erg1 potassium channel
Summary: One of three members of the ether-a-go-go (EAG) POTASSIUM CHANNELS gene family comprising ether-a-go-go (eag), eag-like (elk) and eag-related (erg) subfamilies. Ether-a-go-go-related gene 1 (ERG1) also known as KCNH2, encodes the pore-forming subunit of a rapidly activating-delayed rectifier potassium channel that plays an essential role in the final repolarization of ventricular action potential. Loss-of-function mutations in human hERG1 is associated with life-threatening ARRHYTHMIA.
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- Iqbal S, Lemmens Gruber R. Voltage gated ion channels blockade is the underlying mechanism of BIMU8 induced cardiotoxicity. Toxicol Lett. 2017;277:64-68 pubmed publisher..87mV in fast inactivation of NaV1.5 channel. These experimental findings indicate that BIMU8 is a potent blocker of hERG, NaV1.5 and CaV1.2 cardiac ion channels thus revealing its proarrhythmic potential. ..
- Dong S, VanGelder K, Shi Z, Yu Y, Wu Z, Ferguson R, et al. Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores. Bioorg Med Chem Lett. 2017;27:2559-2566 pubmed publisher..In vivo evaluation of 32 demonstrated blood pressure lowering effects in the spontaneously hypertensive rat model. ..
- Bartolozzi A, Abeywardane A, Bosanac T, Broadwater J, Chen Z, Hutzler J, et al. Discovery and optimization of oxadiazole-based FLAP inhibitors. Bioorg Med Chem Lett. 2017;27:4652-4659 pubmed publisher..Several compounds with favorable in vitro and in vivo properties were identified that were suitable for advanced profiling. ..
- Wang W, MacKinnon R. Cryo-EM Structure of the Open Human Ether-à-go-go-Related K+ Channel hERG. Cell. 2017;169:422-430.e10 pubmed publisher..A subtle structural feature of the hERG selectivity filter might correlate with its fast inactivation rate, which is key to hERG's role in cardiac action potential repolarization. ..
- Salvino J, Srikanth Y, Lou R, Oyer H, Chen N, Kim F. Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer. Bioorg Med Chem Lett. 2017;27:2216-2220 pubmed publisher..Herein we report on a new series of Sigma1 compounds for lead optimization derived from a hybrid pharmacophore approach. ..
- Hyltén Cavallius L, Iepsen E, Wewer Albrechtsen N, Svendstrup M, Lubberding A, Hartmann B, et al. Patients With Long-QT Syndrome Caused by Impaired hERG-Encoded Kv11.1 Potassium Channel Have Exaggerated Endocrine Pancreatic and Incretin Function Associated With Reactive Hypoglycemia. Circulation. 2017;135:1705-1719 pubmed publisher..Furthermore, glucose ingestion increased QT interval and aggravated the cardiac repolarization disturbances in LQT2 patients. URL: http://clinicaltrials.gov. Unique identifier: NCT02775513. ..
- Kang J, Wang L, Chen X, Triggle D, Rampe D. Interactions of a series of fluoroquinolone antibacterial drugs with the human cardiac K+ channel HERG. Mol Pharmacol. 2001;59:122-6 pubmed..HERG channel affinity should be an important criterion for the development of newer fluoroquinolones. ..
- Parent L. A helical segment makes potassium channels go-go. J Biol Chem. 2017;292:7706-7707 pubmed publisher..Matthew D. Perry and colleagues now combine NMR spectroscopy and electrophysiological experiments to explore the functional properties of mutations within an overlooked hERG helix, finding important contributions to channel function. ..
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- Teschemacher A, Seward E, Hancox J, Witchel H. Inhibition of the current of heterologously expressed HERG potassium channels by imipramine and amitriptyline. Br J Pharmacol. 1999;128:479-85 pubmed..Inhibition of IHERG by the prototype TCAs imipramine and amitriptyline may suggest a mechanism for QT prolongation associated with risks of arrhythmia and sudden death that accompany high concentrations of TCAs following overdose. ..