Puerarin alleviates type 2 diabetes by targeting AKT1 to inhibit ferroptosis: Integrating network pharmacology, proteomics and experimental validation [0.03%]
Yulin Chen,Xiaojie Wei,Tian Lin et al.
Yulin Chen et al.
The progression of type 2 diabetes mellitus (T2DM) is closely linked to oxidative stress-induced damage. Ferroptosis is a regulated form of cell death driven by iron-dependent lipid peroxidation. Its underlying mechanism involves an imbalan...
Quinoxaline-based scaffolds as dual VEGFR-2/EGFR kinase inhibitors and apoptotic inducers: Design, synthesis, anticancer evaluation, and in silico study [0.03%]
Alaa Elwan,Samiha A El-Sebaey,Hanan A Al-Ghulikah et al.
Alaa Elwan et al.
Dual inhibition of the epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor-2 (VEGFR-2) represents an effective strategy for achieving synergistic antitumor activity by simultaneously suppressing tumor pro...
Conformationally adaptive benzimidazolium-chalcone hybrid salts as selective TGF-β1 inhibitors [0.03%]
Ebru NurAy,Faruk Kaan Çelik,Hayrani Eren Bostancı et al.
Ebru NurAy et al.
The transforming growth factor-β (TGF-β) signaling pathway is crucial in promoting tumor growth, enabling tumors to evade immune responses, and contributing to resistance against therapies. As a result, it is a significant target for canc...
DA-5: A novel azaindole-based GPX4 inhibitor inducing ferroptosis for targeted therapy of triple-negative breast cancer [0.03%]
Jingjing Du,Kaiqiang Guo,ChaoJie Wang et al.
Jingjing Du et al.
Background: Triple-negative breast cancer (TNBC) is an aggressive subtype lacking the ER, PR, and HER2 receptors, with limited treatment options and poor prognosis. Ferroptosis, an iron-dependent form of regulated cell de...
Sulfated polysaccharides from Laminaria japonica and Porphyra inhibit SARS-CoV-2 main protease: mechanistic insights into molecular interactions [0.03%]
Jinwen Li,Shu Jie Li
Jinwen Li
The replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in host cells relies on its non-structural protein, the main protease (Mpro), a cysteine protease that serves as a primary target for antiviral drug design. Her...
Thieno[3,2-b]pyrrole-annulated BODIPYs: Charge-transfer-assisted intersystem crossing and NIR photosensitization for PDT [0.03%]
D V Sobenin,J A Sutemieva
D V Sobenin
This review focuses on thieno[3,2-b]pyrrole-fused BODIPYs, which serve as a heavy-atom-free alternative to traditional halogenated photosensitizers. This annulation strategy overcomes the limitations of the core platform, enabling efficient...
Discovery of undescribed lovastatin derivatives from Aspergillus aculeatus: natural quorum sensing inhibitors against Pseudomonas aeruginosa [0.03%]
Fei Liu,Yulin Lu,Yi Guo et al.
Fei Liu et al.
Quorum sensing inhibitors against Pseudomonas aeruginosa focus on the "antivirulence strategy" rather than the traditional "bactericidal strategy", promoting the transformation of anti-infective therapy from directly killing bacteria to reg...
Xue Zhao,Ruihan Zhang,Yihan Ma et al.
Xue Zhao et al.
Dysregulation of autophagy and mitophagy is a hallmark of neurodegenerative diseases, including Alzheimer's disease (AD). Chemical intervention targeting these pathways has emerged as one of the promising therapeutic strategies for neurodeg...
Co-crystals of berberine with two natural polyphenols: synthesis, crystal structure and bacteriostasis on aquatic pathogens [0.03%]
Zhi-Chuan Chen,Jia-Yi Li,Jian-Rong Teng et al.
Zhi-Chuan Chen et al.
Pharmaceutical co-crystals could modulate the physio-chemical properties of active pharmaceutical ingredients (APIs) and co-crystal formations (CCFs) via non-covalent interactions, including hydrogen bonds, π-π stacking and hydrophobic ef...
Design, synthesis, and anti-inflammatory evaluation of novel N-(Benzol[d]oxazol-5-yl)sulfonamides as NLRP3 inflammasome inhibitors [0.03%]
Zhendi Shi,Leyan Wang,Jiayue Huang et al.
Zhendi Shi et al.
Aberrant activation of the NLRP3 inflammasome drives the pathogenesis of numerous human inflammatory diseases, highlighting the urgent need for small-molecule inhibitors targeting NLRP3. Building upon the lead compound 15z, we designed and ...