pharmacy
Evelien Vanderlinden, Arnaud Boonen, Sam Noppen, Geert Schoofs, Maya Imbrechts, Nick Geukens, Robert Snoeck, Annelies Stevaert, Lieve Naesens, Graciela Andrei, Dominique Schols
Summary: PRO-2000, a sulfonated polyanionic compound, has anti-SARS-CoV-2 activity by blocking the entry pathway and inhibiting the binding of the S protein to its receptor. It can potentially inhibit a broad range of SARS-CoV-2 variants.
ANTIVIRAL RESEARCH
(2023)
Article
Chemistry, Medicinal
Rui Wang, Annelies Stevaert, Tien Nguyen Truong, Qifei Li, Besir Krasniqi, Benjamin Van Loy, Arnout Voet, Lieve Naesens, Wim Dehaen
Summary: The study investigates the structure-activity relationship of novel coronavirus inhibitors and identifies a class of 1,2,3-triazolo fused triterpenoid compounds with strong antiviral activity against HCoV-229E.
ARCHIV DER PHARMAZIE
(2023)
Meeting Abstract
Cardiac & Cardiovascular Systems
J. Kaes, E. Vanhulle, L. Seldeslachts, C. Hooft, H. Beeckmans, X. Jin, P. Kerckhof, J. Van Slambrouck, D. Van Raemelonck, G. Vande Velde, L. Naesens, D. Schols, L. J. Ceulemans, R. Vos, K. Vertneire, B. M. Vanaudenaerde
JOURNAL OF HEART AND LUNG TRANSPLANTATION
(2023)
Correction
Biochemistry & Molecular Biology
Mohamed Marzouk, Shimaa M. Khalifa, Amal H. Ahmed, Ahmed M. Metwaly, Hala Sh. Mohammed, Hanan A. A. Taie
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Gerardo Andres Libreros-Zuniga, Danilo Pava e Pavao, Vinicius de Morais Barroso, Nathalya Cristina de Moraes Roso Mesquita, Saulo Fehelberg Pinto Braga, Glaucius Oliva, Rafaela Salgado Ferreira, Kelly Ishida, Marcio Vinicius Bertacine Dias
Summary: Tuberculosis is a major global cause of death, and the emergence of drug-resistant strains has increased the burden of this disease. New alternative therapies are constantly needed, and recent research has identified small molecules as potential inhibitors of Ldts in M. tuberculosis, which have antimycobacterial activity.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Xiao-Dong Wang, Yong-Si Liu, Ming-Hao Hu
Summary: In this study, a selffolded fluorescent probe was designed to selectively illuminate G4s by unfolding its intramolecular aggregation mediated by G4 binding. This probe showed more controllable background emission and promising ability to track G4 forming dynamics compared to previous disaggregation-induced emission (DIE) probes.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yu Xiang, Zhuo Yuan, Qichuan Deng, Linshen Xie, Dongke Yu, Jianyou Shi
Summary: This review provides a brief description of the diagnosis, pathogenesis, and potential therapeutic inhibitors for renal fibrosis. Currently, there are no clear therapeutic targets or drugs for renal fibrosis; however, some natural products may have potential efficacy for treating renal fibrosis.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Simone Giovannuzzi, Anna Nikitjuka, Bruna Rafaela Pereira Resende, Michael Smietana, Alessio Nocentini, Claudiu T. Supuran, Jean-Yves Winum
Summary: Boron-based compounds have been extensively studied in medicinal chemistry, playing a crucial role in designing small molecule drugs for various diseases. Boron is particularly valuable in developing inhibitors for metalloenzymes carbonic anhydrases, and it can modulate ligand recognition ability and selectivity. Recent advancements have led to the discovery of novel boron-based inhibitors that can inhibit carbonic anhydrases through a Lewis acid-base mechanism. Further research is needed to fully explore the potential of boron-based inhibitors and advance their clinical applications.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Xinxin Liu, Lei Chen, Ze Chen
Summary: This study developed a nanostructured photosensitizer loaded with oxygen-throttling drug and demonstrated its enhanced cytotoxicity against tumor cells under hypoxic conditions. Animal experiments showed the enhanced tumor targeting capability of the photosensitizer and its inhibitory effect on tumor growth.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Shuai Jiang, Wen-Yan Li, Zai-Feng Yuan, Qin-Shi Zhao
Summary: This study isolated two new dimeric Lycopodium alkaloids and twelve previously undescribed Lycopodium alkaloids from Lycopodiastrum casuarinoides. The structures of these compounds were determined and their inhibitory activities on the Cav3.1 channel were evaluated.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yan Yang, Dong-Xiao Yan, Rui-Xue Rong, Bing-Ye Shi, Man Zhang, Jing Liu, Jie Xin, Tao Xu, Wen-Jie Ma, Xiao-Liu Li, Ke-Rang Wang
Summary: In this study, a series of nucleolar fluorescent probes based on naphthalimide derivatives were designed and synthesized, which could achieve clear nucleolar staining in living cells. The results showed that these probes exhibited good targeting to the cell nucleolus and could bind to RNA and enhance fluorescence. This has positive implications for the diagnosis and treatment of nucleolus-related diseases.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yongxi Dong, Fang Wang, Jinlan Wen, Yongqing Mao, Shanhui Zhang, Tiemei Long, Zhangxiang Yang, Lei Li, Jiquan Zhang, Li Dong, Gang Liu, Jianwei Xu
Summary: The hybrid molecules of Scutellarein and Tertramethylpyrazine show excellent neuroprotective and antiplatelet effects in the treatment of ischemic stroke. Compound 1e is particularly effective, enhancing cell membrane permeability and inhibiting cell uptake, as well as significantly reducing cerebral infarction volume.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yu Chen, Yuanyuan Ying, Jonathan Lalsiamthara, Yuheng Zhao, Saber Imani, Xin Li, Sijing Liu, Qingjing Wang
Summary: This paper examines the role and metabolic regulation of NAD+ in bacteria, highlighting its impact on physiology and virulence. It explores enzymes associated with NAD+ metabolism as potential targets for antibacterial drugs and vaccine candidates. Additionally, it scrutinizes the medical potential of NAD+ and provides insights for its application in biomedicine.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Jon Macicior, Daniel Fernandez, Silvia Ortega-Gutierrez
Summary: Hutchinson-Gilford progeria syndrome (HGPS), also known as progeria, is a rare genetic disease that causes premature aging and significantly reduces life expectancy. Currently, there is only one approved drug for treating progeria, but its efficacy is limited. Progerin levels are believed to be the most important biomarker related to disease severity.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Fuko Hirano, Naoya Kondo, Yusuke Murata, Aya Sudani, Takashi Temma
Summary: Fluorinated alpha-methyl 3BPA derivatives showed improved water solubility, tumor targetability, and biodistribution compared to 3BPA and BPA, resulting in significantly improved tumor-to-normal tissue ratios.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Ying Shi, Jiaqin Tang, Shumeng Zhi, Ruiqi Jiang, Qing Huang, Lei Sun, Zhizhong Wang, Yanran Wu
Summary: Necroptosis is a type of cell death associated with various diseases. In this study, we identified a small molecule inhibitor, SY-1, that effectively blocks necroptosis by inhibiting the phosphorylation of RIP1/RIP3/MLKL pathway. SY-1 also showed protective effects against TNF-induced hypothermia and improved survival in mice with SIRS. These findings highlight the potential therapeutic applications of SY-1.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Andrea Bagan, Sonia Abas, Judith Pala-Pujadas, Alba Irisarri, Christian Grinan-Ferre, Merce Pallas, Itziar Muneta-Arrate, Carolina Muguruza, Luis F. Callado, Belen Perez, Elies Molins, Jose A. Morales-Garcia, Carmen Escolano
Summary: Recent studies have identified the modulation of imidazoline I-2 receptors (I-2-IR) by selective ligands as a potential strategy for treating neurodegenerative diseases. This study reports a family of bicyclic alpha-iminophosphonates that show high affinity and selectivity for I-2-IR and demonstrates their neuroprotective and anti-inflammatory effects in in vitro and in vivo models. The findings emphasize the importance of exploring structurally novel I-2-IR ligands for therapeutic strategies in neurodegeneration.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Qiuping Xiang, Tianbang Wu, Cheng Zhang, Chao Wang, Hongrui Xu, Qingqing Hu, Jiankang Hu, Guolong Luo, Xiaoxi Zhuang, Xishan Wu, Yan Zhang, Yong Xu
Summary: This study reports the discovery of a 1-(indolizin-3-yl)ethan-1-one derivative as a potent and selective CBP bromodomain inhibitor for AML drug development.
BIOORGANIC CHEMISTRY
(2024)
