Structure-activity relationship of 1,4-dihydropyridines as potentiators of the cystic fibrosis transmembrane conductance regulator chloride channel [0.03%]
1,4-二氢吡啶类化合物作为增强囊性纤维化跨膜传导调节因子氯通道活性药物的构效关系研究
Nicoletta Pedemonte,Davide Boido,Oscar Moran et al.
Nicoletta Pedemonte et al.
Mutations occurring in the CFTR gene, encoding for the cystic fibrosis transmembrane conductance regulator chloride channel, cause cystic fibrosis (CF). Mutations belonging to class II, such as DeltaPhe508, give rise to a protein with both ...
Serotonin inhibits neuronal excitability by activating two-pore domain k+ channels in the entorhinal cortex [0.03%]
血清素通过激活内侧嗅周皮质中两孔钾通道抑制神经元兴奋性
Pan-Yue Deng,Shree Kanta S Poudel,Lalida Rojanathammanee et al.
Pan-Yue Deng et al.
The entorhinal cortex (EC) is regarded as the gateway to the hippocampus; the superficial layers (layers I-III) of the EC convey the cortical input projections to the hippocampus, whereas deep layers of the EC relay hippocampal output proje...
Activation of the angiotensin II type 1 receptor leads to movement of the sixth transmembrane domain: analysis by the substituted cysteine accessibility method [0.03%]
血管紧张素Ⅱ受体激活可引起第六跨膜结构域重排的构象改变：替代半胱氨酸通道方法分析
Stéphane S Martin,Brian J Holleran,Emanuel Escher et al.
Stéphane S Martin et al.
The role of transmembrane domain six (TMD6) of the angiotensin II type 1 receptor, which is predicted to undergo conformational changes after agonist binding, was investigated using the substituted-cysteine accessibility method. Each residu...
Adrenomedullin stimulates nitric oxide production from primary rat hypothalamic neurons: roles of calcium and phosphatases [0.03%]
肾上腺髓质素刺激初级大鼠下丘脑神经元一氧化氮的产生：钙和磷酸酶的作用
Yong Xu,Teresa L Krukoff
Yong Xu
Adrenomedullin (ADM) in the brain plays important roles in the maintenance of homeostasis. Although in vivo evidence has suggested that nitric oxide (NO) mediates ADM's effects in the brain, mechanisms for ADM stimulation of NO production i...
Alexander Kollau,Matteo Beretta,Antonius C F Gorren et al.
Alexander Kollau et al.
Bioactivation of nitroglycerin (GTN) into an activator of soluble guanylate cyclase (sGC) is essential for the vasorelaxant effect of the drug. Besides several enzymes that catalyze GTN bioactivation, the reaction with cysteine is the sole ...
Differential intracellular signaling through PAC1 isoforms as a result of alternative splicing in the first extracellular domain and the third intracellular loop [0.03%]
受体异构体的可变胞内信号转导：由于第一个胞外结构域和第三个胞内环选择性剪接导致的PAC1受体异构体间的竞争关系研究
Mina Ushiyama,Ryuji Ikeda,Hideki Sugawara et al.
Mina Ushiyama et al.
Pituitary adenylate cyclase-activating polypeptide (PACAP), a pleiotropic neuropeptide, performs a variety of physiological functions. The PACAP-specific receptor PAC1 has several variants that result mainly from alternative splicing in the...
Chronic intermittent ethanol treatment selectively alters N-methyl-D-aspartate receptor subunit surface expression in cultured cortical neurons [0.03%]
慢性间歇性乙醇处理选择性地改变培养皮层神经元中N-甲基-D天冬氨酸受体亚单位的表面表达
Mei Qiang,Ashley D Denny,Maharaj K Ticku
Mei Qiang
A chronic intermittent ethanol (CIE) exposure regimen consists of repeated episodes of ethanol intoxication and withdrawal. CIE treatment has been reported to result in a significant enhancement of N-methyl-D-aspartate (NMDA) receptor-media...
Regulation of cytochrome P450 2E1 under hypertonic environment through TonEBP in human hepatocytes [0.03%]
人肝细胞中TonEBP在高渗环境下对CYP2E1的调节作用
Takashi Ito,Koko Asakura,Katsuhiko Tougou et al.
Takashi Ito et al.
Whereas the liver as well as the other organs are continually exposed to the change of osmotic status, it has never been investigated whether activities and gene expressions of drug-metabolizing enzymes, including cytochromes P450, are depe...
Small-molecule vasopressin-2 receptor antagonist identified by a g-protein coupled receptor "pathway" screen [0.03%]
一种通过G蛋白偶联受体通路筛选得到的小分子血管加压素2型受体拮抗剂
Buranee Yangthara,Aaron Mills,Varanuj Chatsudthipong et al.
Buranee Yangthara et al.
G-protein-coupled receptors (GPCRs) such as the vasopressin-2 receptor (V(2)R) are an important class of drug targets. We developed an efficient screen for GPCR-induced cAMP elevation using as read-out cAMP activation of cystic fibrosis tra...
Vasoactive intestinal peptide transactivates the androgen receptor through a protein kinase A-dependent extracellular signal-regulated kinase pathway in prostate cancer LNCaP cells [0.03%]
血管活性肠肽通过PKA依赖的ERK信号途径转激活前列腺癌LNCaP细胞中的雄激素受体
Yan Xie,Dennis W Wolff,Ming-Fong Lin et al.
Yan Xie et al.
Acquisition of androgen independence by prostate cancer is the key problem of prostate cancer progression. Vasoactive intestinal peptide (VIP), a neuropeptide, may act as a survival factor for prostate cancer cells under androgen deprivatio...