Article
Biochemistry & Molecular Biology
Yara El-Dash, Emad Elzayat, Amr M. Abdou, Rasha A. Hassan
Summary: Novel hybrid compounds of hexahydrobenzo[4,5]thieno[2,3-d]pyrimidine with aminothiazole scaffolds were synthesized and evaluated for their cytotoxic activity against human tumor cell lines. Compounds 7c, 7d, and 7e showed significant antiproliferative activities, with 7c demonstrating excellent cytotoxic activity against various cancer cell lines. Compound 7c also exhibited potential as a VEGFR-2 inhibitor and induced G2/M phase cell cycle arrest and apoptosis in treated cells.
BIOORGANIC CHEMISTRY
(2021)
Article
Neurosciences
Ahmad Salamian, Diana Legutko, Klaudia Nowicka, Bogna Badyra, Paulina Kazmierska-Grebowska, Bartosz Caban, Tomasz Kowalczyk, Leszek Kaczmarek, Anna Beroun
Summary: The application of a cholinergic agonist in the hippocampus induces the activity of matrix metalloproteinase 9 (MMP-9), affecting the frequency of excitatory and inhibitory synaptic transmission and maintaining the balance between neurons.
Article
Biochemistry & Molecular Biology
Joana Mota, Rosa Direito, Joao Rocha, Joao Fernandes, Bruno Sepodes, Maria Eduardo Figueira, Anabela Raymundo, Ana Lima, Ricardo Boavida Ferreira
Summary: The study isolated and characterized an MMP-2 and -9 inhibitor from Lupinus albus, showing its efficacy in inhibiting MMP-9 activity in colon cancer cells and significantly reducing colitis symptoms in a mouse model. This novel type of MMP inhibitor in lupine, edible and proteinaceous in nature, holds high potential for application as a nutraceutical or functional food targeting pathologies related to high MMP-9 activity in the digestive system.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Jacek Kudelski, Anna Tokarzewicz, Monika Gudowska-Sawczuk, Barbara Mroczko, Piotr Chlosta, Marta Bruczko-Goralewska, Przemyslaw Mitura, Grzegorz Mlynarczyk
Summary: This study aimed to evaluate the expression and activity of matrix metalloproteinase 2 and 9 (MMP-2 and MMP-9) in urinary bladder cancer at different stages. The results showed that the content and activity of MMP-9 were higher than MMP-2, especially in high-grade cancer tissue. MMP-9 may have higher clinical utility as a potential therapeutic option and a diagnostic biomarker for urinary bladder cancer.
Article
Chemistry, Physical
Hany M. Abd El-Lateef, Rasha Mohammed Saleem, Mohammed A. Bazuhair, Ali Hassan Ahmed Maghrabi, Eman Hussain Khalifa Ali, Islam Zaki, Reham E. Masoud
Summary: A new series of hydrazone derivatives were synthesized and screened for their cytotoxic activity against MCF-7 breast cancer cell line. Some compounds exhibited potent cytotoxicity and inhibition of β-tubulin. Flow cytometric analysis revealed that one compound induced cell cycle arrest at G2/M phase and increased apoptosis compared to untreated control. Molecular modeling investigations were conducted to explain the compound's exceptional cytotoxicity and superior ability to inhibit tubulin when compared to CA-4.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Microbiology
Brenda Furtado Costa, Tarcisio Navegante de Queiroz Filho, Adeniele Lopes da Cruz Carneiro, Aline Semblano Carreira Falcao, Maria Sueli da Silva Kataoka, Joao de Jesus Viana Pinheiro, Ana Paula Drummond Rodrigues
Summary: This study examines the presence and activity of MMP-2 and MMP-9 in Leishmania parasites, particularly in two different Leishmania species, L. amazonensis and L. braziliensis. The results show that MMP-9 has significantly higher gelatinolytic activity in L. amazonensis compared to L. braziliensis. The study suggests that MMP-2 and MMP-9 may play a role in the infection dynamics of these Leishmania species and could be potential markers for severe leishmaniasis and therapeutic targets.
Article
Multidisciplinary Sciences
Tarfah Al-Warhi, Matokah Abualnaja, Ola A. Abu Ali, Najiah M. Alyamani, Fahmy G. Elsaid, Ali A. Shati, Sarah Albogami, Eman Fayad, Ali H. Abu Almaaty, Khaled O. Mohamed, Wael M. Alamoudi, Islam Zaki
Summary: Z-configurated isomers are preferred molecules with significant applications in natural products, biologically active compounds, and organic synthesis. In this study, new thiazole analogs were synthesized and evaluated for their inhibitory activity against breast cancer cells and VEGFR-2. Compound 4d showed strong VEGFR-2 inhibitory activity and induced apoptosis through cell cycle arrest.
Article
Chemistry, Medicinal
Tao Chen, Yun Huang, Junxian Hong, Xikang Wei, Fang Zeng, Jialin Li, Geting Ye, Jie Yuan, Yuhua Long
Summary: The latest research suggests that anti-tumor agents with COX-2 inhibitory activity may enhance their efficacy. A series of sclerotiorin derivatives were synthesized and screened for their cytotoxic and COX-2 inhibitory activity. Some compounds showed good cytotoxicity and moderate to good COX-2 inhibition, with potential as anti-tumor agents.
Review
Chemistry, Inorganic & Nuclear
Oguz Ozbek, Meliha Burcu Gurdere
Summary: 2-Aminothiazole derivatives exhibit versatile biological properties and have been extensively studied for their potential as novel drug active substances for cancer treatment. Research on the synthesis and properties of these compounds with anticancer properties is rapidly advancing, providing new directions for the development of alternative drugs for cancer treatment.
PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS
(2021)
Article
Oncology
Grzegorz Mlynarczyk, Monika Gudowska-Sawczuk, Barbara Mroczko, Marta Bruczko-Goralewska, Lech Romanowicz, Anna Tokarzewicz
Summary: Gelatinases A and B, also known as matrix metalloproteinase-2 and matrix metalloproteinase-9 respectively, play a crucial role in breaking down collagen in the extracellular matrix. This study examined the presence, activity, and expression of these gelatinases in human renal cancer. The results showed that MMP-9 had higher content but lower specific activity compared to MMP-2 in renal cancer. The study also revealed changes in the gelatinases in healthy and cancerous tissues of renal cell carcinoma, suggesting the potential of MMPs in the diagnosis and treatment of renal carcinoma.
Article
Biochemistry & Molecular Biology
Elena Chugunova, Gabriele Micheletti, Dario Telese, Carla Boga, Daut Islamov, Konstantin Usachev, Alexander Burilov, Alena Tulesinova, Alexandra Voloshina, Anna Lyubina, Syumbelya Amerhanova, Tatiana Gerasimova, Aisylu Gilfanova, Victor Syakaev
Summary: A series of novel hybrid compounds containing benzofuroxan and 2-aminothiazole moieties were synthesized and found to exhibit potential as anticancer agents, with higher activity and lower toxicity compared to starting materials. The mechanism of action may involve apoptosis induction.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Arno Kirchhain, Asta Zubriene, Visvaldas Kairys, Federico Vivaldi, Andrea Bonini, Denise Biagini, Delio Santalucia, Daumantas Matulis, Fabio Di Francesco
Summary: Matrix metalloproteinases play a crucial role in cancer progression and metastasis, and molecular probes have been successfully used to study their activity. In this study, a series of MMP-2 and MMP-9 binding probes were synthesized, showing high selectivity against MMP-2 and potential for sensor fabrication. The experimental results were confirmed by molecular modeling, indicating the potential application of these probes for targeted enzyme detection.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Abdel Haleem M. Hussein, Ahmed A. Khames, Abu-Bakr A. El-Adasy, Ahmed A. Atalla, Mohamed Abdel-Rady, Mohamed I. A. Hassan, Mahrous A. Abou-Salim, Yaseen A. M. M. Elshaier, Assem Barakat
Summary: Research on new small molecules targeting PDEs, particularly PDE5, is a current and interesting topic. The designed aminothiazole compounds showed potential PDE5 inhibitory activity, with in vivo testing demonstrating similar effects to sildenafil without its known drawbacks, indicating they may be beneficial drug candidates for the treatment of erectile dysfunction.
Article
Biochemistry & Molecular Biology
Yassine Laamari, Ali Oubella, Abdoullah Bimoussa, Az-Eddine El Mansouri, El Mostafa Ketatni, Olivier Mentre, My Youssef Ait Itto, Hamid Morjani, Mostafa Khouili, Aziz Auhmani
Summary: A series of diverse triazoles linked to the hydroxyl group of totarol were synthesized and evaluated for their anticancer activity, showing moderate activities against cancer cell lines. The study provides important insights for further development of anticancer drugs. Compound 3g exhibited significant cytotoxicity against specific cancer cell lines and activated caspase-3 while inhibiting tubulin.
BIOORGANIC CHEMISTRY
(2021)
Article
Immunology
Xinying Zhou, Linmiao Lie, Yao Liang, Hui Xu, Bo Zhu, Yingqi Huang, Lijie Zhang, Zelin Zhang, Qianna Li, Qi Wang, Zhenyu Han, Yulan Huang, Honglin Liu, Shengfeng Hu, Chaoying Zhou, Qian Wen, Li Ma
Summary: This study reveals the significant role of GSK-3alpha/beta pathway in regulating immune response of macrophages to Mycobacterium tuberculosis infection. It also demonstrates that PKC-delta and mTOR can influence the activation of GSK-3alpha/beta and subsequently regulate the expression of MMP-1/9. These findings provide new insights into the immune escape mechanism of tuberculosis and the crosstalk between critical signaling pathways.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Chemistry, Medicinal
Piyusha P. Pagare, Aref Rastegar, Osheiza Abdulmalik, Abdelsattar M. Omar, Yan Zhang, Andrew Fleischman, Martin K. Safo
Summary: This review provides an overview of efforts to modulate Hb allosteric behavior for the treatment of SCD, focusing on aromatic aldehydes. The discovery of molecules like 5-HMF and Voxelotor has reinvigorated interest in developing Hb modulators, potentially providing highly effective oral therapy for SCD and other conditions. The field of Hb modulation is rapidly evolving, with a growing landscape of intellectual property and drug candidates in various stages of preclinical and clinical investigations.
EXPERT OPINION ON THERAPEUTIC PATENTS
(2022)
Article
Chemistry, Multidisciplinary
Maan T. Khayat, Abdelsattar M. Omar, Mahmoud A. Elfaky, Yosra A. Muhammad, Elaf A. Felemban, Khalid M. El-Say, Moustafa E. El-Araby
Summary: Chronic Hepatitis C is a global health threat that requires the development of new antiviral agents. This research focuses on the NS4A binding site to design peptidomimetic inhibitors for the HCV NS3 protease. The study used structure-based techniques to develop 1,2,3,4-tetrahydro-1,7-naphthyridine derivatives as NS4A core mimics. However, challenges were faced in terms of stability and binding potency.
HETEROATOM CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Maan T. Khayat, Abdelsattar M. Omar, Farid Ahmed, Mohammad I. Khan, Sara M. Ibrahim, Yosra A. Muhammad, Azizah M. Malebari, Thikryat Neamatallah, Moustafa E. El-Araby
Summary: This study investigated the structural-activity relationships (SARs) of tirbanibulin, a dual Src kinase/tubulin inhibitor. The newly synthesized compounds showed promising anticancer activity, with the most potent compound demonstrating cytotoxic effects against colon cancer and leukemia cell lines. Mechanistic studies revealed that this compound downregulates several kinases and suppresses specific signaling pathways, suggesting its potential as a lead compound for anticancer drug development.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Plant Sciences
Sabrin R. M. Ibrahim, Abdelsattar M. Omar, Alaa A. Bagalagel, Reem M. Diri, Ahmad O. Noor, Diena M. Almasri, Shaimaa G. A. Mohamed, Gamal A. Mohamed
Summary: Thiophenes are natural metabolites with diverse bioactivities. This review provides an overview of the natural thiophene derivatives reported in the past seven years, including their sources, biosynthesis, spectral data, and bioactivities. In addition, in silico studies were conducted using an artificial intelligence tool to predict potential drug targets and evaluate ligand-target interactions.
Article
Microbiology
Abdelsattar M. Omar, Gamal A. Mohamed, Sabrin R. M. Ibrahim
Summary: This review provides an overview of the research on fungal chaetomugilins and chaetoviridins, including their structures, separation, characterization, biosynthesis, and bioactivities. Additionally, their potential as antiviral agents against the SARS-CoV-2 protease is evaluated using docking studies and molecular dynamics simulations.
Article
Crystallography
Ahmed M. El-Agrody, Ahmed M. Fouda, Hany M. Mohamed, Mohammed Y. Alshahrani, Hazem A. Ghabbour, Abd El-Galil E. Amr, Rawda M. Okasha, Ahmed M. Naglah, Abdulrahman A. Almehizia, Ahmed A. Elhenawy
Summary: A target compound, 2-amino-4-(2,3-dichlorophenyl)-6-methoxy-4H-benzo[h]chromene-3-carbonitrile (4), was successfully synthesized and characterized. In vitro experiments demonstrated its strong and selective cytotoxicity against cancer cell lines. Promising inhibition efficacy was observed against EGFR and VEGFR-2 kinases.
Article
Oncology
Abdelsattar M. Omar, Maan T. Khayat, Farid Ahmed, Yosra A. Muhammad, Azizah M. Malebari, Sara M. Ibrahim, Mohammad I. Khan, Dhaval K. Shah, Wayne E. Childers, Moustafa E. El-Araby
Summary: Tirbanibulin (KX2-391) exhibits dual inhibition of Src kinase and tubulin polymerization, showing universal anti-cancer activity. However, analogues of KX2-391 have been found to inhibit oncogenic kinases other than Src. Compound 4e, a synthesized analogue, exhibits higher activity against leukemia cell lines and its mechanism does not involve tubulin polymerization or Src inhibition.
FRONTIERS IN ONCOLOGY
(2022)
Review
Food Science & Technology
Mohamed A. Farag, Mona. M. Rezk, Mohamed Hamdi Elashal, Moustafa El-Araby, Shaden. A. M. Khalifa, Hesham R. El-Seedi
Summary: Artificial sweeteners are popular worldwide due to their lower calorie content and potential health benefits. However, their safety remains controversial. This review focuses on low-calorie protein/peptide sweeteners, comparing synthetic and natural sweeteners, and presenting their health benefits and safety in terms of metabolic profiles and gut interaction.
FOOD RESEARCH INTERNATIONAL
(2022)
Article
Biochemistry & Molecular Biology
Gamal A. A. Mohamed, Abdelsattar M. M. Omar, Moustafa E. E. El-Araby, Shaza Mass, Sabrin R. M. Ibrahim
Summary: Tagetes minuta L. contains flavonoids that exhibit notable alpha-amylase inhibition, making them potential candidates for treating diabetes. These active compounds have favorable drug-like properties and further research is needed to validate their efficacy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Abdelsattar M. Omar, Osheiza Abdulmalik, Khalid M. El-Say, Mohini S. Ghatge, Mojisola Cyril-Olutayo, Steven Paredes, Mohammed Al-Awadh, Moustafa E. El-Araby, Martin K. Safo
Summary: This study designed and synthesized novel molecules to improve the metabolic stability of sickle cell disease and demonstrated their effectiveness in vitro.
CHEMICAL BIOLOGY & DRUG DESIGN
(2023)
Article
Biochemistry & Molecular Biology
Yosra A. Muhammad, Abdelsattar M. Omar, Farid Ahmed, Maan T. Khayat, Azizah M. Malebari, Sara M. Ibrahim, Shaza A. Mass, Mahmoud A. Elfaky, Moustafa E. El-Araby
Summary: Designing kinase inhibitors that bind to the substrate site of oncogenic kinases is a promising approach to kinase inhibition. In this study, compounds with ortho-substitutions were synthesized and their cellular and subcellular activities were investigated. One of the compounds showed substantial activity against cancer cell lines and exhibited similar trends in kinase inhibition as a previously identified compound.
CHEMICAL BIOLOGY & DRUG DESIGN
(2023)
Article
Chemistry, Multidisciplinary
Moustafa E. El-Araby, Mohammad I. Khan, Yosra A. Muhammad, Mohammed Razeeth Shait Mohammed, Mahmood H. Dalhat, Majed A. Alharbi, Shaza Mass, Magid Abou Gharbia, Maan T. Khayat, Abdelsattar M. Omar
Summary: AMP-activated Protein Kinase (AMPK) plays conflicting roles in solid tumor progression, having both anticancer effects and promoting the survival of existing cancer cells. The compound MAK-11 demonstrates high inhibitory effects on cancer growth, especially in 3D tumor models.
Article
Chemistry, Multidisciplinary
Hany E. A. Ahmed, Adel Amer, Samir A. Senior, Saleh Ihmaid, Mohammad Almalghrabi, Abdel-Moneim El Massry, Sahar Ahmed, Arafa Musa, Mohannad A. Almikhlafi, Samir A. Salama, Ahmed A. Elhenawy
Summary: In this study, new active 1,2,4-triazine derivatives were identified as novel cancer preventive agents that target CYP1A1 activity through the application of quantitative structure-activity relationship (QSAR) theory. The activities of newly synthesized analogs were successfully predicted using a rational guide provided by the QSAR equation. DFT calculation and molecular modeling analysis were used to determine the physicochemical parameters and binding interactions of the investigated compounds.
JOURNAL OF COMPUTATIONAL BIOPHYSICS AND CHEMISTRY
(2022)
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)