Phosphorylation of G Protein-Coupled Receptors: From the Barcode Hypothesis to the Flute Model [0.03%]
从扫描仪假说至长号模型-七回转蛋白偶联受体的磷酸化研究进展
Zhao Yang,Fan Yang,Daolai Zhang et al.
Zhao Yang et al.
Seven transmembrane G protein-coupled receptors (GPCRs) are often phosphorylated at the C terminus and on intracellular loops in response to various extracellular stimuli. Phosphorylation of GPCRs by GPCR kinases and certain other kinases c...
AEE788 Inhibits Basal Body Assembly and Blocks DNA Replication in the African Trypanosome [0.03%]
AEE788抑制基础体组装并阻止非洲锥虫DNA复制
Catherine Sullenberger,Daniel Piqué,Yuko Ogata et al.
Catherine Sullenberger et al.
Trypanosoma brucei causes human African trypanosomiasis (HAT). The pyrrolopyrimidine AEE788 (a hit for anti-HAT drug discovery) associates with three trypanosome protein kinases. Herein we delineate the effects of AEE788 on T. brucei using ...
Xin Xin Xiong,Xin Yao Qiu,Dian Xing Hu et al.
Xin Xin Xiong et al.
Hepatocellular carcinoma (HCC) is the fifth most common and the third most deadly malignant tumor worldwide. Hypoxia and related oxidative stress are heavily involved in the process of HCC development and its therapies. However, direct and ...
SH479, a Betulinic Acid Derivative, Ameliorates Experimental Autoimmune Encephalomyelitis by Regulating the T Helper 17/Regulatory T Cell Balance [0.03%]
SH479通过调节T辅助细胞17/调节性T细胞平衡改善实验性自身免疫性脑脊髓炎
Jing Li,Ji Jing,Yang Bai et al.
Jing Li et al.
CD4+ T helper cells, especially T helper 17 (TH17) cells, combined with immune regulatory network dysfunction, play key roles in autoimmune diseases including multiple sclerosis (MS). Betulinic acid (BA), a natural pentacyclic triterpenoid,...
p38 β Mitogen-Activated Protein Kinase Signaling Mediates Exenatide-Stimulated Microglial β-Endorphin Expression [0.03%]
P38β丝裂原活化蛋白激酶介导胰高血糖素样肽-1受体激动剂刺激的小胶质细胞内源性大麻素生成
Hai-Yun Wu,Xiao-Fang Mao,Hui Fan et al.
Hai-Yun Wu et al.
Recent discoveries established that activation of glucagon-like peptide-1 receptors (GLP-1Rs) mediates neuroprotection and antinociception through microglial β-endorphin expression. This study aimed to explore the underlying signaling mech...
GRK2 Mediates Arginine Vasopressin-Induced Interleukin-6 Production via Nuclear Factor-κB Signaling Neonatal Rat Cardiac Fibroblast [0.03%]
精氨酸血管紧张素诱导核因子通过GRK2介导的新生大鼠心脏纤维化细胞信号传导诱导白细胞介素-6产生
Feifei Xu,Shuzhen Sun,Xiaojun Wang et al.
Feifei Xu et al.
Interleukin 6 (IL-6), which is elevated in patients with congestive heart failure and acts as both a chronic marker of inflammation and an acute-phase reactant, is associated with myocardial damage. Circulating levels of arginine vasopressi...
Differential Effects of Oxytocin Receptor Antagonists, Atosiban and Nolasiban, on Oxytocin Receptor-Mediated Signaling in Human Amnion and Myometrium [0.03%]
催产素受体拮抗剂阿托西班和诺拉西班对人胎盘膜和子宫肌层中催产素受体介导的信号转导的影响不同
Sung Hye Kim,Oliver Pohl,Andre Chollet et al.
Sung Hye Kim et al.
One of the most established roles of oxytocin (OT) is in inducing uterine contractions and labor. Apart from inducing contractions, our recent studies showed that OT can also activate proinflammatory pathways in both human myometrial and am...
Structural and Preclinical Studies of Computationally Designed Non-Nucleoside Reverse Transcriptase Inhibitors for Treating HIV infection [0.03%]
计算设计用于治疗HIV感染的非核苷逆转录酶抑制剂的结构和药理研究
Shalley N Kudalkar,Jagadish Beloor,Albert H Chan et al.
Shalley N Kudalkar et al.
The clinical benefits of HIV-1 non-nucleoside reverse transcriptase (RT) inhibitors (NNRTIs) are hindered by their unsatisfactory pharmacokinetic (PK) properties along with the rapid development of drug-resistant variants. However, the clin...
A New Molecular Mechanism To Engineer Protean Agonism at a G Protein-Coupled Receptor [0.03%]
在G蛋白偶联受体上工程化变构激动的新分子机制
Anna De Min,Carlo Matera,Andreas Bock et al.
Anna De Min et al.
Protean agonists are of great pharmacological interest as their behavior may change in magnitude and direction depending on the constitutive activity of a receptor. Yet, this intriguing phenomenon has been poorly described and understood, d...
Sequence-Specific Regulation of Endocytic Lifetimes Modulates Arrestin-Mediated Signaling at the µ Opioid Receptor [0.03%]
µ阿片受体的序列特异性内吞寿命调节对其介导的神经激肽受体信号的影响
Zara Y Weinberg,Amanda S Zajac,Tiffany Phan et al.
Zara Y Weinberg et al.
Functional selectivity at the µ opioid receptor (µR), a prototypical G-protein-coupled receptor that is a physiologically relevant target for endogenous opioid neurotransmitters and analgesics, has been a major focus for drug discovery in...