Synthesis and structure-activity relationship study of a library of 1-substituted [1,2,4]triazolo[4,3- a]quinolines as valuable chemical probes for paraxonase-2 (PON2) [0.03%]
一类1位取代的[1,2,4]三氮唑并[4,3-a]喹啉化合物库的合成及其结构活性关系对叔丁基过氧化物酶(PON2)的有价值化学物质的作用研究
Elisa Bianconi,Eros Antonio Lampitella,Fatima Nigro et al.
Elisa Bianconi et al.
A plethora of studies have demonstrated the pathophysiological roles played by paraxonase 2 (PON2) in oxidative stress control, inhibition of apoptosis, infections, and the progression of various types of malignancies. The continuous intere...
Discovery of ferulic acid carbamate derivatives as dual-targeting agents of BuChE and Nrf2 for Alzheimer's disease [0.03%]
发现香豆酸碳酰胺衍生物作为BuChE和Nrf2双靶向剂用于阿尔茨海默病
Kejing Lao,Yingze Li,Yueyan Xiao et al.
Kejing Lao et al.
Given the multifactorial aetiology of Alzheimer's disease, multi-target strategies have emerged as a promising therapeutic approach. In this study, we designed and synthesised a series of ferulic acid carbamate derivatives to selectively in...
Inhibition of prolyl-tRNA synthetase and efflux pumps as a dual-targeting strategy against multidrug-resistant bacteria [0.03%]
针对耐多药细菌的脯氨酰-tRNA合成酶和外排泵双靶点抑制策略
Cristiane Tambascia,Jaqueline Cristina Silva,Barbara Carvalho Dos Reis et al.
Cristiane Tambascia et al.
Aminoacyl-tRNA synthetases have been widely exploited as targets for antiparasitic and antifungal inhibitors; however, they have received little attention as targets in multidrug-resistant (MDR) bacteria. Here we describe the biochemical ch...
Drug-likeness prioritised selection identifies anti- Escherichia coli candidates confirmed by molecular docking, dynamics simulations, and antibacterial assays [0.03%]
基于类药性优先筛选的体外抗大肠杆菌活性虚拟筛选及验证研究
Beibei Yu,Haoyu Zhu,Lu Xu et al.
Beibei Yu et al.
To address the imbalance between antibacterial potency and developability in cephalosporin discovery against Escherichia coli, we developed a comprehensive screening strategy guided by the principle of maximum drug-likeness. An integrated e...
Yiqian Hou,Yanying Zhao,Qinghua He et al.
Yiqian Hou et al.
The Warburg effect, a hallmark of cancer, positions lactate dehydrogenase (LDH) as a key therapeutic target. Mammals possess three LDH isozymes (LDH-A, LDH-B, LDH-C) with distinct properties. This review critically re-evaluates the simplist...
Screening of peptide inhibitors targeting YAP-TEAD4 interaction: affinity evaluation and anti-AML cell activity [0.03%]
靶向YAP-TEAD4相互作用的多肽抑制剂筛选：亲和力评价及抗白血病活性研究
Xiaotian Yang,Shudan Yang,Guoqiang Lin et al.
Xiaotian Yang et al.
Aberrant activation of YAP-TEAD4 drives tumorigenesis, progression, and chemoresistance. Disrupting their interaction serves as an alternative anticancer strategy, with peptides better adapting to the large, flat interaction interface. In t...
Application of 18 β-glycyrrhetinic acid Fluorescent probes in cell imaging [0.03%]
甘草次酸荧光探针的细胞成像应用研究
Yifan Zhao,Hongxia Sun,Zhiwei Yan et al.
Yifan Zhao et al.
Fluorescently labelled small molecule probes (fluorescent probes) play an important role in cell imaging and are often used in combination with light-affinity probes to determine the subcellular localisation of target proteins. To investiga...
Mislocalisation of FLT3-ITD receptor contributes to MV4-11 leukaemia cell resistance to antibody-drug conjugate [0.03%]
FLT3-ITD受体定位错误导致白血病细胞抵抗抗体药物偶联物治疗
Wariya Nirachonkul,Mark P Farrell,Thomas J Tolbert et al.
Wariya Nirachonkul et al.
FMS-like tyrosine kinase 3 (FLT3/CD135) regulates haematopoiesis and is frequently mutated as FLT3-internal tandem duplication (FLT3-ITD) in acute myeloid leukaemia (AML), associated with poor prognosis. Although FLT3 inhibitors show clinic...
Design, synthesis and antiproliferative activity of oxadiazole derivatives as potent glycogen synthase kinase-3/histone deacetylase 6 dual inhibitors [0.03%]
一类有效的糖原合成酶激酶-3/组蛋白去乙酰酶6双靶点抑制剂的氧化氮杂环化合物的设计、合成及抗增殖活性研究
Changchun Ye,Zilu Chen,Jiantao Jiang et al.
Changchun Ye et al.
A series of oxadiazole-based dual inhibitors targeting GSK3 and HDAC6 were rationally designed by integrating key pharmacophores into a single molecule. Among these derivatives, 4-(((5-(benzo[d][1, 3]dioxol-5-yl)-1,3,4-oxadiazol-2-yl)thio)m...
Pesticidal evaluation of novel dual-chiral N-cyano sulfiliminyl anthranilic diamides derivatives [0.03%]
新型双手性氰基磺酰亚胺基苯并恶嗪二酰胺类杀虫剂的开发研究
Xiaomin Li,Mukuo Wang,Shuying Li et al.
Xiaomin Li et al.
To develop eco-friendly pesticides with novel modes of action for insect management, a series of dual-chiral N-cyano sulfilimine-substituted anthranilic diamides were designed and synthesised de novo, and their insecticidal activities were ...