Taxane-type anticancer drugs, including paclitaxel and its semi-synthetic derivatives docetaxel and cabazitaxel, are widely applied to chemotherapy of malignancy like breast cancer, ovarian cancer, non-small cell lung cancer and prostate cancer. However, their clinical applications are generally limited by scarce natural resources, various side effects and multidrug resistance. Therefore, it is significant to develop paclitaxel-mimics with simplified structure, fewer side effects and improved pharmaceutical properties. Based on our investigation on chemistry of paclitaxel, the current review summarized the most recent advances in the design, synthesis and biological activities of paclitaxel-mimics, which could be appealing to researchers in the field of medicinal chemistry and oncology. Meanwhile, smart design, interesting synthesis and potential bioactivities of these novel compounds may also provide valuable reference for the wider scientific communities.
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http://dx.doi.org/10.1016/j.fitote.2016.02.010 | DOI Listing |
Am J Physiol Heart Circ Physiol
January 2025
Comenius University Bratislava, Faculty of Pharmacy, Department of Pharmacology and Toxicology, Bratislava, Slovakia.
Cholinesterase (ChE) inhibitors are under consideration to be used in the treatment of cardiovascular pathologies. A prerequisite to advancing ChE inhibitors into the clinic is their thorough characterization in the heart. The aim here was to provide a detailed analysis of cardiac ChE to understand their molecular composition, localization, and physiological functions.
View Article and Find Full Text PDFJAMA Neurol
January 2025
Department of Neurology, Beijing Tiantan Hospital, Capital Medical University, Beijing, China.
Importance: Trials have not demonstrated superiority of alteplase or tenecteplase vs standard care in patients with mild stroke and have raised safety concerns. Prourokinase is an alternative fibrinolytic that may have a favorable safety profile, and the benefit-risk profile of prourokinase in mild stroke is unknown.
Objective: To investigate the efficacy and safety of prourokinase in mild ischemic stroke within 4.
Cell Biochem Biophys
January 2025
Department of Electronics and Communication Engineering, Hajee Mohammad Danesh Science and Technology University, Dinajpur, 5200, Bangladesh.
Blood components play a crucial role in maintaining human health and accurately detecting them is essential for medical diagnostics. A cutting-edge sensor utilizing PCF revealed to precisely identify a wide range of blood components with WBCs (white blood cells), RBCs (red blood cells), HB (hemoglobin), platelets, and plasma. A numerical analysis was performed using COMSOL Multiphysics software to assess the capabilities of the sensor.
View Article and Find Full Text PDFDiscov Nano
January 2025
Institute of Physiology II, University of Münster, Robert-Koch-Str. 27b, 48149, Münster, Germany.
Metastatic cancer cells undergo metabolic reprogramming, which involves changes in the metabolic fluxes, including endocytosis, nucleocytoplasmic transport, and mitochondrial metabolism, to satisfy their massive demands for energy, cell division, and proliferation compared to normal cells. We have previously demonstrated the ability of two different types of compounds to interfere with linchpins of metabolic reprogramming, Pitstop-2 and 1,6-hexanediol (1,6-HD). 1,6-HD disrupts glycolysis enzymes and mitochondrial function, enhancing reactive oxygen species production and reducing cellular ATP levels, while Pitstop-2 impedes clathrin-mediated endocytosis and small GTPases activity.
View Article and Find Full Text PDFFunct Integr Genomics
January 2025
Children's Medical Center, Peking University First Hospital, No.5 Le Yuan Road, Daxing District, 100034, Beijing, China.
Long-read sequencing has emerged as a transformative technology in recent years, offering significant potential for the molecular diagnosis of unresolved genetic disorders. Despite its promise, the comprehensive detection and clinical annotation of genomic variants remain intricate and technically demanding. We present SUMMER, an integrated and structured workflow specifically designed to process raw Nanopore sequencing reads.
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