G protein-coupled receptor kinase 3 couples atypical chemokine receptor 4 independent of G proteins [0.03%]
不依赖G蛋白的G蛋白偶联受体激酶3与非典型趋化因子受体4相耦合
Thomas D Lamme,Isabel B Sánchez Arroyo,Martine J Smit et al.
Thomas D Lamme et al.
Atypical chemokine receptors (ACKRs) indirectly mediate cell migration through chemokine scavenging, which generally requires phosphorylation by G protein-coupled receptor kinases (GRKs) to efficiently control chemokine levels. Despite not ...
Structural and molecular determinants of glutamate transporter allosteric modulators [0.03%]
谷氨酸转运蛋白别构调节剂的结构和分子决定因素
Katelyn L Reeb,Satyaki Saha,Xiaowei Bogetti et al.
Katelyn L Reeb et al.
Excitatory amino acid transporters (EAATs) are critical regulators of synaptic glutamate levels in the central nervous system. Dysregulated central nervous system glutamatergic homeostasis is implicated in many neurological diseases, highli...
Role of GPR55 in glutamatergic and dopaminergic signaling: A review of preclinical evidence in neuropsychiatric disorders [0.03%]
GPR55在神经精神疾病中对谷氨酸能和多巴胺能信号传导的作用：临床前证据综述
Sanjay N Awathale,Kartik T Nakhate,Noor Ali et al.
Sanjay N Awathale et al.
G protein-coupled receptor 55 (GPR55) has gained increasing attention for its involvement in various neuropsychiatric disorders. Emerging evidence highlights the critical role of this receptor in modulating brain functions through complex i...
Identification of potent and selective small molecule TALK-1 inhibitors that promote β-cell function [0.03%]
一种能够促进β细胞功能的TALK-1强效小分子抑制剂的鉴定
Arya Y Nakhe,Jordyn R Dobson,Prasanna K Dadi et al.
Arya Y Nakhe et al.
The two-pore domain K+ (K2P) channel TALK-1 is a key regulator of β-cell electrical excitability, Ca2+ handling, and glucose-stimulated insulin secretion. KCNK16, the gene encoding TALK-1, is the most abundant β-cell K+ channel transcript...
Kristan H Cleveland,John D Scott
Kristan H Cleveland
Endocrine signaling relies heavily on the second messenger cAMP to influence different functional outcomes including hormone secretion, steroidogenesis, ion channel regulation, and cell growth. Selectivity of cAMP action is often achieved t...
The CaMKII D135N mutation blocks kinase activity and reduces GluN2B binding [0.03%]
钙调神经磷酸酶II(D135N)突变阻止了激酶活性并减少了GluN2B的结合
Matthew E Larsen,C Madison Barker,Raul Satoshi Vargas et al.
Matthew E Larsen et al.
Three recent studies claimed that induction of long-term potentiation of synaptic strength requires structural rather than enzymatic functions of the Ca2+/calmodulin-dependent protein kinase II (CaMKII). One study used the CaMKII D135N muta...
Maraviroc alleviates neuropathic pain symptoms in a mouse model of spared nerve injury [0.03%]
马瓦立克鼠神经痛模型中马瓦利克减轻神经病理性疼痛症状
Wei Zhao,Cigdem Sevim Bayrak,Fiona Chen et al.
Wei Zhao et al.
Chronic pain represents a major health problem in the health care system. According to the CDC data brief in 2020, 20.4% of adults have chronic pain. There has been no promising therapy for chronic pain. Currently available treatments inclu...
Identification and characterization of selective inhibitors of Nav1.9 voltage dependent sodium channels [0.03%]
钠离子通道Nav1.9特异性抑制剂的鉴定和表征
Franck Potet,Sonia Santos,Allison Gallucci et al.
Franck Potet et al.
Voltage-gated sodium channels play fundamental roles in physiological and pathophysiological electrical excitability of the nervous and muscular systems. This involves several sodium channel subtypes, including Nav1.9, which has been geneti...
Mechanisms for enhancement of μ-opioid receptor-mediated antinociception in the central nervous system through gallein-dependent modulation of downstream G protein βγ subunit signaling [0.03%]
通过gallein依赖的下游G蛋白βγ亚基信号调节增强中枢神经系统中μ-阿片受体介导的抗痛觉机制
Jacob A Ormes,Alan V Smrcka,Emily M Jutkiewicz
Jacob A Ormes
The clinical utility of μ-opioid receptor (MOR) agonists is limited by side effects and tolerance. G protein βγ subunits (Gβγ) are critical mediators of MOR signaling that not only drive anticonception but also regulate phospholipase C...
Trimethylamine N-oxide induces macrophage M1 polarization via the Piezo1/Yes-associated protein pathway [0.03%]
通过Piezo1/YAP信号通路诱导巨噬细胞M1极化的三甲胺N氧化物研究
Haiyan Xiang,Congcong Li,Yanhua Tang et al.
Haiyan Xiang et al.
Trimethylamine N-oxide (TMAO), a gut microbiota-derived metabolite, has been implicated in cardiometabolic inflammation; however, the intracellular signaling mechanisms linking TMAO to macrophage polarization remain incompletely defined. Th...