Development of safe drugs: the hERG challenge

S Kalyaanamoorthy, KH Barakat - Medicinal research reviews, 2018 - Wiley Online Library
Drug‐induced blockade of human ether‐a‐go‐go‐related gene (hERG) remains a major
impediment in delivering safe drugs to the market. Several drugs have been withdrawn from …

Pushing the boundaries of molecular representation for drug discovery with the graph attention mechanism

Z **ong, D Wang, X Liu, F Zhong, X Wan… - Journal of medicinal …, 2019 - ACS Publications
Hunting for chemicals with favorable pharmacological, toxicological, and pharmacokinetic
properties remains a formidable challenge for drug discovery. Deep learning provides us …

Computational investigations of hERG channel blockers: New insights and current predictive models

BO Villoutreix, O Taboureau - Advanced drug delivery reviews, 2015 - Elsevier
Identification of potential human Ether-a-go-go Related-Gene (hERG) potassium channel
blockers is an essential part of the drug development and drug safety process in …

Coloring molecules with explainable artificial intelligence for preclinical relevance assessment

J Jiménez-Luna, M Skalic, N Weskamp… - Journal of Chemical …, 2021 - ACS Publications
Graph neural networks are able to solve certain drug discovery tasks such as molecular
property prediction and de novo molecule generation. However, these models are …

Pred‐hERG: A novel web‐accessible computational tool for predicting cardiac toxicity

RC Braga, VM Alves, MFB Silva, E Muratov… - Molecular …, 2015 - Wiley Online Library
The blockage of the hERG K+ channels is closely associated with lethal cardiac arrhythmia.
The notorious ligand promiscuity of this channel earmarked hERG as one of the most …

Structure-based prediction of hERG-related cardiotoxicity: A benchmark study

TM Creanza, P Delre, N Ancona, G Lentini… - Journal of Chemical …, 2021 - ACS Publications
Drug-induced blockade of the human ether-à-go-go-related gene (hERG) channel is today
considered the main cause of cardiotoxicity in postmarketing surveillance. Hence, several …

cardioToxCSM: A Web Server for Predicting Cardiotoxicity of Small Molecules

S Iftkhar, AGC de Sá, JPL Velloso, R Aljarf… - Journal of Chemical …, 2022 - ACS Publications
The design of novel, safe, and effective drugs to treat human diseases is a challenging
venture, with toxicity being one of the main sources of attrition at later stages of …

Alarms about structural alerts

VM Alves, EN Muratov, SJ Capuzzi, R Politi, Y Low… - Green …, 2016 - pubs.rsc.org
Structural alerts are widely accepted in chemical toxicology and regulatory decision support
as a simple and transparent means to flag potential chemical hazards or group compounds …

Deep Learning-driven research for drug discovery: Tackling Malaria

BJ Neves, RC Braga, VM Alves… - PLoS computational …, 2020 - journals.plos.org
Malaria is an infectious disease that affects over 216 million people worldwide, killing over
445,000 patients annually. Due to the constant emergence of parasitic resistance to the …

Prediction of arrhythmia susceptibility through mathematical modeling and machine learning

M Varshneya, X Mei, EA Sobie - Proceedings of the …, 2021 - National Acad Sciences
At present, the QT interval on the electrocardiographic (ECG) waveform is the most common
metric for assessing an individual's susceptibility to ventricular arrhythmias, with a long QT …