John Janetzko,Nicole A Perry-Hauser
John Janetzko
Effects of two structurally diverse positive allosteric modulators on signaling bias at the μ-opioid receptor [0.03%]
两种结构不同的正变构调节剂对μ-阿片受体信号偏差的影响
Mengchu Li,Kelsey E Kochan,M Alexander Stanczyk et al.
Mengchu Li et al.
The μ-opioid receptor (MOR) is responsible for the analgesic actions of opioid drugs as well as their unwanted actions, including respiratory depression and addiction liability. Following agonist occupancy, MOR can signal via G-protein and...
Distinctive patterns of G protein coupling induced by the structurally similar 5-HT2A receptor ligands ketanserin and altanserin in human prefrontal cortex [0.03%]
结构类似的5-ht2a受体配体ketanserin和altanserin诱导的人类前额皮质g蛋白偶联的独特模式
Patricia Miranda-Azpiazu,Carolina Muguruza,Tomasz Maciej Stepniewski et al.
Patricia Miranda-Azpiazu et al.
Antipsychotic activity of certain 5-HT2A receptor (5-HT2AR) antagonists has been attributed to inverse agonism. 5-HT2AR hallucinogenic agonists exhibit biased agonism toward Gi/o proteins. Ketanserin and altanserin are 2 structurally simila...
Both calcium-sensing receptor intracellular C-terminal domains support homodimer signaling [0.03%]
钙感受器受体的两个胞内C端结构域均可支持同源二聚体信号转导
Lenah S Binmahfouz,Mahvash A Goolam,Eleanor Barker et al.
Lenah S Binmahfouz et al.
Extracellular calcium-sensing receptors (CaSRs) are required for whole-body calcium homeostasis and operate as homodimers, shown structurally to bind only one heterotrimeric G protein at a time. Whether the intracellular domain (ICD) of the...
Mice carrying the human dopamine D2 receptor pathogenic mutation p.Met374Arg exhibit hyperactivity and aberrant D2 receptor function [0.03%]
携带人类多巴胺D2受体致病突变p.Met374Arg的小鼠表现出过度活跃和D2受体功能异常
Dayana Rodriguez-Contreras,Joseph J Lebowitz,Cheryl Reed et al.
Dayana Rodriguez-Contreras et al.
Two human dopamine D2 receptor mutations cause dominant hyperkinetic movement disorders. The phenotype of carriers of the DRD2 variant c.634A>T, p.Ile212Phe (D2-I212F) is less severe than that of carriers of the variant c.1121 T>G, p.Met374...
LZ-106 inhibits anchorage-independent growth of non-small cell lung cancer cells by a positive feedback between reactive oxygen species induction and autophagy flux blockage [0.03%]
LZ-106通过正反馈（诱导活性氧和阻断自噬流）抑制非小细胞肺癌的贴壁独立生长
Ruixuan Wang,Jingyuan Feng,Fei Meng et al.
Ruixuan Wang et al.
Metastasis remains a formidable challenge in the treatment of non-small cell lung cancer (NSCLC), necessitating novel therapeutic strategies targeting anchorage-independent growth (AIG). This study investigates the inhibitory effects of LZ-...
Cholesterol residence time drives regulation of the G protein-coupled cholecystokinin receptor [0.03%]
胆固醇驻留时间驱动调控胆囊收缩素G蛋白偶联受体
Chirine Toufaily,Yuanyuan Ma,Emmanuel D Barbosa et al.
Chirine Toufaily et al.
Membrane cholesterol modulates the ability of cholecystokinin to act at the type 1 cholecystokinin receptor (CCK1R), with elevated levels of this lipid that can be present in obesity, disrupting stimulus-activity coupling. This occurs via d...
Cholesterol residence time drives regulation of the G protein-coupled cholecystokinin receptor [0.03%]
胆固醇停留时间决定了G蛋白偶联胆囊收缩素受体的调节作用
Chirine Toufaily,Yuanyuan Ma,Emmanuel D Barbosa et al.
Chirine Toufaily et al.
Membrane cholesterol modulates the ability of cholecystokinin to act at the type 1 cholecystokinin receptor (CCK1R), with elevated levels of this lipid that can be present in obesity, disrupting stimulus-activity coupling. This occurs via d...
Voltage sensor interaction site for a selective small molecule Nav1.1 sodium channel potentiator that enhances firing of fast-spiking interneurons [0.03%]
一种选择性的电压门控钠通道Nav1.1的小分子激动剂的作用位点，可增强快振细胞内神经元的放电能力
Allison Gallucci,Franck Potet,Sonia Santos et al.
Allison Gallucci et al.
Nav1.1 voltage-gated sodium (Nav) channels encoded by the SCN1A gene are critical to high frequency action potential generation in inhibitory interneurons and so play a crucial role in maintaining the excitatory-inhibitory balance in the br...
Differential RELA and GR recruitment to the BIRC3/BIRC2 locus: Molecular insight as to combinatorial regulation by proinflammatory cytokines and glucocorticoid [0.03%]
BIRC3/BIRC2位点的RELA和GR的不同募集：揭示促炎症细胞因子与糖皮质激素联合调控的分子机制
Andrew J Thorne,Alex Gao,Amandah Necker-Brown et al.
Andrew J Thorne et al.
In pulmonary epithelial cells, baculoviral inhibitor of apoptosis repeat-containing (BIRC) gene, BIRC3, and to a lesser extent, BIRC2, mRNAs were upregulated by interleukin (IL)-1β and tumor necrosis factor-α. Glucocorticoids also induced...