Amiodarone irrecoverably impairs the function of human ether-a-go-go-related gene potassium channels [0.03%]
胺碘酮不可逆地损害人ether-a-go-go相关基因钾通道的功能
Illia Gelman,Wentao Li,Jun Guo et al.
Illia Gelman et al.
The class III antiarrhythmic drug amiodarone (AMIO) inhibits the rapidly activating delayed rectifier K+ current that is conducted by the human ether-a-go-go-related gene (hERG) encoded channel. Like other class III antiarrhythmic drugs, AM...
Identification of small molecule ligands for GPR83 that modulate morphine antinociception and reward [0.03%]
用于GPR83的小分子配体的鉴定可调节吗啡的抗痛觉和犒赏效应
Ivone Gomes,Seshat M Mack,Roberto Sanchez et al.
Ivone Gomes et al.
The opioid crisis showcases a need for novel therapeutic avenues to treat drug abuse. GPR83, a recently deorphanized G protein-coupled receptor shown to blunt morphine reward learning and regulate pain, is activated by the neuropeptide PEN ...
Vsevolod V Gurevich
Vsevolod V Gurevich
Activation of most G protein-coupled receptors (GPCRs) initiates several branches of signaling. The consequences of some of these can be therapeutically beneficial, whereas others may cause unwanted side effects. Therefore, search for ligan...
Introduction of a single carboxylic acid converts the cyclic oligomeric depsipeptide ent-verticilide from a ryanodine receptor 2 (RyR2) inhibitor to RyR2 activator [0.03%]
一种羧酸的引入可将环状寡聚叠肽ent-verticilide从ryanodine受体2(RyR2)抑制剂转变为激动剂
Tri Q Do,Daniel J Blackwell,Abigail N Smith et al.
Tri Q Do et al.
Cyclic oligomeric depsipeptides represent a distinct structural class of naturally occurring compounds known for their wide-ranging biological activities. We previously reported that the unnatural form of verticilide (ent-verticilide) inhib...
Inhibition of constitutive activity of the atypical chemokine receptor 3 by the small-molecule inverse agonist VUF16840 [0.03%]
小分子反激动剂VUF16840抑制非典型趋化因子受体3的组成型活性
Reggie Bosma,Desislava Nesheva,Merel Rijnsburger et al.
Reggie Bosma et al.
The atypical chemokine receptor 3 (ACKR3) has emerged as a promising drug target for the treatment of cancer, cardiovascular, and autoimmune diseases. In this study, we present the pharmacological characterization of VUF16840, the first sma...
Predictive modeling and functional characterization of the ceRNA regulatory network in cisplatin resistance of non-small cell lung cancer [0.03%]
顺铂耐药的非小细胞肺癌的竞争性内分泌RNA调控网络的预测建模及功能表征
Hongyuan Li,Rui Zhang,Wenjun Tao et al.
Hongyuan Li et al.
Non-small cell lung cancer remains the leading cause of cancer-related mortality worldwide. Cisplatin-based chemotherapy is a primary treatment strategy for non-small cell lung cancer, but acquired drug resistance limits its therapeutic eff...
Predicting compounds that interact with the 2 known agonist-induced conformations of the human β1-adrenoceptor [0.03%]
预测与人类β1肾上腺素受体已知激动剂诱导构象相互作用的化合物
Jillian G Baker,Victor Jun Yu Lim,Richard G W Proudman et al.
Jillian G Baker et al.
The β1-adrenoceptor exists in at least 2 agonist-stabilized conformational ensembles: a "catecholamine" ensemble induced via the intrahelical binding site through which catecholamines and most agonists act and a "secondary" ensemble of con...
Transient receptor potential vanilloid 3 activation accelerates keratinocyte migration in vitro but not dermal wound healing in vivo [0.03%]
瞬时受体电位香草酸受体3活化加速角质形成细胞的迁移但不能促进真皮伤口愈合
Carolin Zosel,Anne-Kathrin Krause,Anne Müglitz et al.
Carolin Zosel et al.
The non-selective Ca2+ permeable transient receptor potential vanilloid 3 (TRPV3) ion channel is highly expressed in mouse keratinocytes, where its activation causes an accelerated cell migration and proliferation via an epidermal growth fa...
Electrophysiological characterization of the state-dependent inhibition of Kv7.1 and IKs by UCL2077 [0.03%]
UCL2077对Kv7.1和IKs的选择性依赖型抑制作用的电生理学表征
Daniel Sastre,Efthimios Kyriakis,Julia Schauer et al.
Daniel Sastre et al.
In cardiomyocytes, Kv7.1 associates with the regulatory subunit KCNE1 to generate the delayed rectifier potassium current IKs, which plays a crucial role in cardiac repolarization at elevated heart rates. Gain-of-function mutations in eithe...
Retraction notice to "17β-Estradiol, Genistein, and 4-Hydroxytamoxifen Induce the Proliferation of Thyroid Cancer Cells through the G Protein-Coupled Receptor GPR30" [Mol Pharmacol 70 (2006) 1414-1423] [0.03%]
撤销"Molecular Pharmacology"上题为“17β-雌二醇、大豆异黄酮和4-羟基他莫昔芬通过G蛋白偶联受体GPR30诱导甲状腺癌细胞增殖”[Mol Pharmacol 70 (2006) 1414-1423]的论文
Adele Vivacqua,Daniela Bonofiglio,Lidia Albanito et al.
Adele Vivacqua et al.