$\textit{Herschel}$-ATLAS:The connection between star formation and AGN activity in radio-loud and radio-quiet active galaxies by Gurkan, G, Hardcastle, M, Jarvis, M, Smith, D, Bourne, N, Dunne, L, Maddox, S, Ivison, R, Fritz, J

“…Radio-loud AGN are classified as high-excitation and low-excitation radio galaxies (HERGs, LERGs) using their emission lines and WISE 22-μm luminosity. …”

Four ways to fit an ion channel model by Clerx, M, Beattie, K, Gavaghan, D, Mirams, G

“…We compare these methods using a set of experiments in which hERG1a current was measured in nine Chinese Hamster Ovary (CHO) cells. …”

Human Purkinje in silico model enables mechanistic investigations into automaticity and pro-arrhythmic abnormalities by Trovato, C, Passini, E, Nagy, N, Varro, A, Abi-Gerges, N, Severi, S, Rodriguez, B

“…Simulations demonstrate the human Purkinje Trovato2020 model is the first one to yield: (i) all key AP features consistent with human Purkinje recordings; (ii) Automaticity with funny current up-regulation (iii) EADs at slow pacing and with 85% hERG block; (iv) DADs following fast pacing; (v) conduction velocity of 160 cm/s in a Purkinje fibre, as reported in human. …”

Identification, Synthesis, Conformation and Activity of an Insulin-like Peptide from a Sea Anemone by Michela L. Mitchell, Mohammed Akhter Hossain, Feng Lin, Ernesto L. Pinheiro-Junior, Steve Peigneur, Dorothy C. C. Wai, Carlie Delaine, Andrew J. Blyth, Briony E. Forbes, Jan Tytgat, John D. Wade, Raymond S. Norton

“…IlO1_i1 did not bind to the insulin or insulin-like growth factor receptors, but showed weak activity against K_V1.2, 1.3, 3.1, and 11.1 (hERG) channels, as well as Na_V1.4 channels. …”
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Antiarrhythmic Effects of Vernakalant in Human-Induced Pluripotent Stem Cell-Derived Cardiomyocytes from a Patient with Short QT Syndrome Type 1 by Qiang Xu, Xuemei Huang, Zenghui Meng, Yingrui Li, Rujia Zhong, Xin Li, Lukas Cyganek, Ibrahim El-Battrawy, Ibrahim Akin, Xiaobo Zhou, Huan Lan

“…Vernakalant failed to suppress the hERG channel currents but reduced the outward small-conductance calcium-activated potassium channel current. …”
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Design, Synthesis, and Biological Evaluation of 2-Substituted Aniline Pyrimidine Derivatives as Potent Dual Mer/c-Met Inhibitors by Daowei Huang, Ying Chen, Jixia Yang, Bingyang Zhao, Shouying Wang, Tingting Chai, Jie Cui, Xiaolei Zhou, Zhenhua Shang

“…Additionally, compound <b>18c</b> displayed good antiproliferative activities on HepG2, MDA-MB-231, and HCT116 cancer cells, along with favorable safety profiles in hERG testing. Notably, it exhibited exceptional liver microsomal stability in vitro, with a half-life of 53.1 min in human liver microsome. …”
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Toxicological Screening of Four Bioactive Citroflavonoids: In Vitro, In Vivo, and In Silico Approaches by Rolffy Ortiz-Andrade, Jesús Alfredo Araujo-León, Amanda Sánchez-Recillas, Gabriel Navarrete-Vazquez, Avel Adolfo González-Sánchez, Sergio Hidalgo-Figueroa, Ángel Josabad Alonso-Castro, Irma Aranda-González, Emanuel Hernández-Núñez, Tania Isolina Coral-Martínez, Juan Carlos Sánchez-Salgado, Victor Yáñez-Pérez, M. A. Lucio-Garcia

“…Furthermore, we used the ACD/Tox Suite to predict toxicological parameters such as hERG channel blockade, CYP450 inhibition, and acute toxicity in animals. …”
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Structural repurposing of SGLT2 inhibitor empagliflozin for strengthening anti-heart failure activity with lower glycosuria by Yixiang Xu, Chao Zhang, Kai Jiang, Xinchun Yang, Feng Chen, Zhiyang Cheng, Jinlong Zhao, Jiaxing Cheng, Xiaokang Li, Xin Chen, Luoyifan Zhou, Hao Duan, Yunyuan Huang, Yaozu Xiang, Jian Li

“…Furthermore, JX01 showed good safety profiles in respect of single-dose/repeat-dose toxicity and hERG activity, and good pharmacokinetic properties in both mouse and rat species. …”
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Plectasin, First Animal Toxin-Like Fungal Defensin Blocking Potassium Channels through Recognizing Channel Pore Region by Fang Xiang, Zili Xie, Jing Feng, Weishan Yang, Zhijian Cao, Wenxin Li, Zongyun Chen, Yingliang Wu

“…Besides Kv1.3 channel, plectasin could less inhibit Kv1.1, Kv1.2, IKCa, SKCa3, hERG and KCNQ channels at the concentration of 1 μΜ. …”
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Beauvericin counteracted multi-drug resistant Candida albicans by blocking ABC transporters by Yaojun Tong, Mei Liu, Yu Zhang, Xueting Liu, Ren Huang, Fuhang Song, Huanqin Dai, Biao Ren, Nuo Sun, Gang Pei, Jiang Bian, Xin-Ming Jia, Guanghua Huang, Xuyu Zhou, Shaojie Li, Buchang Zhang, Takashi Fukuda, Hiroshi Tomoda, Satoshi Ōmura, Richard D. Cannon, Richard Calderone, Lixin Zhang

“…Toxicity evaluation of BEA, including acute toxicity test, Ames test, and hERG (human ether-à-go-go-related gene) test promised that BEA can be harnessed for treatment of candidiasis, especially the candidiasis caused by ABC overexpressed multi-drug resistant C. albicans.…”
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Computational modeling and synthesis of pyridine variants of benzoyl-phenoxy-acetamide with high glioblastoma cytotoxicity and brain tumor penetration by Charles H. Ingraham, Joanna Stalinska, Sean C. Carson, Susan B. Colley, Monika Rak, Adam Lassak, Francesca Peruzzi, Krzysztof Reiss, Branko S. Jursic

“…Initially, over 100 structural BPA variations were analyzed and their physicochemical properties, such as water solubility (− logS), calculated partition coefficient (ClogP), probability for BBB crossing (BBB_SCORE), probability for CNS penetration (CNS-MPO) and calculated cardiotoxicity (hERG), were evaluated. This integrated approach allowed us to select pyridine variants of BPA that show improved BBB penetration, water solubility, and low cardiotoxicity. …”
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Integrated analysis of the voltage-gated potassium channel-associated gene KCNH2 across cancers by Zequn Zheng, Yongfei Song

“…Abstract KCNH2 encodes the human ether-a-go-go-related gene (hERG) potassium channel and is an important repolarization reserve for regulating cardiac electrical activity. …”
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High-conductance surface-anchoring of a mechanically flexible platform-based porphyrin complex by Nadine Hauptmann, Lynn Groß, Kristof Buchmann, Katharina Scheil, Christian Schütt, Franziska L Otte, Rainer Herges, Carmen Herrmann, Richard Berndt

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Biochemical and Electrophysiological Characterization of Two Sea Anemone Type 1 Potassium Toxins from a Geographically Distant Population of Bunodosoma caissarum by André J. Zaharenko, Jan Tytgat, José C. Freitas, Adriano M. C. Pimenta, José E. P. W. Bicudo, Gabriela G. Montandon, Juliana S. Cassoli, Bruno Madio, Diego J. B. Orts, Steve Peigneur

“…Their functional characterization was performed by means of a wide electrophysiological screening on 12 different subtypes of KV channels (KV1.1–KV1.6; KV2.1; KV3.1; KV4.2; KV4.3; hERG and Shaker IR). BcsTx1 shows a high affinity for rKv1.2 over rKv1.6, hKv1.3, Shaker IR and rKv1.1, while Bcstx2 potently blocked rKv1.6 over hKv1.3, rKv1.1, Shaker IR and rKv1.2. …”
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Drug‐induced shortening of the electromechanical window is an effective biomarker for in silico prediction of clinical risk of arrhythmias by Passini, E, Trovato, C, Morissette, P, Sannajust, F, Bueno-Orovio, A, Rodriguez, B

“…Due to its dependence on Ca2+‐transient, the EMw was also shown to be more sensitive than AP prolongation in distinguishing between pure hERG blockers and multichannel compounds also blocking the calcium current.…”

Simulation of the effects of extracellular calcium changes leads to a novel computational model of human ventricular action potential with a revised calcium handling by C Bartolucci, E Passini, J Hyttinen, M Paci, S Severi

“…We also used BPS2020 to generate an experimentally-calibrated population of models to investigate: (i) the occurrence of repolarization abnormalities in response to hERG current block; (ii) the rate adaptation variability; (iii) the occurrence of alternans and delayed after-depolarizations at fast pacing. …”

Variability in high-throughput ion-channel screening data and consequences for cardiac safety assessment by Elkins, R, Davies, MR, Brough, S, Gavaghan, D, Cui, Y, Abi-Gerges, N, Mirams, G

“…Methods: We quantified the variability associated with concentration-effect curves fitted to recordings from high-throughput Molecular Devices IonWorks® Quattro™ screens when detecting block of IKr (hERG), INa (NaV1.5), ICaL (CaV1.2), IKs (KCNQ1/minK) and Ito (Kv4.3/KChIP2.2), and the Molecular Devices FLIPR® Tetra fluorescence screen for ICaL (CaV1.2), for control compounds used at AstraZeneca and GlaxoSmithKline. …”

Evaluation of rosuvastatin-induced QT prolongation risk using real-world data, in vitro cardiomyocyte studies, and mortality assessment by Yeryung Koo, Sung-Ae Hyun, Byung Jin Choi, Yujeong Kim, Tae Young Kim, Hong-Seok Lim, Joung-Wook Seo, Dukyong Yoon

“…Abstract Drug-induced QT prolongation is attributed to several mechanisms, including hERG channel blockage. However, the risks, mechanisms, and the effects of rosuvastatin-induced QT prolongation remain unclear. …”
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Hydrocotyle bonariensis Comm ex Lamm (Araliaceae) leaves extract inhibits IKs not IKr potassium currents: Potential implications for anti-arrhythmic therapy by Komla Kaboua, Aklesso Mouzou, Tcha Pakoussi, Mindede Assih, Aurelien Chatelier, Aboudoulatifou Diallo, Patrick Bois, Jocelyn Bescond

“…Experimental procedure: The patch clamp experiments for IK currents recording were performed on the HEK 293 (Human Embryonic Kidney 293) cell line, stably transfected with either KCNQ1 and KCNE1 genes encoding the channel responsible for the ''IKs'' current (HEK293 IKs), or with hERG (human ether-a-go-go related gene) gene encoding ''IKr'' current (HEK293 IKr). …”
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Novel CFTR Activator Cact-3 Ameliorates Ocular Surface Dysfunctions in Scopolamine-Induced Dry Eye Mice by Dongkyu Jeon, Ikhyun Jun, Ho K. Lee, Jinhong Park, Bo-Rahm Kim, Kunhi Ryu, Hongchul Yoon, Tae-im Kim, Wan Namkung

“…Among them, the most potent CFTR activator, Cact-3 (7-(3,4-dimethoxyphenyl)-N-(4-ethoxyphenyl)pyrazolo [1,5-α]pyrimidine-2-carboxamide), produced large and sustained Cl⁻ currents in WT-CFTR-expressing FRT cells with no alterations of ANO1 and hERG channel activity. The application of Cact-3 strongly activated CFTR in the ocular epithelia of mice and it also significantly increased CFTR-mediated Cl⁻ transport in a primary cultured human conjunctival epithelium. …”
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