Discovery, biological evaluation, and molecular modeling of novel alkylamine-based Cbl-b inhibitors [0.03%]
Jinyu Tu,Yi Guan,Xi Gu et al.
Jinyu Tu et al.
Cbl-b, an E3 ubiquitin ligase, is a critical negative regulator of T-cell activation and an attractive target for cancer immunotherapy. Current small-molecule inhibitors largely rely on hydrophobic π-π stacking interactions with the gatek...
Biosynthesis-guided classification of Hirsutane sesquiterpenoids and their structural diversification [0.03%]
Mengjiao Guo,Chunlei Wang,Chengwei Liu
Mengjiao Guo
Hirsutane-type sesquiterpenoids are a distinctive class of fungal natural products characterized by a compact linear triquinane (5/5/5) scaffold. First reported in 1947, this family has expanded to structurally diverse metabolites exhibitin...
Heteroatom-modified chlorins in photodynamic therapy: phosphorus- and sulfur-containing strategies to enhance targeting and selectivity [0.03%]
J A Sutemieva,D V Sobenin
J A Sutemieva
Chlorins are widely used chromophores in photodynamic therapy, yet their performance is often limited by aqueous aggregation, nonoptimal biodistribution, insufficient control over intracellular localization, and microenvironmental constrain...
Pyrazolo[1,5-c]quinazoline-based heterocycles exhibit potent antileishmanial activity: Mechanistic insights and toxicity profile [0.03%]
Sandeep Kaur,Kushvinder Kumar,Shivani Thakur et al.
Sandeep Kaur et al.
Leishmaniasis remains a major global health challenge, with current chemo-therapeutics limited by high cost, toxicity, and poor bio-availability. In this study, seventeen new pyrazolo[1,5-c]quinazoline derivatives were designed and synthesi...
Investigation of tyrosinase inhibitory components in Camellia reticulata and the inhibitory mechanism, binding behavior of TeGG to tyrosinase [0.03%]
Chunhao Yang,Zhongyi Chen,Xiuxia Yang et al.
Chunhao Yang et al.
Camellia reticulata Lindl., an ornamental plant cultivated in Southwest China, was investigated as a potential source of novel natural tyrosinase inhibitors. Three tannins, 1,2,3,6-tetragalloylglucose (TeGG), procyanidin B2, and procyanidin...
Targeted design of a novel fungicide against the cytochrome bc1 complex: Mechanistic insights and potent antifungal activity [0.03%]
Min Liu,Siying Yu,Ji Liu et al.
Min Liu et al.
Conventional non-covalent bc1 complex inhibitors are widely used in plant fungal disease control, but their efficacy is increasingly compromised by resistance, underscoring the need for new agents. To address this, a series of cytochrome bc...
ATI-1 mediated disruption of the VCP-UFL1-Beclin1 axis thwarts autophagy initiation to trigger metabolic catastrophe in autophagy-addicted cancers [0.03%]
Tong Liu,Min Zhao,Jing Gao et al.
Tong Liu et al.
Targeting autophagy initiation represents a promising strategy to disrupt the metabolic resilience of cancer cells. In this study, we identified ATI-1 as a novel small-molecule inhibitor that selectively blocks the early stages of autophago...
Jin-Xin Wang,Xin-Miao Wu,Shao-Lin Zhang et al.
Jin-Xin Wang et al.
A unique type of naphthalimide-derived cephalosporins (NCs) as potential multitargeting antibacterial candidates was developed to address the growing threat of drug-resistant bacteria. Some prepared NCs exhibited potent antibacterial activi...
Carltonine B derivatives: Synthesis and structure-activity relationship insights for selective butyrylcholinesterase inhibition [0.03%]
Abdullah Al Mamun,Jan Konecny,Martina Hrabinova et al.
Abdullah Al Mamun et al.
Butyrylcholinesterase (BChE) is recognized as a promising therapeutic target for the late stages of Alzheimer's disease (AD) due to its role in the hydrolysis of acetylcholine (ACh), while acetylcholinesterase (AChE) activity declines durin...
Behlis Onder,Berna Erdogdu,Sefik Onder et al.
Behlis Onder et al.
The global rise of antimicrobial resistance has renewed interest in phage therapy as a viable alternative to conventional antibiotics. Reliable assessment of the therapeutic potential of bacteriophages requires advanced analytical strategie...