Contributions of Protease-Activated Receptors PAR1 and PAR4 to Thrombin-Induced GPIIbIIIa Activation in Human Platelets [0.03%]
人血小板中蛋白酶活化受体PAR1和PAR4在凝血酶诱导的GPIIbIIIa激活中的作用研究
Matthew T Duvernay,Kayla J Temple,Jae G Maeng et al.
Matthew T Duvernay et al.
Human platelets display a unique dual receptor system for responding to its primary endogenous activator, α-thrombin. Because of the lack of efficacious antagonists, the field has relied on synthetic peptides and pepducins to describe prot...
Contribution of Organic Anion-Transporting Polypeptides 1A/1B to Doxorubicin Uptake and Clearance [0.03%]
有机阴离子转运多肽1A/1B在多柔比星摄取和清除中的作用
Hannah H Lee,Brenda F Leake,Richard B Kim et al.
Hannah H Lee et al.
The organic anion-transporting polypeptides represent an important family of drug uptake transporters that mediate the cellular uptake of a broad range of substrates including numerous drugs. Doxorubicin is a highly efficacious and well-est...
André S Pupo,J Adolfo García-Sáinz
André S Pupo
G protein-coupled receptors are sensors that interact with a large variety of elements, including photons, ions, and large proteins. Not surprisingly, these receptors participate in the numerous normal physiologic processes that we refer to...
Discovery and Characterization of Novel GPR39 Agonists Allosterically Modulated by Zinc [0.03%]
新型GPR39激动剂的发现与表征及其与锌的别构调节作用
Seiji Sato,Xi-Ping Huang,Wesley K Kroeze et al.
Seiji Sato et al.
In this study, we identified two previously described kinase inhibitors-3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(3-methyl-1H-pyrazol-5-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine (LY2784544) and 1H-benzimidazole-4-carboxylic acid...
State-Dependent Allosteric Inhibition of the Human SLC13A5 Citrate Transporter by Hydroxysuccinic Acids, PF-06649298 and PF-06761281 [0.03%]
羟基延胡索酸通过人类SLC13A5柠檬酸转运蛋白的状态依赖别构抑制作用治疗线粒体三羧酸循环缺陷症
Marie-Laure Rives,Morena Shaw,Bin Zhu et al.
Marie-Laure Rives et al.
In the liver, citrate is a key metabolic intermediate involved in the regulation of glycolysis and lipid synthesis and reduced expression of the hepatic citrate SLC13A5 transporter has been shown to improve metabolic outcomes in various ani...
The 2016 John J. Abel Award Lecture: Targeting the Mechanical Microenvironment in Cancer [0.03%]
2016约翰•阿贝尔奖学术讲座：针对癌症的机械微环境作用靶点
Hannah E Majeski,Jing Yang
Hannah E Majeski
Past decades of cancer research have mainly focused on the role of various extracellular and intracellular biochemical signals on cancer progression and metastasis. Recent studies suggest an important role of mechanical forces in regulating...
Extracellular Loop 2 of the Adenosine A1 Receptor Has a Key Role in Orthosteric Ligand Affinity and Agonist Efficacy [0.03%]
腺苷A1受体胞外环2结构域在正构配体亲和力及激动效率中的关键作用
Anh T N Nguyen,Jo-Anne Baltos,Trayder Thomas et al.
Anh T N Nguyen et al.
The adenosine A1 G protein-coupled receptor (A1AR) is an important therapeutic target implicated in a wide range of cardiovascular and neuronal disorders. Although it is well established that the A1AR orthosteric site is located within the ...
Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity [0.03%]
腺苷A1受体第二个胞外环对其别构调节剂结合、信号转导和协同性的作用
Anh T N Nguyen,Elizabeth A Vecchio,Trayder Thomas et al.
Anh T N Nguyen et al.
Allosteric modulation of adenosine A1 receptors (A1ARs) offers a novel therapeutic approach for the treatment of numerous central and peripheral disorders; however, despite decades of research, there is a relative paucity of structural info...
Molecular Basis for Inhibition of the Na+/Citrate Transporter NaCT (SLC13A5) by Dicarboxylate Inhibitors [0.03%]
二羧酸抑制剂作用于Na+/柠檬酸转运蛋白NaCT(SLC13A5)的分子机制研究
Ana M Pajor,Cesar A de Oliveira,Kun Song et al.
Ana M Pajor et al.
The Na+/citrate transporter, NaCT (SLC13A5), is a therapeutic target for metabolic diseases. Citrate is an important signaling molecule that regulates the activity of lipid- and glucose-metabolizing enzymes in cells. Previous studies identi...
Gβγ Pathways in Cell Polarity and Migration Linked to Oncogenic GPCR Signaling: Potential Relevance in Tumor Microenvironment [0.03%]
与致癌G蛋白偶联受体信号传导相关的细胞极性及迁移的Gβγ通路及其在肿瘤微环境中的潜在作用
José Vázquez-Prado,Ismael Bracho-Valdés,Rodolfo Daniel Cervantes-Villagrana et al.
José Vázquez-Prado et al.
Cancer cells and stroma cells in tumors secrete chemotactic agonists that exacerbate invasive behavior, promote tumor-induced angiogenesis, and recruit protumoral bone marrow-derived cells. In response to shallow gradients of chemotactic st...