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 ...
Discovery of novel coumarin-containing triazolo[1,5-a]pyrimidine derivatives as potent ABCB1 inhibitor for modulation of multidrug resistance [0.03%]
一类新型肉桂酰三唑并基嘧啶衍生物ABCB1抑制剂的发现及其逆转肿瘤多药耐药的作用研究
Nan Ye Hmone,Xuefei Tian,Dandan Zhou et al.
Nan Ye Hmone et al.
ABCB1-mediated drug efflux is a key determinant of multidrug resistance (MDR) in cancer. To overcome this mechanism, a series of thiol-substituted aminocoumarin-derived, coumarin-containing triazolo[1,5-a]pyrimidine derivatives (5a-5s) was ...
Reactive oxygen species (ROS) research in drug discovery and drug delivery: Can the medium Be a Trojan Horse disguised as something benign? [0.03%]
药物发现和给药中的活性氧（ROS）研究：媒介会是化身为无害之物的特洛伊木马吗？
Shubham Bansal,Binghe Wang
Shubham Bansal
In studying the roles of reactive oxygen species (ROS) in various biological processes, the availability of appropriate cell culture models is critical. Addition of H2O2 to cells is commonly used to simulate oxidative stress. In doing so, g...
Palladium-catalysed synthesis of small-molecule epigenetic inhibitors as anticancer therapeutics [0.03%]
钯催化合成小分子表观遗传抑制剂作为抗癌药物疗法
Ram Sharma,Mandeep Rana,Amandeep Thakur et al.
Ram Sharma et al.
Palladium-catalysed reactions have emerged as indispensable tools in medicinal chemistry, enabling the precise construction of C-C and C-N bonds across a wide spectrum of drug-like molecular frameworks. This manuscript comprehensively exami...
Design, synthesis and anti-breast cancer activity evaluation of 6,7-dihydro-5 H-pyrrolo[3,4- d]pyrimidine-based PARP1/ATR dual inhibitors [0.03%]
基于6,7-二氢-5H-吡咯并[3,4-D]嘧啶的PARP1 / ATR双靶点抑制剂的设计、合成及抗乳腺癌活性研究
Meng-Lan He,Zong-Hao Wang,Xia Yao et al.
Meng-Lan He et al.
PARP1 inhibitors are FDA-approved for BRCA1/2-mutated breast cancer but show limited efficacy in wild-type cancers and face resistance issues. To overcome these, we designed novel 6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidine-based compounds inte...
Diethyl Phthalate (DEP) as a potential osteosarcoma risk factor: a multi-omics study integrating network Toxicology, single-cell RNA sequencing, and molecular docking [0.03%]
邻苯二甲酸二乙酯(DEP)作为潜在骨肉瘤风险因素的组学研究：整合网络毒理学、单细胞RNA测序和分子对接分析
Shangqi Yin,Wuzheng Liu,Chunxiao Gao et al.
Shangqi Yin et al.
Diethyl phthalate (DEP), a common plasticiser and endocrine disruptor, has been linked to cancer, but its role in osteosarcoma (OS) remains unclear. This study integrated network toxicology, transcriptomics, protein-protein interaction (PPI...
Integrating virtual screening and molecular dynamics simulations to identify emodin as a PYCR1 inhibitor modulating docetaxel sensitivity in prostate cancer [0.03%]
基于虚拟筛选和分子动力学模拟整合的新型PYCR1抑制剂白鲜皮素并探索其对前列腺癌耐药逆转作用及机制研究
Shuai Liu,Yongfeng Lao,Long Cheng et al.
Shuai Liu et al.
Docetaxel (DTX) resistance is the main cause of treatment failure in castration-resistant prostate cancer (CRPC). Pyrroline-5-carboxylic acid reductase 1 (PYCR1) is an enzyme involved in proline metabolism. It is highly expressed in various...