In vitro and in vivo pharmacological characterization of 5-[(R)-2-(5, 6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one (indacaterol), a novel …

…, D Farr, JR Fozard, JR Leighton-Davies… - … of Pharmacology and …, 2006 - ASPET
Here, we describe the preclinical pharmacological profile of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one
(indacaterol), a novel, chirally pure …

Miniaturized receptor binding assays: complications arising from ligand depletion

CMS Carter, JR Leighton-Davies… - Journal of …, 2007 - journals.sagepub.com
The advent of miniaturized assay formats has made possible the screening of large numbers
of compounds against a single target, known as high-throughput screening. Despite this …

ATP priming of macrophage-derived chemokine responses in CHO cells expressing the CCR4 receptor

EM Rosethorne, JR Leighton-Davies, D Beer… - Naunyn-Schmiedeberg's …, 2004 - Springer
The mechanism by which ATP primes for subsequent macrophage-derived chemokine (MDC)
mediated intracellular calcium (Ca 2+ i ) responses at the human CCR4 receptor stably …

[HTML][HTML] R-Spondin potentiates Wnt/β-catenin signaling through orphan receptors LGR4 and LGR5

H Ruffner, J Sprunger, O Charlat, J Leighton-Davies… - PloS one, 2012 - journals.plos.org
The Wnt/β-catenin signaling pathbway controls many important biological processes. R-Spondin
(RSPO) proteins are a family of secreted molecules that strongly potentiate Wnt/β-…

The influence of receptor kinetics on the onset and duration of action and the therapeutic index of NVA237 and tiotropium

DA Sykes, MR Dowling, J Leighton-Davies… - … of Pharmacology and …, 2012 - ASPET
Studies under nonphysiological conditions suggest that long receptor residency time is
responsible for the 24-h duration of action of the long-acting muscarinic antagonist (LAMA) …

Class III phosphatidylinositol 4-kinase alpha and beta are novel host factor regulators of hepatitis C virus replication

…, SC Zhao, C Mickanin, J Leighton-Davies… - Journal of …, 2009 - Am Soc Microbiol
Host factor pathways are known to be essential for hepatitis C virus (HCV) infection and
replication in human liver cells. To search for novel host factor proteins required for HCV …

[HTML][HTML] Identification of the C3a receptor (C3AR1) as the target of the VGF-derived peptide TLQP-21 in rodent cells

S Hannedouche, V Beck, J Leighton-Davies… - Journal of Biological …, 2013 - ASBMB
TLQP-21, a peptide derived from VGF (non-acronymic) by proteolytic processing, has been
shown to modulate energy metabolism, differentiation, and cellular response to stress. …

Blockade of metallothioneins 1 and 2 increases skeletal muscle mass and strength

…, C Dornelas, C Fryer, J Leighton-Davies… - … and cellular biology, 2017 - Taylor & Francis
Metallothioneins are proteins that are involved in intracellular zinc storage and transport.
Their expression levels have been reported to be elevated in several settings of skeletal …

[HTML][HTML] MiR-210 promotes sensory hair cell formation in the organ of corti

…, F Sigoillot, M Beibel, A Werner, J Leighton-Davies… - BMC genomics, 2016 - Springer
Background Hearing loss is the most common sensory defect afflicting several hundred million
people worldwide. In most cases, regardless of the original cause, hearing loss is related …

Design and synthesis of a library of chemokine antagonists

…, A Glen, T Howe, T Keller, J Leighton-Davies… - Bioorganic & medicinal …, 2011 - Elsevier
A library of chemokine antagonists has been synthesized using a combination of solid and
solution-phase chemistry. Structures of known chemokine antagonists were used to produce …