Pore Polarity and Charge Determine Differential Block of Kir1.1 and Kir7.1 Potassium Channels by Small-Molecule Inhibitor VU590 [0.03%]
孔道极性和电荷决定了小分子抑制剂VU590对钾通道Kir1.1和Kir7.1的不同阻断作用
Sujay V Kharade,Jonathan H Sheehan,Eric E Figueroa et al.
Sujay V Kharade et al.
VU590 was the first publicly disclosed, submicromolar-affinity (IC50 = 0.2 μM), small-molecule inhibitor of the inward rectifier potassium (Kir) channel and diuretic target, Kir1.1. VU590 also inhibits Kir7.1 (IC50 ∼ 8 μM), and has been ...
TCL1A Single-Nucleotide Polymorphisms and Estrogen-Mediated Toll-Like Receptor-MYD88-Dependent Nuclear Factor- κ B Activation: Single-Nucleotide Polymorphism- and Selective Estrogen Receptor Modulator-Dependent Modification of Inflammation and Immune Response [0.03%]
TCL1A单核苷酸多态性与雌激素介导的TLR-MYD88依赖型NF- κ B活化：单核苷酸多态性和选择性雌激素受体调节剂对炎症和免疫反应的影响
Ming-Fen Ho,James N Ingle,Tim Bongartz et al.
Ming-Fen Ho et al.
In a previous genome-wide association study (GWAS) for musculoskeletal adverse events during aromatase inhibitor therapy for breast cancer, we reported that single nucleotide polymorphisms (SNPs) near the TCL1A gene were associated with thi...
Identification of AICP as a GluN2C-Selective N-Methyl-d-Aspartate Receptor Superagonist at the GluN1 Glycine Site [0.03%]
识别AICP为选择性作用于谷氨酸N-甲基-D天冬氨酸受体GluN1甘氨酸位点的GluN2C超激动剂
Maja Jessen,Kristen Frederiksen,Feng Yi et al.
Maja Jessen et al.
N-methyl-d-aspartate (NMDA)-type ionotropic glutamate receptors mediate excitatory neurotransmission in the central nervous system and are critically involved in brain function. NMDA receptors are also implicated in psychiatric and neurolog...
C-X-C Motif Chemokine Receptor 3 Splice Variants Differentially Activate Beta-Arrestins to Regulate Downstream Signaling Pathways [0.03%]
C-X-C基序趋化因子受体3拼接变体通过差异激活β-arrestin来调节下游信号通路
Jeffrey S Smith,Priya Alagesan,Nimit K Desai et al.
Jeffrey S Smith et al.
Biased agonism, the ability of different ligands for the same receptor to selectively activate some signaling pathways while blocking others, is now an established paradigm for G protein-coupled receptor signaling. One group of receptors in...
Statins Attenuate Activation of the NLRP3 Inflammasome by Oxidized LDL or TNF α in Vascular Endothelial Cells through a PXR-Dependent Mechanism [0.03%]
PXR依赖机制下调OX-LDL或TNFα诱导的内皮细胞中NLRP3炎性小体激活及通路基因表达的作用研究
Shaolan Wang,Xinya Xie,Ting Lei et al.
Shaolan Wang et al.
Excessive activation of the NLRP3 inflammasome is implicated in cardiovascular diseases. Statins exert an anti-inflammatory effect independent of their cholesterol-lowering effect. This study investigated the potential role of statins in th...
Alterations of Histone Modifications Contribute to Pregnane X Receptor-Mediated Induction of CYP3A4 by Rifampicin [0.03%]
环蛋白X受体介导的rifampicin诱导CYP3A4表達组蛋白修饰的变化
Liang Yan,Yiting Wang,Jingyang Liu et al.
Liang Yan et al.
CYP3A4 is one of the major drug-metabolizing enzymes in human and is responsible for the metabolism of 60% of clinically used drugs. Many drugs are able to induce the expression of CYP3A4, which usually causes drug-drug interactions and adv...
Direct Binding of the Corrector VX-809 to Human CFTR NBD1: Evidence of an Allosteric Coupling between the Binding Site and the NBD1:CL4 Interface [0.03%]
正确结合剂VX-809与人类CFTR NBD1直接结合：在结合位点和NBD1:CL4界面之间存在别构耦合的证据
Rhea P Hudson,Jennifer E Dawson,P Andrew Chong et al.
Rhea P Hudson et al.
Understanding the mechanism of action of modulator compounds for the cystic fibrosis transmembrane conductance regulator (CFTR) is key for the optimization of therapeutics as well as obtaining insights into the molecular mechanisms of CFTR ...
α 2 Subunit-Containing GABAA Receptor Subtypes Are Upregulated and Contribute to Alcohol-Induced Functional Plasticity in the Rat Hippocampus [0.03%]
含有α2亚单位的GABA受体在酒精诱导的大鼠海马神经可塑性中的作用
A Kerstin Lindemeyer,Yi Shen,Ferin Yazdani et al.
A Kerstin Lindemeyer et al.
Alcohol (EtOH) intoxication causes changes in the rodent brain γ-aminobutyric acid receptor (GABAAR) subunit composition and function, playing a crucial role in EtOH withdrawal symptoms and dependence. Building evidence indicates that with...
β-Arrestin-Mediated Regulation of the Human Ether-a-go-go-Related Gene Potassium Channel [0.03%]
β肾上皮素调节人类 Ether-à-go-go 相关基因钾通道功能
Matthew G Sangoi,Shawn M Lamothe,Jun Guo et al.
Matthew G Sangoi et al.
The rapidly activating delayed rectifier K+ channel (IKr) is encoded by the human ether-a-go-go-related gene (hERG), which is important for the repolarization of the cardiac action potential. Mutations in hERG or drugs can impair the functi...