2 H-pyrazolo[3,4- d]pyrimidin-4-amine derivatives as novel selective fibroblast growth factor receptor 2 (FGFR2) inhibitors [0.03%]
Pinglian Wu,Zhaodi Tian,Weizhong Shen et al.
Pinglian Wu et al.
Although FGFR2 is a well-validated oncogenic target, no selective FGFR2 inhibitors have been approved for clinical use. In this study, we report the discovery of 2H-pyrazolo[3,4-d]pyrimidin-4-amine derivative as novel, irreversible FGFR2 in...
Sunny Periyasamy,Thyla Jarrett,Joe Truong et al.
Sunny Periyasamy et al.
The degradation of overexpressed proteins has emerged as a promising strategy for halting disease progression, particularly in cancer. Traditional small-molecule drugs often face limitations in the elimination of pathogenic proteins, leadin...
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%]
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%]
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...