cAMP Signaling Compartmentation: Adenylyl Cyclases as Anchors of Dynamic Signaling Complexes [0.03%]
环腺苷酸信号隔室化：环腺苷酸酶作为动态信号复合物的锚定位点
Timothy B Johnstone,Shailesh R Agarwal,Robert D Harvey et al.
Timothy B Johnstone et al.
It is widely accepted that cAMP signaling is compartmentalized within cells. However, our knowledge of how receptors, cAMP signaling enzymes, effectors, and other key proteins form specific signaling complexes to regulate specific cell resp...
S1P1 Modulator-Induced G αi Signaling and β-Arrestin Recruitment Are Both Necessary to Induce Rapid and Efficient Reduction of Blood Lymphocyte Count In Vivo [0.03%]
体内快速有效减少血液淋巴细胞计数需要S1P1调制剂诱导的Gαi信号和β-arrestin募集
Magdalena Birker-Robaczewska,Martin Bolli,Markus Rey et al.
Magdalena Birker-Robaczewska et al.
S1P1 (sphingosine-1-phosphate receptor 1) agonists prevent lymphocyte egress from secondary lymphoid organs and cause a reduction in the number of circulating blood lymphocytes. We hypothesized that S1P1 receptor modulators with pathway-sel...
Diversity of Nicotinic Acetylcholine Receptor Positive Allosteric Modulators Revealed by Mutagenesis and a Revised Structural Model [0.03%]
变体分析和修正结构模型揭示尼古丁乙酰胆碱受体阳性 allosteric 模仿物的多样性
Joseph Newcombe,Anna Chatzidaki,Tom D Sheppard et al.
Joseph Newcombe et al.
By combining electrophysiological and computational approaches we have examined a series of positive allosteric modulators (PAMs) acting on the human α7 nicotinic acetylcholine receptor (nAChR). Electrophysiological studies have focused on...
Drugs and Scaffold That Inhibit Cytochrome P450 27A1 In Vitro and In Vivo [0.03%]
体外和体内抑制细胞色素P450 27A1的药物和支架
Morrie Lam,Natalia Mast,Irina A Pikuleva
Morrie Lam
Cytochrome P450 27A1 (CYP27A1) is a ubiquitous enzyme that hydroxylates cholesterol and other sterols. Complete CYP27A1 deficiency owing to genetic mutations is detrimental to human health, whereas 50% of activity retention is not and does ...
Slowly Signaling G Protein-Biased CB2 Cannabinoid Receptor Agonist LY2828360 Suppresses Neuropathic Pain with Sustained Efficacy and Attenuates Morphine Tolerance and Dependence [0.03%]
偏向G蛋白信号的CB2受体激动剂LY2828360缓慢抑制神经病理性疼痛并具有持久疗效，并可减弱吗啡耐受性和依赖性
Xiaoyan Lin,Amey S Dhopeshwarkar,Megan Huibregtse et al.
Xiaoyan Lin et al.
The CB2 cannabinoid agonist LY2828360 lacked both toxicity and efficacy in a clinical trial for osteoarthritis. Whether LY2828360 suppresses neuropathic pain has not been reported, and its signaling profile is unknown. In vitro, LY2828360 w...
Propofol Is an Allosteric Agonist with Multiple Binding Sites on Concatemeric Ternary GABAA Receptors [0.03%]
异丙酚是串联型GABAA受体的变构激动剂并具有多个结合位点
Daniel J Shin,Allison L Germann,Alexander D Johnson et al.
Daniel J Shin et al.
GABAA receptors can be directly activated and potentiated by the intravenous anesthetic propofol. Previous photolabeling, modeling, and functional data have identified two binding domains through which propofol acts on the GABAA receptor. T...
Identification of an Oleanane-Type Triterpene Hedragonic Acid as a Novel Farnesoid X Receptor Ligand with Liver Protective Effects and Anti-inflammatory Activity [0.03%]
橄榄酸衍生成分为法尼酯X受体配体及保肝抗炎活性物质的鉴定研究
Yi Lu,Weili Zheng,Shengchen Lin et al.
Yi Lu et al.
Farnesoid X receptor (FXR) and G-protein-coupled bile acid receptor 1 (GPBAR1) are two important bile acid (BA) receptors. As non-BAs drug template for GPBAR1, none of the natural oleanane-type triterpenes have been reported as FXR ligands,...
GABA Type A Receptor Activation in the Allosteric Coagonist Model Framework: Relationship between EC50 and Basal Activity [0.03%]
变构激动剂模型框架中的GABAA受体激活：EC50与基础活性之间的关系
Gustav Akk,Daniel J Shin,Allison L Germann et al.
Gustav Akk et al.
The concerted transition model for multimeric proteins is a simple formulation for analyzing the behavior of transmitter-gated ion channels. We used the model to examine the relationship between the EC50 for activation of the GABA type A (G...
Molecular Imaging of GLUT1 and GLUT5 in Breast Cancer: A Multitracer Positron Emission Tomography Imaging Study in Mice [0.03%]
小鼠乳腺癌的分子影像：一种针对GLUT1和GLUT5的多示踪剂正电子发射断层扫描成像研究
Melinda Wuest,Ingrit Hamann,Vincent Bouvet et al.
Melinda Wuest et al.
Use of [18F]FDG-positron emission tomography (PET) in clinical breast cancer (BC) imaging is limited mainly by insufficient expression levels of facilitative glucose transporter (GLUT)1 in up to 50% of all patients. Fructose-specific facili...
Irreversible Activation and Stabilization of Soluble Guanylate Cyclase by the Protoporphyrin IX Mimetic Cinaciguat [0.03%]
市售血红素类似物西那西呱可激活并稳定可溶性鸟苷酸环化酶
Alexander Kollau,Marissa Opelt,Gerald Wölkart et al.
Alexander Kollau et al.
Belonging to the class of so-called soluble guanylate cyclase (sGC) activators, cinaciguat and BAY 60-2770 are interesting therapeutic tools for the treatment of various cardiovascular pathologies. The drugs are supposed to preferentially s...