Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: evidence for a …

WS Redfern, L Carlsson, AS Davis… - Cardiovascular …, 2003 - academic.oup.com
Objective: To attempt to determine the relative value of preclinical cardiac electrophysiology
data (in vitro and in vivo) for predicting risk of torsade de pointes (TdP) in clinical use …

H1‐antihistamines: inverse agonism, anti‐inflammatory actions and cardiac effects

R Leurs, MK Church… - Clinical & Experimental …, 2002 - Wiley Online Library
This review addresses novel concepts of histamine H1‐receptor function and attempts to
relate them to the anti‐inflammatory effects of H1‐antihistamines. Furthermore, the …

Saxitoxin, a toxic marine natural product that targets a multitude of receptors

LE Llewellyn - Natural product reports, 2006 - pubs.rsc.org
Covering: up to the end of 2005Saxitoxin (STX) was discovered early last century and can
contaminate seafood and drinking water, and over time has become an invaluable research …

AfroDb: a select highly potent and diverse natural product library from African medicinal plants

F Ntie-Kang, D Zofou, SB Babiaka, R Meudom… - PloS one, 2013 - journals.plos.org
Computer-aided drug design (CADD) often involves virtual screening (VS) of large
compound datasets and the availability of such is vital for drug discovery protocols. We …

Toward a Pharmacophore for Drugs Inducing the Long QT Syndrome:  Insights from a CoMFA Study of HERG K+ Channel Blockers

A Cavalli, E Poluzzi, F De Ponti… - Journal of medicinal …, 2002 - ACS Publications
In this paper, we present a pharmacophore for QT-prolonging drugs, along with a 3D QSAR
(CoMFA) study for a series of very structurally variegate HERG K+ channel blockers. The …

NANPDB: a resource for natural products from Northern African sources

F Ntie-Kang, KK Telukunta, K Döring… - Journal of natural …, 2017 - ACS Publications
Natural products (NPs) are often regarded as sources of drugs or drug leads or simply as a
“source of inspiration” for the discovery of novel drugs. We have built the Northern African …

Role of the cytosolic chaperones Hsp70 and Hsp90 in maturation of the cardiac potassium channel HERG

E Ficker, AT Dennis, L Wang, AM Brown - Circulation research, 2003 - ahajournals.org
The human ether-a-gogo–related gene (hERG) encodes the α subunit of the cardiac
potassium current I Kr. Several mutations in hERG produce trafficking-deficient channels that …

Integrating virtual screening in lead discovery

TI Oprea, H Matter - Current opinion in chemical biology, 2004 - Elsevier
Target-and ligand-based virtual screening have emerged as resource-saving techniques
that have been successfully applied to identify novel chemotypes in biologically active …

QT prolongation through hERG K+ channel blockade: Current knowledge and strategies for the early prediction during drug development

M Recanatini, E Poluzzi, M Masetti… - Medicinal research …, 2005 - Wiley Online Library
Prolongation of the QT interval of the electrocardiogram is a typical effect of Class III
antiarrhythmic drugs, achieved through blockade of potassium channels. In the past decade …

The hERG potassium channel and hERG screening for drug-induced torsades de pointes

JC Hancox, MJ McPate, A El Harchi… - Pharmacology & …, 2008 - Elsevier
Drug-induced torsades de pointes (TdP) arrhythmia is a major safety concern in the process
of drug design and development. The incidence of TdP tends to be low, so early pre-clinical …