Results 81 to 90 of about 31,297 (199)

Antiplasmodial Activity and Pharmacokinetic Profiling of Cryptolepine and 2,7‐Dibromocryptolepine With a View to Informing the Design of Novel Antimalarial Cryptolepine Analogues

Drug Development Research, Volume 87, Issue 2, April 2026.
ABSTRACT The roots of the climbing shrub Cryptolepis sanguinolenta are traditionally used in West Africa for the treatment of malaria. The principal constituent, cryptolepine (1), has been shown to have antimalarial activity but there are concerns regarding its toxicity on account of its DNA‐intercalating property.
Elodie Chenu, James Duffy, Arnold Donkor Forkuo, Stephen Y. Gbedema, Seham Abdelall, Muhammad Wahajuddin, Huw S. Jones, Colin W. Wright   +7 more
wiley   +1 more source

Evaluation of clinical cardiac safety of zilurgisertib, an activin receptor‐like kinase‐2 (ALK2) inhibitor, in healthy participants

Clinical Pharmacology in Drug Development, Volume 15, Issue 2, February 2026.
Abstract The oral, small molecule inhibitor of activin receptor‐like kinase‐2, zilurgisertib (INCB000928), is under evaluation in fibrodysplasia ossificans progressiva. Cardiac safety was assessed using electrocardiogram (ECG) parameters and a plasma concentration‐heart rate‐corrected QT (C‐QTc) interval analysis of pooled data from single ascending ...
Yan‐ou Yang, Hong Yang, Xing Liu, Xiaohua Gong, Jay Getsy, Kevin Rockich   +5 more
wiley   +1 more source

Validation of a [3H]Astemizole Binding Assay in HEK293 Cells Expressing HERG K+ Channels

Journal of Pharmacological Sciences, 2004
A radioligand binding assay for the HERG (human ether-a-go-go-related gene) K+ channel was developed to identify compounds which may have inhibitory activity and potential cardiotoxicity.
Peter J.S. Chiu, Karen F. Marcoe, Sidney E. Bounds, Chun-Hsiung Lin, Jin-Jye Feng, Atsui Lin, Fong-Chi Cheng, William J. Crumb, Richard Mitchell   +8 more
doaj   +1 more source

Project Retrosight. Understanding the returns from cardiovascular and stroke research: Policy Report [PDF]

, 2011
Copyright @ 2011 RAND Europe. All rights reserved. The full text article and the summary of the article are both available via the links below.This project explores the impacts arising from cardiovascular and stroke research funded 15-20 years ago and ...
Buxton, MJ, Grant, J, Hanney, S, on behalf of the Project Retrosight Team, Pollitt, A, Wooding, S   +5 more
core  

Cytotoxic and Antileishmanial Potential of Pilocarpus microphyllus Essential Oil: In Vitro and In Silico Study

Chemistry &Biodiversity, Volume 23, Issue 1, January 2026.
Jaborandi (Pilocarpus microphyllus) essential oil is obtained by removal and characterization using GC‐MS, revealing γ‐cadinene and trans‐caryophyllene as major constituents. The oil exhibits biological activity, with antifungal action against Candida spp.
Juniel Cruz Silva, Maria Gabriela Araújo Mendes, Paulo Sérgio de Araujo Sousa, Alyne Rodrigues de Araújo Nobre, Michel Muálem de Moraes Alves, Fernando Aécio de Amorim Carvalho, Tatiane Caroline Daboit, José de Sousa Lima Neto, Ygor Victor Ferreira Pinheiro, Ytallo da Costa Sousa, Edymilaís da Silva Sousa, José Delano Barreto Marinho Filho, Ana Jérsia Araújo, Francisco Artur Silva Filho, Sidney Gonçalo de Lima, Leiz Maria Costa Véras   +15 more
wiley   +1 more source

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

CardioGenAI: a machine learning-based framework for re-engineering drugs for reduced hERG liability

Journal of Cheminformatics
The link between in vitro hERG ion channel inhibition and subsequent in vivo QT interval prolongation, a critical risk factor for the development of arrythmias such as Torsade de Pointes, is so well established that in vitro hERG activity alone is often ...
Gregory W. Kyro, Matthew T. Martin, Eric D. Watt, Victor S. Batista   +3 more
doaj   +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

A minK-HERG complex regulates the cardiac potassium current I(Kr). [PDF]

, 1997
MinK is a widely expressed protein of relative molecular mass approximately 15K that forms potassium channels by aggregation with other membrane proteins.
Fishman, GI, Goldstein, SA, McDonald, TV, Meyers, MB, Ming, Z, Palma, E, Wang, KW, Yu, Z   +7 more
core  

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