Structure-Based Rational Design and Evaluation of BET-Aurora Kinase Dual-Inhibitors for Treatment of Cancers.

Simultaneous inhibition of the bromodomain and extra-terminal domain and Aurora kinases is a promising anticancer therapeutic strategy. Based on our previous study on BET-kinase dual inhibitors, we employed the molecular docking approach to design novel dual BET-Aurora kinase A inhibitors. Through several rounds of optimization and with the guidance of the solved cocrystal structure of BRD4 bound to inhibitor , we finally obtained a series of highly potent dual BET-Aurora kinase A inhibitors.

An arabinogalactan from Lycium barbarum mitigated DSS caused intestinal injury via inhibiting mucosal damage and regulating the gut microbiota disorder.

Intestinal injury and microbiota disorder take part in the development of UC. In this research, we obtained an arabinogalactan (LBP-m) from Lycium barbarum and firstly characterized its physicochemical properties. LBP-m was a homogeneous polysaccharide (172 kDa) consisted of Ara, Gal, Glc, GalA, and GlcA with a mole ratio of 1.

Regulation of macrophage-mediated osteogenesis by kaempferol liposomes in trauma-induced heterotopic ossification.

Background: Heterotopic ossification (HO) is characterized by abnormal bone formation outside the skeleton following injury or inherited disease, leading to limb dysfunction and neurological deficits. Current treatment options for HO are largely ineffective.

Methods: A network pharmacological analysis was conducted to identify the active ingredients and protein targets in Astragalus and Cinnamon Twig Five-Substance Decoction (ACTFSD) on HO.

Discrimination of Benign and Malignant Thyroid Nodules through Comparative Analyses of Human Saliva Samples via Metabolomics and Deep-Learning-Guided Label-free SERS.

Thyroid nodules are a very common entity. The overall prevalence in the populace is estimated to be around 65-68%, among which a small portion (less than 5%) is malignant (cancerous). Therefore, it is important to discriminate benign thyroid nodules from malignant thyroid nodules.

Enhanced Control of Nonlinear Systems Under Control Input Constraints and Faults: A Neural Network-Based Integral Fuzzy Sliding Mode Approach.

Many existing control techniques proposed in the literature tend to overlook faults and physical limitations in the systems, which significantly restricts their applicability to practical, real-world systems. Consequently, there is an urgent necessity to advance the control and synchronization of such systems in real-world scenarios, specifically when faced with the challenges posed by faults and physical limitations in their control actuators. Motivated by this, our study unveils an innovative control approach that combines a neural network-based sliding mode algorithm with fuzzy logic systems to handle nonlinear systems.