Assay Conditions Influence Affinities of Rat Organic Cation Transporter 1: Analysis of Mutagenesis in the Modeled Outward-Facing Cleft by Measuring Effects of Substrates and Inhibitors on Initial Uptake [0.03%]
测定条件影响大鼠有机阳离子转运体1的亲和力：通过测量底物和抑制剂对初始摄取的影响分析模型外侧裂隙中的诱变效应
Valentin Gorboulev,Saba Rehman,Christoph M Albert et al.
Valentin Gorboulev et al.
The effects of mutations in the modeled outward-open cleft of rat organic cation transporter 1 (rOCT1) on affinities of substrates and inhibitors were investigated. Human embryonic kidney 293 cells were stably transfected with rOCT1 or rOCT...
Concentrative Transport of Antifolates Mediated by the Proton-Coupled Folate Transporter (SLC46A1); Augmentation by a HEPES Buffer [0.03%]
HEPES缓冲液介导的叶酸转运蛋白（SLC46A1）依赖的抗叶酸集中传输；HEPES缓冲液增强效应
Rongbao Zhao,Mitra Najmi,Srinivas Aluri et al.
Rongbao Zhao et al.
The proton-coupled folate transporter (PCFT) is ubiquitously expressed in solid tumors to which it delivers antifolates, particularly pemetrexed, into cancer cells. Studies of PCFT-mediated transport, to date, have focused exclusively on th...
Biased Agonism in Drug Discovery-Is It Too Soon to Choose a Path? [0.03%]
偏向性激动剂在药物研发中的作用-现在就确定其地位是否为时过早？
Martin C Michel,Steven J Charlton
Martin C Michel
A single receptor can activate multiple signaling pathways that have distinct or even opposite effects on cell function. Biased agonists stabilize receptor conformations preferentially stimulating one of these pathways, and therefore allow ...
G Protein-Coupled Receptors as Targets for Approved Drugs: How Many Targets and How Many Drugs? [0.03%]
已批准药物的作用靶点：G蛋白偶联受体-G蛋白偶联受体类药物作用靶点知多少？
Krishna Sriram,Paul A Insel
Krishna Sriram
Estimates vary regarding the number of G protein-coupled receptors (GPCRs), the largest family of membrane receptors that are targeted by approved drugs, and the number of such drugs that target GPCRs. We review current knowledge regarding ...
A Computational-Based Approach to Identify Estrogen Receptor α/ β Heterodimer Selective Ligands [0.03%]
一种基于计算的鉴定雌激素受体α/β异二聚选择性配体的方法
Carlos G Coriano,Fabao Liu,Chelsie K Sievers et al.
Carlos G Coriano et al.
The biologic effects of estrogens are transduced by two estrogen receptors (ERs), ERα and ERβ, which function in dimer forms. The ERα/α homodimer promotes and the ERβ/β inhibits estrogen-dependent growth of mammary epithelial cells; t...
(Z)-2-(3,4-Dichlorophenyl)-3-(1 H-Pyrrol-2-yl)Acrylonitrile Exhibits Selective Antitumor Activity in Breast Cancer Cell Lines via the Aryl Hydrocarbon Receptor Pathway [0.03%]
(Z)-2-(3,4-二氯苯基)-3-(1H-吡咯-2-基)丙烯腈通过芳烃受体通路在乳腺癌细胞系中表现出选择性抗肿瘤活性
Jayne Gilbert,Geoffry N De Iuliis,Mark Tarleton et al.
Jayne Gilbert et al.
We have previously reported the synthesis and breast cancer selectivity of (Z)-2-(3,4-dichlorophenyl)-3-(1H-pyrrol-2-yl)acrylonitrile (ANI-7) in cancer cell lines. To further evaluate the selectivity of ANI-7, we have expanded upon the init...
The Bioactive Protein-Ligand Conformation of GluN2C-Selective Positive Allosteric Modulators Bound to the NMDA Receptor [0.03%]
与谷氨酸NMDA受体结合的GluN2C亚型选择性正向别构调节剂的活性蛋白-配体构象
Thomas M Kaiser,Steven A Kell,Hirofumi Kusumoto et al.
Thomas M Kaiser et al.
N-methyl-d-aspartate (NMDA) receptors are ligand-gated, cation-selective channels that mediate a slow component of excitatory synaptic transmission. Subunit-selective positive allosteric modulators of NMDA receptor function have therapeutic...
Moving Synergistically Acting Drug Combinations to the Clinic by Comparing Sequential versus Simultaneous Drug Administrations [0.03%]
通过比较序贯与联合给药推动协同作用的药物组合进入临床
Saketh S Dinavahi,Mohammad A Noory,Raghavendra Gowda et al.
Saketh S Dinavahi et al.
Drug combinations acting synergistically to kill cancer cells have become increasingly important in melanoma as an approach to manage the recurrent resistant disease. Protein kinase B (AKT) is a major target in this disease but its inhibito...
Comparative Study
Molecular pharmacology. 2018 Mar;93(3):190-196. DOI:10.1124/mol.117.110759 2018
Peilan Zhou,Jiebing Jiang,Hui Yan et al.
Peilan Zhou et al.
The μ-opioid receptor (MOR) is a Gi/o protein-coupled receptor that mediates analgesic, euphoric, and reward effects. Using a bacterial two-hybrid screen, we reported that the carboxyl tail of the rat MOR associates with A20-binding inhibi...
Pharmacologic Evidence for a Putative Conserved Allosteric Site on Opioid Receptors [0.03%]
阿片受体上一个假设的保守别构位点的药理学证据
Kathryn E Livingston,M Alexander Stanczyk,Neil T Burford et al.
Kathryn E Livingston et al.
Allosteric modulators of G protein-coupled receptors, including opioid receptors, have been proposed as possible therapeutic agents with enhanced selectivity. BMS-986122 is a positive allosteric modulator (PAM) of the μ-opioid receptor (µ...