Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
Similar Publications
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 PDFTowards Improved Peptidic α-Ketoamide Inhibitors of the Plasmodial Subtilisin-Like SUB1: Exploration of N-Terminal Extensions and Cyclic Constraints.
ChemMedChem
January 2025
Université de Montpellier: Universite de Montpellier, IBMM, Pôle Chimie Balard, Campus CNRS, 34093, Montpellier, FRANCE.
After more than 15 years of decline, the Malaria epidemy has increased again since 2017, reinforcing the need to identify drug candidates active on new targets involved in at least two biological stages of the Plasmodium life cycle. The SUB1 protease, which is essential for parasite egress in both hepatic and blood stages, would meet these criteria. We previously reported the structure-activity relationship analysis of α-ketoamide-containing inhibitors encompassing positions P4-P2'.
View Article and Find Full Text PDFPostcolitis Alterations in Dose-Dependent Effects of 5-HT1A Agonist Buspirone on Nociceptive Activity of the Raphe Magnus and Dorsal Raphe Neurons in Rats.
Eur J Neurosci
January 2025
Laboratory of Cortico-Visceral Physiology, Pavlov Institute of Physiology of the Russian Academy of Sciences, Saint Petersburg, Russia.
The serotonergic raphe magnus (RMg) and dorsal raphe (DR) nuclei are crucial pain-regulating structures, which nociceptive activity is shown to be altered in gut pathology, but the underlying neuroplastic changes remain unclear. Considering the importance of 5-HT1A receptors in modulating both pain and raphe neuronal activity, in this study, we aimed to determine whether 5-HT1A-dependent visceral and somatic nociceptive processing within the RMg and DR is modified in postcolitis conditions. In anaesthetised male Wistar rats, healthy control and recovered from TNBS-induced colitis, the microelectrode recordings of RMg and DR neuron responses to noxious colorectal distension (CRD) or tail squeezing (TS) were performed prior and after intravenous administration of 5-HT1A agonist, buspirone.
View Article and Find Full Text PDFWhole-genome sequencing and secondary metabolite exploration of the novel BN with broad-spectrum antagonistic activity against fungal plant pathogens.
Front Microbiol
January 2025
School of Biological and Pharmaceutical Engineering, Lanzhou Jiaotong University, Lanzhou, Gansu, China.
The utilization of chemical pesticides recovers 30%-40% of food losses. However, their application has also triggered a series of problems, including food safety, environmental pollution, pesticide resistance, and incidents of poisoning. Consequently, green pesticides are increasingly seen as viable alternatives to their chemical counterparts.
View Article and Find Full Text PDFSulforaphane as a promising anti-caries agents: inhibitory effects on and caries control in a rat model.
Front Microbiol
January 2025
State Key Laboratory of Oral Diseases & National Center for Stomatology & National Clinical Center for Oral Diseases, West China Hospital of Stomatology, Sichuan University, Chengdu, Sichuan, China.
Dental caries has been one of the most prevalent diseases globally over the last few decades, threatening human oral and general health. The most critical aspect in caries control is to inhibit the dominant cariogenic bacteria (). Sulforaphane (SFN), a compound found in a wide range of cruciferous plants, has demonstrated bacteriostatic activities against various pathogenic bacteria.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!