Constitutive activity among orphan G protein-coupled receptors: Molecular mechanisms and pharmacological perspectives [0.03%]
孤儿G蛋白偶联受体的组成型活化：分子机制与药理学观点
Ryan E Murphy,Hudson R Smith,John A Allen
Ryan E Murphy
Recent advancements in the study of orphan G protein-coupled receptors (oGPCRs) have revealed a large number with high levels of constitutive G protein signaling. Structural studies have suggested a new paradigm in which many constitutively...
Amantadine derivative Amt-1 enhances antiviral defense against influenza A virus via Nrf2/HO-1 pathway [0.03%]
胺达拉米衍生化合物Amt-1通过Nrf2/HO-1通路增强抗A型流感病毒的防御能力
Shixin Li,Jingyan Wei,Shaofen Zhou et al.
Shixin Li et al.
The rise of drug-resistant influenza A virus (IAV) strains and severe lung injury caused by excessive inflammation highlight the need for new antivirals that combine antiviral and immunomodulatory effects. Adamantane, an established anti-IA...
Transient receptor potential ankyrin 1 promotes the expression of interferon-stimulated antiviral genes in human A549 lung epithelial cells [0.03%]
瞬时受体电位锚定1通道蛋白促进人A549肺上皮细胞中I型干扰素刺激的抗病毒基因表达
Samu Luostarinen,Antti Pemmari,Julia Vistbacka et al.
Samu Luostarinen et al.
Transient receptor potential ankyrin 1 (TRPA1) is an ion channel known for its chemosensory function in neurons, causing pain and neurogenic inflammation. TRPA1 is activated by many noxious compounds including some inflammatory mediators. W...
Mechanism-based inactivation of human aldehyde oxidase by erlotinib: Mechanistic insights from structural analogs and molecular docking [0.03%]
基于机制的依洛替尼对人类醛氧化酶失活：结构类似物和分子对接的机理见解
Jia Rong Kweh,Nicholas Kai Ming Ng,Le Min Ngoh et al.
Jia Rong Kweh et al.
Aldehyde oxidase (AOX1) is a cytosolic molybdo-flavoenzyme that metabolizes azaheterocyclic drugs. Erlotinib and gefitinib are azaheterocyclic drugs. We deployed structural analogs to investigate the molecular interaction between these drug...
Rajika Roy,Walter J Koch
Rajika Roy
G protein-coupled receptor kinases (GRKs) are a class of serine/threonine kinases that shut down active signaling mediated by agonist-bound G protein-coupled receptors. Of all the diseases that arise from dysfunctional G protein-coupled rec...
Elucidating molecular mechanisms governing tumor necrosis factor-alpha-mediated regulation of amyloid beta 42 uptake in blood-brain barrier endothelial cells [0.03%]
阐明肿瘤坏死因子α介导的血脑屏障内皮细胞摄取β淀粉样蛋白42的分子机制
Vrishali S Salian,Geoffry L Curan,Val J Lowe et al.
Vrishali S Salian et al.
Cerebrovascular inflammation is prevalent in a majority of patients with Alzheimer disease. Elevated levels of inflammatory cytokines, such as tumor necrosis factor-α (TNF-α), circulating in the plasma have been shown to cause the inflamm...
The effects of hippocampal miR-34c-5p on the age-related discrepancies in susceptibility to traumatic stress in the post-traumatic stress disorder mice model [0.03%]
海马区miR-34c-5p在应激性创伤易感性的年龄差异中的作用机制研究小鼠 PTSD 模型中的作用效应研究
Shuwen Yu,Ting Li,Tingting Li et al.
Shuwen Yu et al.
Post-traumatic stress disorder is a highly prevalent and debilitating psychiatric condition characterized by symptoms such as depression, anxiety, and persistent fear. Although traumatic stress significantly affects both adolescents and adu...
The utility of 2,5-dimethoxy-4-iodoamphetamine for the study of serotonin 2A and 2C receptors [0.03%]
2,5-二甲氧基-4-碘苯乙胺在五羟色胺2A和2C受体研究中的应用价值
Lindsay P Cameron,Alaina M Jaster,Raul A Ramos et al.
Lindsay P Cameron et al.
2,5-dimethoxy-4-iodoamphetamine (DOI) is a phenethylamine psychedelic with high affinity for 5-HT2 receptors. In 2022 and 2023, the US Drug Enforcement Administration proposed to place DOI, along with a similar compound, 2,5-dimethoxy-4-chl...
Activation of TRPV3 channels in bladder cancer cells stimulates ATP release [0.03%]
TRPV3通道在膀胱癌细胞中的激活刺激了ATP的释放
Jonas Janenz,Andrea Leipe,Nicole Urban et al.
Jonas Janenz et al.
Transient receptor potential vanilloid 3 (TRPV3) is a thermosensitive Ca2+-permeable ion channel that plays essential roles in epithelial barrier function. Although its expression and function have been well characterized in the skin and, t...
Emerging roles of ubiquitin-specific proteases in the cardiovascular system [0.03%]
泛素特异性蛋白酶在心血管系统中的新兴作用
Bipradas Roy,Preston C Nibley,Richard Jiang et al.
Bipradas Roy et al.
The universal posttranslational modification ubiquitination was originally discovered in the 1980s as a tag appended to cellular proteins to mark them for degradation by the 26S proteasomal complex. Subsequent discoveries have established u...