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Discovery of noncovalent diaminopyrimidine-based Inhibitors for glioblastoma via a dual FAK/DNA targeting strategy.
Eur J Med Chem
January 2025
School of Pharmaceutical Sciences, Guizhou University, Guiyang, 550025, China. Electronic address:
Temozolomide, a widely used alkylating agent for glioblastoma treatment, faces significant challenges due to the development of resistance, which severely impacts patient survival. This underscores the urgent need for novel strategies to overcome this barrier. Focal adhesion kinase (FAK), an intracellular non-receptor tyrosine kinase, is highly expressed in glioblastoma cells and has been identified as a promising therapeutic target for anti-glioblastoma drug development.
View Article and Find Full Text PDFInsights into NEK2 inhibitors as antitumor agents: From mechanisms to potential therapeutics.
Eur J Med Chem
January 2025
Department of Respiratory and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, Institute of Respiratory Healthand, Department of Frontiers Science Center for Disease-related Molecular Network, Core Facilities, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China. Electronic address:
NEK2, a serine/threonine protein kinase, is integral to mitotic events such as centrosome duplication and separation, microtubule stabilization, spindle assembly checkpoint, and kinetochore attachment. However, NEK2 overexpression leads to centrosome amplification and chromosomal instability, which are significantly associated with various malignancies, including liver, breast, and non-small cell lung cancer. This overexpression could facilitate tumor development and confer resistance to therapy by promoting aberrant cell division and centrosome amplification.
View Article and Find Full Text PDFTranscriptomic response of an algal species (raphidocelis subcapitata) exposed to 22 per- and polyfluoroalkyl substances.
Environ Toxicol Chem
January 2025
United States Environmental Protection Agency, Center for Computational Toxicology and Exposure, Great Lakes Toxicology and Ecology Division, Duluth, MN, USA.
Per- and polyfluoroalkyl substances (PFAS) are a large class of chemicals of concern for both human and environmental health because of their ubiquitous presence in the environment, persistence, and potential toxicological effects. Despite this, ecological hazard data are limited to a small number of PFAS even though there are over 4000 identified PFAS. Traditional toxicity testing will likely be inadequate to generate necessary hazard information for risk assessment.
View Article and Find Full Text PDFExploring the Anti-Adherence Potential of Skt35 to Combat Catheter-Associated Staphylococcus aureus Infections: Efficacy, Toxicity and Mechanism of Action.
Chem Biodivers
January 2025
Toxicology and Pharmacology Laboratory, Department of Biotechnology, Faculty of Science and Humanities, SRM Institute of Science and Technology, Kattankulatur, India.
Catheter-associated urinary tract infections (CAUTIs), often caused by biofilm-forming Staphylococcus aureus, present significant clinical challenges. Skt35, a dioxopiperidinamide derivative of cinnamic acid, was investigated for its potential antibacterial and antibiofilm activities against S. aureus biofilms.
View Article and Find Full Text PDFSpatiotemporal analysis of agricultural drought variability in the uMkhanyakude District Municipality, KwaZulu-Natal.
Environ Monit Assess
January 2025
Department of Life and Consumer Sciences, University of South Africa, Johannesburg, South Africa.
Exploring drought dynamics has become urgent due to unprecedented climate change. Projections indicate that drought events will become increasingly widespread globally, posing a significant threat to the sustainability of the agricultural sector. This growing challenge has resulted in heightened interest in understanding drought dynamics and their impacts on agriculture.
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