Development of a Cell-Based Recombinant Green Fluorescent Protein Assay System for Generalized Discovery of Viral Protease Inhibitors [0.03%]
一种用于常规发现病毒蛋白酶抑制剂的基于细胞的重组绿色荧光蛋白测定系统的开发
Yan Feng,Xiaoyan Wu,Ruiting Chen et al.
Yan Feng et al.
Viral proteases are critical targets for antiviral drug development, but current screening methods for protease inhibitors often require high biosafety levels or lack cell-based relevance. Here, we developed a novel cell-based assay system ...
Conformational Heterogeneity Underlying Divergent Signaling in Class A G Protein-Coupled Receptors [0.03%]
类A G蛋白偶联受体产生差异信号的构象异质性基础
Kyriakos Georgiou,Antonios Kolocouris
Kyriakos Georgiou
Class A G protein-coupled receptors (GPCRs) are targets for ∼36% of commercial drugs. GPCRs in their apo-forms exhibit conformational heterogeneity, and more than a single active and inactive conformation exists in equilibrium. Distinct tr...
Mapping the Progression of Therapy-Induced Senescence to Therapy Tolerance: An Evolutionarily Conserved Mechanism for Optimizing Cancer Treatment with Senotherapeutics [0.03%]
将由治疗诱导衰老进展至治疗耐受的机制映射出来：一种通过使用抗衰老疗法优化癌症治疗的进化保守机制
Gargi Mukherjee,Neha Dutta,Muthumeena Ramanathan et al.
Gargi Mukherjee et al.
Therapy-induced senescence (TIS) is a reversible growth arrest induced by anticancer treatments, which may contribute to the development of long-term therapy resistance in tumor cells. Senotherapeutics, agents targeting senescent cells, are...
Treatment of Parkinson's Disease with an Anti-Inflammasome NLRP3 Inhibitor Derived from a Natural Product [0.03%]
来自天然产物的抗炎小体NLRP3抑制剂治疗帕金森病
Wenqian Li,Jiuliang Zhang,Qiang Chen et al.
Wenqian Li et al.
Parkinson's disease (PD), the second most prevalent neurodegenerative disorder afflicting human health, is primarily characterized by the degeneration of dopaminergic neurons in the midbrain, leading to movement disorders as the main clinic...
Chrono-Pharmacology for Cancer: Harnessing Circadian Regulations of the Cell Cycle and Immune Response Dynamics for Precision Therapy [0.03%]
肿瘤chrono药理学：利用生物钟调节细胞周期和免疫反应动力学的精准治疗
Murlidhar Madhukar,Sandip Das,Kavipriya M et al.
Murlidhar Madhukar et al.
The circadian rhythms and cell cycle are closely interlinked, creating a fundamental regulatory axis vital for tissue homeostasis, which is frequently dysregulated in cancers. The circadian apparatus, which is regulated by the core clock co...
N'‑(1-Phenylethylidene)benzohydrazide Cytotoxicity Is Lysine-Specific Demethylase 1 Independent and Linked to Iron-Sulfur Cluster Disruption in Ewing Sarcoma [0.03%]
N'-(1-苯乙基亚甲基)水杨酰肼细胞毒性独立于赖氨酸去甲基化酶1且与伊文斯肉瘤中的铁硫辅因子簇紊乱相关
John W Sherman,Galen C Rask,Bingcong Xiong et al.
John W Sherman et al.
The noncompetitive lysine-specific demethylase 1 (LSD1) inhibitors SP-2509 and SP-2577 are N'-(1-phenylethylidene)-benzohydrazides that display potent activity in Ewing sarcoma. They block transcriptional regulation of the causative oncogen...
Lands' Cycle at the Crossroads: Phospholipid Remodelling, Oxidative Stress, Cellular Toxicity, and Therapeutic Targeting [0.03%]
磷脂重塑、氧化应激、细胞毒性与治疗靶向的十字路口：lands途径处在转折点上
Airam Roggero,Marcos H Toyama,Sergio F Sousa
Airam Roggero
The Lands cycle is a fundamental process for the continuous renewal of phospholipids in cell membranes, directly influencing their fluidity and functionality. This cycle is particularly active in tissues such as the nervous and immune syste...
Atomoxetine Drug Properties for Repurposing as a Candidate Alzheimer's Disease Therapeutic Agent [0.03%]
用于老药新用的托莫西汀的药物属性以治疗阿尔茨海默病
Laura L Demsey,Danielle Burch,Evan Lin et al.
Laura L Demsey et al.
Ongoing Alzheimer's disease (AD) drug development research addresses the need for therapeutic agents that can ameliorate cognitive symptoms and attenuate the course of AD synaptic deficits and neurodegeneration. There is growing interest in...
Mild and Severe Hypertension Differentially Induce Internal Circadian Misalignment, Sleep-Wake Fragmentation, and Neurocardiac Desynchronization in Rats [0.03%]
轻度和重度高血压在大鼠中诱导不同的内源性昼夜节律失调、睡眠片段化及神经心血管不同步现象
Neeraj Kumar,Sairam Krishnamurthy
Neeraj Kumar
Hypertension is a major cardiovascular risk factor that perturbs neurohumoral regulation, yet its integrated effects on circadian sleep-wake organization and neurocardiac coupling remain unclear. We examined whether the severity of hyperten...
Development of Novel 18F‑Labeled Selective Orexin‑2 Receptor Radioligands for Positron Emission Tomography [0.03%]
新型氟-18标记的选择性下丘脑泌素-2受体放射配体正电子发射断层显像的发展
Jian Rong,Chunyu Zhao,Ahmad F Chaudhary et al.
Jian Rong et al.
The orexin-2 receptor (OX2R), a G protein-coupled receptor activated by the neuropeptides, orexin A and B, plays an integral role in orchestrating motivation, feeding behavior, and the sleep-wake cycle. Pharmacological modulation of OX2R ha...