Receptor-mediated activation of heterotrimeric G-proteins: current structural insights [0.03%]
异三聚体G蛋白受体介导激活的结构洞察当前见解
Christopher A Johnston,David P Siderovski
Christopher A Johnston
G-protein-coupled receptors (GPCRs) serve as catalytic activators of heterotrimeric G-proteins (Galphabetagamma) by exchanging GTP for the bound GDP on the Galpha subunit. This guanine nucleotide exchange factor activity of GPCRs is the ini...
Antidiabetes and antiobesity effect of cryptotanshinone via activation of AMP-activated protein kinase [0.03%]
激活腺苷酸活化蛋白激酶的抗糖尿病和抗肥胖作用：隐丹参酮的作用
Eun Ju Kim,Seung-Nam Jung,Kun Ho Son et al.
Eun Ju Kim et al.
Metabolic disorders, including type 2 diabetes and obesity, represent major health risks in industrialized countries. AMP-activated protein kinase (AMPK) has become the focus of a great deal of attention as a novel therapeutic target for th...
Pioglitazone and rosiglitazone decrease prostaglandin E2 in non-small-cell lung cancer cells by up-regulating 15-hydroxyprostaglandin dehydrogenase [0.03%]
吡格列酮和罗格列酮通过上调15-羟基前列腺素脱氢酶减少非小细胞肺癌细胞中的前列腺素E2
Saswati Hazra,Raj K Batra,Hsin H Tai et al.
Saswati Hazra et al.
Lung cancer cells elaborate the immunosuppressive and antiapoptotic mediator prostaglandin E(2) (PGE(2)), a product of cyclooxygenase-2 (COX-2) enzyme activity. Because peroxisome proliferator-activated receptor (PPAR)gamma ligands, such as...
Trapping of a nonpeptide ligand by the extracellular domains of the gonadotropin-releasing hormone receptor results in insurmountable antagonism [0.03%]
非肽配体与促性腺激素释放激素受体胞外区结合致不可逆性拮抗作用
Trudy A Kohout,Qiu Xie,Shelby Reijmers et al.
Trudy A Kohout et al.
Drugs that exhibit insurmountable antagonism are proposed to provide improved clinical efficacy through extended receptor blockade. Long-term suppression of the gonadotropin-releasing hormone receptor (GnRHR) is an important therapeutic app...
Nigrostriatal damage preferentially decreases a subpopulation of alpha6beta2* nAChRs in mouse, monkey, and Parkinson's disease striatum [0.03%]
nigrostriatal损伤选择性地减少小鼠，猴和帕金森病纹状体中的一组α6β2*nAChRs亚群
Tanuja Bordia,Sharon R Grady,J Michael McIntosh et al.
Tanuja Bordia et al.
Parkinson's disease is a neurodegenerative movement disorder characterized by a loss of substantia nigra dopamine neurons, and corresponding declines in molecular components present on striatal dopaminergic nerve terminals. These include th...
Building a pharmacological lexicon: small molecule discovery in academia [0.03%]
构建药理学词典：学术界的small molecule发现
John S Lazo,Linda S Brady,Ray Dingledine
John S Lazo
Small molecules are powerful pharmacological tools to dissect biological events. There is now considerable interest in expanding efforts to identify and use small molecules targeting proteins encoded in the genomes of humans and pathogenic ...
Inhibition of transforming growth factor beta signaling reduces pancreatic adenocarcinoma growth and invasiveness [0.03%]
转化生长因子β信号转导的抑制可减少胰腺癌的生长和侵袭性
Nicholas J Gaspar,Lingyun Li,Ann M Kapoun et al.
Nicholas J Gaspar et al.
Transforming growth factor beta (TGFbeta) is a pleiotropic factor that regulates cell proliferation, angiogenesis, metastasis, and immune suppression. Dysregulation of the TGFbeta pathway in tumor cells often leads to resistance to the anti...
Hypoxia inhibits paclitaxel-induced apoptosis through adenosine-mediated phosphorylation of bad in glioblastoma cells [0.03%]
缺氧通过腺苷介导的坏蛋白磷酸化抑制胶质母细胞瘤细胞中的紫杉醇诱导的凋亡
Stefania Merighi,Annalisa Benini,Prisco Mirandola et al.
Stefania Merighi et al.
Solid tumors contain hypoxic cells that are resistant to radiotherapy and chemotherapy. The resistance in glioblastoma has been linked to the expression of antiapoptotic Bcl-2 family members. In this study, we found that in human glioblasto...
Glycogen synthase kinase 3 regulates N-methyl-D-aspartate receptor channel trafficking and function in cortical neurons [0.03%]
糖原合成酶激酶3调控皮层神经元中N-甲基-D-天冬氨酸受体通道的转运和功能
Paul Chen,Zhenglin Gu,Wenhua Liu et al.
Paul Chen et al.
Emerging evidence has suggested that glycogen synthase kinase 3 (GSK-3) is a key regulatory kinase involved in a plethora of processes in the nervous system, including neuronal development, mood stabilization, and neurodegeneration. However...
Evidence that curcumin suppresses the growth of malignant gliomas in vitro and in vivo through induction of autophagy: role of Akt and extracellular signal-regulated kinase signaling pathways [0.03%]
姜黄素通过诱导自噬抑制恶性胶质瘤体内外生长的证据：Akt和细胞外信号调节激酶信号通路的作用
Hiroshi Aoki,Yasunari Takada,Seiji Kondo et al.
Hiroshi Aoki et al.
Autophagy is a response of cancer cells to various anticancer therapies. It is designated as programmed cell death type II and characterized by the formation of autophagic vacuoles in the cytoplasm. The Akt/mammalian target of rapamycin (mT...