PTC-Assisted Chemoselective S-Alkylation of 5-Mercapto-1,3,4-Oxadiazol Derivative: Multi-Target Anticancer via EGFR, Telomerase, and Thymidylate Synthase Inhibition With Apoptosis Induction [0.03%]
基于PTC导向的化学选择性S-烷基化合成5-巯基-1,3,4-恶二唑衍生物及其抗癌活性研究
Asmaa Zakaria,Ahmed A Al-Karmalawy,Samia S Hawas et al.
Asmaa Zakaria et al.
Multi-target enzyme inhibition represents a promising strategy to overcome resistance and improve therapeutic outcomes in cancer therapy. In this study, a new series of 1,3,4-oxadiazole derivatives was synthesized and evaluated for cytotoxi...
Heteromerization, Biased Agonism, and Allosteric Modulation of G Protein-Coupled Receptors in Addiction: Mechanistic Insights and Therapeutic Implications [0.03%]
成瘾障碍中G蛋白偶联受体异聚化、偏向性激动和别构调节的机制及治疗意义
Khaled A Alhosaini,Mohammed M Alanazi,Ibrahim N Alsulaihim et al.
Khaled A Alhosaini et al.
G protein-coupled receptors (GPCRs) are core transducers of psychoactive drug action, shaping second messenger signaling, ion channel function, and neurotransmitter release in reward- and stress-related circuits. Despite decades of therapeu...
FGF18 Ameliorates HIV-1 Tat-Induced Blood-Brain Barrier Disruption via Wnt/β-Catenin Signaling [0.03%]
FGF18通过Wnt/β-catenin信号传导改善HIV-1 Tat诱导的血脑屏障破坏
Pengfei Zhang,Song Wei,Fanyu Fu et al.
Pengfei Zhang et al.
Dysregulated expression of tight junction proteins and compromise of blood-brain barrier (BBB) integrity are associated with pathological progression of HIV-1-associated neurocognitive disorders (HAND). Fibroblast growth factor-18 (FGF18), ...
TRIM47 Promotes Atherosclerosis by Activating NF-κB Signaling via IκBα Ubiquitination [0.03%]
TRIM47通过IκBα泛素化激活NF-κB信号促进动脉粥样硬化
Xiaoming Qin,Jiachen Luo,Yiqian Yuan et al.
Xiaoming Qin et al.
Atherosclerosis, a major contributor to cardiovascular diseases, is characterized by chronic inflammation in arterial walls. The role of NF-κB signaling in this process is well-established, but the upstream regulators remain incompletely u...
Hexahydroquinoline Featuring Amide Functionality: A Promising Scaffold With Calcium Channel Blocking Activity [0.03%]
具有酰胺功能的己氢_QUINOLINE：一种有前途的钙通道阻滞剂骨架
Ebru Koçak Aslan,Kevin Lam,Sun Huang et al.
Ebru Koçak Aslan et al.
Hexahydroquinoline (HHQ) is a widely recognized scaffold that has garnered considerable attention owing to its diverse pharmacological properties. The structure of HHQ includes a 1,4-dihydropyridine (DHP) ring, which serves as the pharmacop...
Structure-Guided Optimization and Biological Validation of 1,3,4-Thiadiazole-Based SIRT2 Inhibitors Reinforcing Channel Entrance Interactions [0.03%]
基于结构的优化及生物验证硫氮杂环化合物SIRT2抑制剂以强化通道入口作用力
Ahmet Bugra Aksel,Fikriye Ozgencil,Filiz Bakar-Ates et al.
Ahmet Bugra Aksel et al.
SIRT2, the cytoplasmic member of the sirtuin family, is generally acknowledged to promote cancer and contribute to the progression of various pathologies, including neurodegeneration, inflammation, obesity, and bacterial infection through t...
Ceritinib Induces Mitochondrial Fragmentation in Thyroid Cancer Cells by Targeting Drp-1 [0.03%]
色瑞替尼通过靶向Drp-1诱导甲状腺癌细胞线粒体片段化
Dongguang Qin,Wei Ding,Xuesong Wu et al.
Dongguang Qin et al.
Mitochondrial dynamics play a crucial role in thyroid cancer progression by regulating apoptosis, metabolism, and oxidative stress. Ceritinib, a tyrosine kinase inhibitor, shows potential anticancer effects; however, its impact on mitochond...
Zeylenone Attenuates Tamoxifen Resistance by Directly Binding to CTCF and Inhibiting the CTCF-CENPK-JAK1/STAT3 Signaling Axis in Breast Cancer [0.03%]
泽来诺通过直接与CTCF结合并抑制CTCF-CENPK-JAK1/STAT3信号轴来缓解乳腺癌中tamoxifen耐药性
Gang Li,Zhiping Deng,Wenqing Zhang et al.
Gang Li et al.
This study was designed to investigate the effects of zeylonone (Zey) on attenuating tamoxifen (TAM) resistance in breast cancer cells in vitro and in vivo and its underlying mechanisms. Database analysis and clinical sample validation reve...
Pyrrolidine Derivatives in Modern Drug Discovery: Emerging Structure Activity Relationships and Dual Antidiabetic-Anticancer Potential [0.03%]
现代药物发现中的吡咯烷衍生物：新兴的结构活性关系及潜在的抗糖尿病和抗癌作用
Aeyaz Ahmad Bhat,Meraj Ahmed,Noureddine Elboughdiri et al.
Aeyaz Ahmad Bhat et al.
Pyrrolidine, a five-membered nitrogen-containing heterocycle, has emerged as an important structural motif in medicinal chemistry owing to its pronounced pharmacological versatility, conformational flexibility, and favorable physicochemical...
Exploring Pyrazolo[3,4-b]Pyridine and Spiro-Oxindole Hybrids as Selective CDK2 or EGFR Inhibitors for Targeted Cancer Therapy: Design, Synthesis, and Molecular Modeling Insights [0.03%]
作为靶向癌症治疗的选择性CDK2或EGFR抑制剂的吡唑并[3,4-b]吡啶和螺-氧吲哚杂化的探索：设计、合成及分子建模见解
Ahmed K B A W Farouk,Aya A A Al-Tanany,Mohamed R Elnagar et al.
Ahmed K B A W Farouk et al.
A new series of pyrazolo[3,4-b]pyridine and spiro-oxindole derivatives were rationally designed, synthesized, and biologically assessed as either CDK2 or EGFR inhibitors with potential anticancer activity. The CDK2 inhibitory evaluation of ...