Novel Mode of Antagonist Binding in NMDA Receptors Revealed by the Crystal Structure of the GluN1-GluN2A Ligand-Binding Domain Complexed to NVP-AAM077 [0.03%]
谷氨酸N-甲基-D-天冬氨酸（NMDA）型受体GluN1-GluN2A配体结合域与NVP-AAM077复合物的晶体结构
Annabel Romero-Hernandez,Hiro Furukawa
Annabel Romero-Hernandez
Competitive antagonists against N-methyl-D-aspartate (NMDA) receptors have played critical roles throughout the history of neuropharmacology and basic neuroscience. There are currently numerous NMDA receptor antagonists containing a variety...
Dexamethasone Downregulates Endothelin Receptors and Reduces Endothelin-Induced Production of Matrix Metalloproteinases in Cultured Rat Astrocytes [0.03%]
地塞米松下调内皮素受体并减少内皮素诱导的培养大鼠星形胶质细胞基质金属蛋白酶的产生
Yutaka Koyama,Ayano Ukita,Kana Abe et al.
Yutaka Koyama et al.
In brain disorders, astrocytes change phenotype to reactive astrocytes and are involved in the induction of neuroinflammation and brain edema. The administration of glucocorticoids (GCs), such as dexamethasone (Dex), reduces astrocytic acti...
Up-regulated Ectonucleotidases in Fas-Associated Death Domain Protein- and Receptor-Interacting Protein Kinase 1-Deficient Jurkat Leukemia Cells Counteract Extracellular ATP/AMP Accumulation via Pannexin-1 Channels during Chemotherapeutic Drug-Induced Apoptosis [0.03%]
Fas相关死亡域蛋白和受体相互作用蛋白激酶1缺陷Jurkat白血病细胞中上调的胞外核苷酸酶通过化疗药物诱导凋亡时的pannexin-1通道对抗细胞外ATP/AMP累积
Andrea M Boyd-Tressler,Graham S Lane,George R Dubyak
Andrea M Boyd-Tressler
Pannexin-1 (Panx1) channels mediate the efflux of ATP and AMP from cancer cells in response to induction of extrinsic apoptosis by death receptors or intrinsic apoptosis by chemotherapeutic agents. We previously described the accumulation o...
Molecular Basis of Metabolism-Mediated Conversion of PK11195 from an Antagonist to an Agonist of the Constitutive Androstane Receptor [0.03%]
PK11195代谢介导的固有安雄酮受体拮抗剂向激动剂转换的分子机制研究
Bryan Mackowiak,Linhao Li,Matthew A Welch et al.
Bryan Mackowiak et al.
The constitutive androstane receptor (CAR) plays an important role in xenobiotic metabolism, energy homeostasis, and cell proliferation. Antagonism of the CAR represents a key strategy for studying its function and may have potential clinic...
Yan Zhang,Hong-Kun Wu,Fengxiang Lv et al.
Yan Zhang et al.
MG53 (also known as tripartite motif, TRIM72) is a cardiac and skeletal muscle-specific TRIM-family protein that exhibits multiple biologic functions. First, MG53 participates in plasma membrane repair of the heart, skeletal muscle, and, ot...
Rapid Throughput Analysis of GABAA Receptor Subtype Modulators and Blockers Using DiSBAC1(3) Membrane Potential Red Dye [0.03%]
一种使用DiSBAC1(3)膜电位红染料快速分析GABAA受体亚型调节剂和阻断剂的方法
Atefeh Mousavi Nik,Brandon Pressly,Vikrant Singh et al.
Atefeh Mousavi Nik et al.
Fluorometric imaging plate reader membrane potential dye (FMP-Red-Dye) is a proprietary tool for basic discovery and high-throughput drug screening for G-protein-coupled receptors and ion channels. We optimized and validated this potentiome...
GABABR-Induced EGFR Transactivation Promotes Migration of Human Prostate Cancer Cells [0.03%]
GABABR诱导的EGFR转激活促进人前列腺癌细胞迁移
Shuai Xia,Cong He,Yini Zhu et al.
Shuai Xia et al.
G protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs) act in concert to regulate cell growth, proliferation, survival, and migration. Metabotropic GABAB receptor (GABABR) is the GPCR for the main inhibitory neurotransmitt...
Tumor Microenvironment Targeting and Responsive Peptide-Based Nanoformulations for Improved Tumor Therapy [0.03%]
基于肽的纳米递送系统在肿瘤治疗中的应用及针对肿瘤微环境的设计与响应
Hao Qin,Yanping Ding,Ayeesha Mujeeb et al.
Hao Qin et al.
The tumor microenvironment participates in all stages of tumor progression and has emerged as a promising therapeutic target for cancer therapy. Rapid progress in the field of molecular self-assembly using various biologic molecules has res...
A Glutamate-Substituted Mutant Mimics the Phosphorylated and Active Form of Guanylyl Cyclase-A [0.03%]
谷氨酸替代突变体模仿鸟苷酸环化酶-A磷酸化和激活形式
Neil M Otto,William G McDowell,Deborah M Dickey et al.
Neil M Otto et al.
Multisite phosphorylation is required for activation of guanylyl cyclase (GC)-A, also known as NPR-A or NPR1, by cardiac natriuretic peptides (NPs). Seven chemically identified sites (Ser-487, Ser-497, Thr-500, Ser-502, Ser-506, Ser-510, an...
Negative Regulation of Human Pregnane X Receptor by MicroRNA-18a-5p: Evidence for Suppression of MicroRNA-18a-5p Expression by Rifampin and Rilpivirine [0.03%]
人孕烷X受体的microRNA-18a-5p负性调节：利福平和Rilpivirine抑制MicroRNA-18a-5p表达的确证
Devinder Sharma,Abdullah A Turkistani,Wenjun Chang et al.
Devinder Sharma et al.
Small noncoding microRNAs act as post-transcriptional regulators of gene expression involved in diverse biologic functions. Pregnane X receptor (PXR, NR1I2), a member of the superfamily of nuclear receptors, is a transcription factor govern...