Design, synthesis, and biological evaluation of tyrcinnamine derivatives as bactericides [0.03%]
酪氨链霉素衍生物的 дизайн, 合成和 生物 评价作为细菌icide
Lijie Zheng,Baoyue Wei,Ji Pang et al.
Lijie Zheng et al.
Structural modification of bioactive natural products plays a vital role in the development of new drugs. Herein, we report the design and synthesis of twelve new tyrcinnamin derivatives (6a-8a, 6b-7b, 6c-8c, 10, and 13-15) using tyrcinnami...
2 H-pyrazolo[3,4- d]pyrimidin-4-amine derivatives as novel selective fibroblast growth factor receptor 2 (FGFR2) inhibitors [0.03%]
两种H-吡唑并[3,4-d]嘧啶-4-胺衍生物作为新型选择性成纤维细胞生长因子受体2（FGFR2）抑制剂的研究
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...
PROTACs in cancer therapy: targeted degradation of GPX4, PARP and epigenetic regulators [0.03%]
癌细胞治疗中的靶向蛋白降解：GPX4、PARP及表观遗传调控因子 PROTACs 的研究进展
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%]
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...