Results 91 to 100 of about 5,479 (195)

Construction of an integrated database for hERG blocking small molecules.

PLoS ONE, 2018
The inhibition of the hERG potassium channel is closely related to the prolonged QT interval, and thus assessing this risk could greatly facilitate the development of therapeutic compounds and the withdrawal of hazardous marketed drugs.
Tomohiro Sato, Hitomi Yuki, Keiji Ogura, Teruki Honma   +3 more
doaj   +1 more source

Effect of thapsigargin (1 µM) on voltage-dependent activation of hERG channel.

, 2013
Inset shows the voltage clamp protocol. a-f: Representative current traces in HEK293 cells transfected with WT-hERG, WT/E637K-hERG, and E637K-hERG in the presence or absence of thapsigargin.
Justin Michael Karush (423498), Ningsheng Liu (335951), Xiaoyan Huang (112885), Yanna Ba (112883), Jiangfang Lian (112879), Xiaoli Lu (423497), Jianqing Zhou (112889), Ying Wang (11406), Haiyan Mao (335948), Xi Yang (112884)   +9 more
core   +1 more source

Advances in New Approach Methodologies at FDA's Division of Applied Regulatory Science

Clinical Pharmacology &Therapeutics, Volume 120, Issue 5, Page 1250-1254, November 2026.
New Approach Methodologies (NAMs) represent a paradigm shift in drug development and regulatory science, offering human‐relevant alternatives to traditional preclinical models. This mini‐review highlights recent advances in NAM development, validation, and regulatory application from FDA's Division of Applied Regulatory Science (DARS).
Ksenia Blinova, Kimberly Chiu, Anik Chaturbedi, Jahan Cooper, Tromondae K. Feaster, Paula L. Hyland, Lidiya Stavitskaya, Wendy W. Wu, Jeffry Florian, Rodney Rouse   +9 more
wiley   +1 more source

Ginkgo biloba Extract and Ginkgolide Antiarrhythmic Potential by Targeting hERG and ICa-L Channel

Journal of Pharmacological Sciences, 2013
We investigated the effects of Ginkgo biloba extract (GBE) and ginkgolide (GLD) on human ether-a-go-go-related gene (hERG)-encoded K+ channels and its underlying mechanisms in the hERG-HEK293 cell line by determining GBE- and GLD-induced changes in ...
Xin Zhao, Hong Yao, Hao-Lan Yin, Qi-Lei Zhu, Jia-Liang Sun, Wei Ma, Yuan-Qi Shi, Zhao-Guang Liang, Bao-Xin Li   +8 more
doaj   +1 more source

In Silico Clinical Trials in Drug Development: Virtual Patients, Applications, and Regulatory Convergence

Clinical Pharmacology &Therapeutics, Volume 120, Issue 5, Page 1181-1194, November 2026.
Conventional clinical trials remain the benchmark for evaluating therapeutic safety and efficacy, yet they are constrained by escalating costs, withdrawal over the extended follow‐up periods, recruitment difficulties, ethical limits, and a restricted ability to characterize heterogeneous populations.
Maximilian Balmus, Sheng‐Ya Wang, Edward W. G. Ashton, Rosie K. Barrows, Molly Monks, Yuzhang Ge, Arthur Lefebvre, Steven A. Niederer   +7 more
wiley   +1 more source

Mechanisms underlying probucol-induced hERG-channel deficiency

, 2015
Yuan-Qi Shi,1,* Cai-Chuan Yan,1,* Xiao Zhang,1 Meng Yan,1 Li-Rong Liu,1 Huai-Ze Geng,1 Lin Lv,1 Bao-Xin Li1,21Department of Pharmacology, Harbin Medical University, 2State-Province Key Laboratory of Biopharmaceutical Engineering, Harbin, Heilongjiang ...
Yan M, Yan CC, Lv L, Liu LR, Li BX, Zhang X, Shi YQ, Geng HZ   +7 more
core  

Effect of PD-118057 (3 µM) on voltage-dependent activation of hERG channel.

, 2013
Inset shows the voltage clamp protocol. a-f: Representative current traces in HEK293 cells transfected with WT-hERG, WT/E637K-hERG, and E637K-hERG in the presence or absence of PD-118057.
Justin Michael Karush (423498), Ningsheng Liu (335951), Xiaoyan Huang (112885), Yanna Ba (112883), Jiangfang Lian (112879), Xiaoli Lu (423497), Jianqing Zhou (112889), Ying Wang (11406), Haiyan Mao (335948), Xi Yang (112884)   +9 more
core   +1 more source

Pediatric Developmental Safety Assessment and New Approach Methodologies: US FDA/Triangle CERSI Workshop Report

Clinical Pharmacology &Therapeutics, Volume 120, Issue 5, Page 1240-1249, November 2026.
Pediatric developmental safety assessment presents distinct challenges in drug development. Children undergo dynamic changes in organ systems and drug disposition pathways during development, and drug‐related effects may be delayed or manifested differently than in adults.
Gilbert J. Burckart, Gelareh Abulwerdi, Christin L. Daniels, Calib Choi, Rebecca Racz, Jean‐Pierre Valentin, Kristin Ardlie, Nicholas Tatonetti, Susan Laffan, Marjory Moreau, Will Redfern, Lang Li, James J. Hickman, Rajanikanth Madabushi, Bhagwat Prasad, Lynne Yao, Paul B. Watkins   +16 more
wiley   +1 more source

Plasmepsins as Antimalarial Drug Targets—Then, Now, and the Future

Medicinal Research Reviews, Volume 46, Issue 6, Page 1574-1602, November 2026.
ABSTRACT Malaria is a devastating disease caused by Plasmodium parasites. Plasmodium parasites express ten cathepsin D‐like aspartyl proteases, called plasmepsins (PMs). These PMs have diverse roles fulfill diverse functions throughout the parasite's lifecycle, though several exhibit functional redundancies. Among them, PMV, PMIV, and PMX are essential
Brad E. Sleebs
wiley   +1 more source

Electrophysiological characterization of a small molecule activator on human ether-a-go-go-related gene (hERG) potassium channel

Journal of Pharmacological Sciences, 2019
The human ether-a-go-go-related gene (hERG) encodes the K+ channel that carries the rapid component of the delayed rectifier current in the human heart. Reduction of hERG activity induced by gene mutations or pharmacological inhibition is responsible for
Xiuming Dong, Yani Liu, Heling Niu, Gongxin Wang, Liying Dong, Anruo Zou, KeWei Wang   +6 more
doaj   +1 more source