Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Derek J. Trezise"'
Autor:
Andrew J. Powell, Michael J. Carr, Dramane I. Laine, Stacey L. Walsh, Emma Ward, David L. Downie, Derek J. Trezise, Mao Xiang Chen, Helen F. Sneddon, Kelly M Gatfield
Publikováno v:
SLAS Discovery. 20:242-253
The epithelial sodium channel (ENaC) plays a crucial role in salt and water homeostasis and is primarily involved in sodium reabsorption in the kidney and lung. Modulators of ENaC function, particularly within lung epithelia, could offer potential tr
Publikováno v:
Cancer Research. 78:749-749
Monoclonal antibodies (mAb) and antibody-drug conjugates (ADCs) are widely used as anti-cancer therapeutics. A key property of these biologics is the extent and rate of internalization into different cells, which governs their efficacy, safety and ph
Autor:
Kalpana Patel, Derek J. Trezise, Nevine Holtz, Tim Dale, Gillian Lovell, Nicola Bevan, Miniver Oliver, Tim Jackson, Nicholas Dana
Publikováno v:
Cancer Research. 78:5030-5030
The tumor-associated extracellular matrix (ECM) provides critical biochemical micro-environment cues, as well as an essential structural scaffold, for solid tumors to survive and grow (see Pickup et al. 2014 for review). With a view to enabling more
Autor:
Tim Dale, Helen J. Meadows, Andrew J. Powell, Jeffrey J. Clare, Emma C. Hollands, Andrew Baxter, Derek J. Trezise
Publikováno v:
SLAS Discovery. 14:769-780
Gamma-amino butyric acid (GABA)-activated Cl- channels are critical mediators of inhibitory postsynaptic potentials in the CNS. To date, rational design efforts to identify potent and selective GABA(A) subtype ligands have been hampered by the absenc
Autor:
David D. Miller, Marianne L. Jensen, Charlotte Hougaard, Dorte Strøbæk, Palle Christophersen, Tim Dale, David John Davies, Birgitte L. Eriksen, Derek J. Trezise
Publikováno v:
Molecular Pharmacology. 76:569-578
A new small molecule, 4-(2-methoxy-phenylcarbamoyloxymethyl)-piperidine-1-carboxylic acid tert-butyl ester (GW542573X), is presented as an activator of small-conductance Ca2+-activated K+ (SK, KCa2) channels and distinguished from previously publishe
Autor:
Derek J. Trezise, Jean-Philippe Walhin, Noel W. Davies, Leanne Partington, Martine Hamann, Adele Gibson, Martin J. Main, Karen Affleck, Amanda Jowett
Publikováno v:
The Journal of Physiology. 587:2255-2274
Proteins of the CLCA gene family including the human ClCa1 (hClCa1) have been suggested to constitute a new family of chloride channels mediating Ca2+-dependent Cl− currents. The present study examines the relationship between the hClCa1 protein an
Publikováno v:
Combinatorial Chemistry & High Throughput Screening. 12:96-106
The tractability of ion channels as drug targets has been significantly improved by the advent of planar array electrophysiology platforms which have dramatically increased the capacity for electrophysiological profiling of lead series compounds. How
Publikováno v:
Neuropharmacology. 53:58-70
Group I metabotropic glutamate receptors (mGluRs) contribute to spinal sensitization and synaptic plasticity but the underlying mechanisms are unknown. Here, group I mGluR modulation of evoked monosynaptic excitatory postsynaptic currents (EPSCs) in
Autor:
Emma C. Hollands, Derek J. Trezise, Victoria H John, David L. Downie, Mao Xiang Chen, Tim Dale, Leanne Partington, Helen J. Meadows
Publikováno v:
SLAS Discovery. 12:50-60
Planar array electrophysiology techniques were applied to assays for modulators of recombinant hIK and hSK3 Ca2+-activated K+ channels. In CHO-hIK-expressing cells, under asymmetric K+ gradients, small-molecule channel activators evoked time- and vol
Autor:
Amanda Jowett, Derek J. Trezise, Guy W. J. Moss, Mao Xiang Chen, Anthony H. Dickenson, Rie Suzuki, Parmvir K. Bahia, David C. H. Benton
Publikováno v:
The Journal of Neuroscience. 25:3489-3498
We investigated the role of small-conductance calcium-activated potassium (SK) and intermediate-conductance calcium-activated potassium channels in modulating sensory transmission from peripheral afferents into the rat spinal cord. Subunit-specific a