Outputs (68)

Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human β1-adrenoceptor (2013)
Journal Article
Baker, J. G., Hill, S. J., & Proudman, R. G. (2013). Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human β1-adrenoceptor. PLoS ONE, 8(11), https://doi.org/10.1371/journal.pone.0077582

β-blockers are widely used to improve symptoms and prolong life in heart disease primarily by inhibiting the actions of endogenous catecholamines at the β1-adrenoceptor. There are two common naturally occurring polymorphisms within the human β1-adren... Read More about Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human β1-adrenoceptor.

Increased function of pronociceptive TRPV1 at the level of the joint in a rat model of osteoarthritis pain (2013)
Journal Article
Kelly, S., Chapman, R., Woodhams, S., Sagar, D. R., Turner, J., Burston, J., …Chapman, V. (2014). Increased function of pronociceptive TRPV1 at the level of the joint in a rat model of osteoarthritis pain. Annals of the Rheumatic Diseases, 74, https://doi.org/10.1136/annrheumdis-2013-203413

Objectives Blockade of transient receptor potential vanilloid 1 (TRPV1) with systemic antagonists attenuates osteoarthritis (OA) pain behaviour in rat models, but on-target-mediated hyperthermia has halted clinical trials. The present study investiga... Read More about Increased function of pronociceptive TRPV1 at the level of the joint in a rat model of osteoarthritis pain.

Identification of multiple binding sites for the THAP domain of the Galileo transposase in the long terminal inverted-repeats (2013)
Journal Article
Marzo, M., Liu, D., Ruiz, A., & Chalmers, R. (2013). Identification of multiple binding sites for the THAP domain of the Galileo transposase in the long terminal inverted-repeats. Gene, 525(1), https://doi.org/10.1016/j.gene.2013.04.050

Galileo is a DNA transposon responsible for the generation of several chromosomal inversions in Drosophila. In contrast to other members of the P-element superfamily, it has unusually long terminal inverted-repeats (TIRs) that resemble those of Foldb... Read More about Identification of multiple binding sites for the THAP domain of the Galileo transposase in the long terminal inverted-repeats.

Synthesis and in vitro and in vivo characterization of highly β1-Selective β-Adrenoceptor partial agonists (2013)
Journal Article
Mistry, S. N., Baker, J. G., Fischer, P. M., Hill, S. J., Gardiner, S. M., & Kellam, B. (2013). Synthesis and in vitro and in vivo characterization of highly β1-Selective β-Adrenoceptor partial agonists. Journal of Medicinal Chemistry, 56(10), https://doi.org/10.1021/jm400348g

β-Adrenoceptor antagonists boast a 50-year use for symptomatic control in numerous cardiovascular diseases. One might expect highly selective antagonists are available for the human β-adrenoceptor subtype involved in these diseases, yet few truly β1-... Read More about Synthesis and in vitro and in vivo characterization of highly β1-Selective β-Adrenoceptor partial agonists.

Heavy and light roles: myosin in the morphogenesis of the heart (2013)
Journal Article
England, J., & Loughna, S. (2013). Heavy and light roles: myosin in the morphogenesis of the heart. Cellular and Molecular Life Sciences, 70(7), https://doi.org/10.1007/s00018-012-1131-1

Myosin is an essential component of cardiac muscle, from the onset of cardiogenesis through to the adult heart. Although traditionally known for its role in energy transduction and force development, recent studies suggest that both myosin heavy-cha... Read More about Heavy and light roles: myosin in the morphogenesis of the heart.

D-amphetamine and antipsychotic drug effects on latent inhibition in mice lacking dopamine D2 receptors (2013)
Journal Article
Bay-Richter, C., O'Callaghan, M., Mathur, N., O'Tuathaigh, C., Heery, D., Fone, K. C., …Moran, P. (in press). D-amphetamine and antipsychotic drug effects on latent inhibition in mice lacking dopamine D2 receptors. Neuropsychopharmacology, 38(8), https://doi.org/10.1038/npp.2013.50

Drugs that induce psychosis, such as D-amphetamine (AMP), and those that alleviate it, such as antipsychotics, are suggested to exert behavioral effects via dopamine receptor D2 (D2). All antipsychotic drugs are D2 antagonists, but D2 antagonism und... Read More about D-amphetamine and antipsychotic drug effects on latent inhibition in mice lacking dopamine D2 receptors.

Hsmar1 transposition is sensitive to the topology of the transposon donor and the target (2013)
Journal Article
Claeys Bouuaert, C., & Chalmers, R. (2013). Hsmar1 transposition is sensitive to the topology of the transposon donor and the target. PLoS ONE, 8(1), Article 0053690. https://doi.org/10.1371/journal.pone.0053690

Hsmar1 is a member of the Tc1-mariner superfamily of DNA transposons. These elements mobilize within the genome of their host by a cut-and-paste mechanism. We have exploited the in vitro reaction provided by Hsmar1 to investigate the effect of DNA su... Read More about Hsmar1 transposition is sensitive to the topology of the transposon donor and the target.

The extracellular signal-regulated kinase (ERK) pathway: a potential therapeutic target in hypertension (2012)
Journal Article
Roberts, R. E. (2012). The extracellular signal-regulated kinase (ERK) pathway: a potential therapeutic target in hypertension. Journal of Experimental Pharmacology, 4, https://doi.org/10.2147/JEP.S28907

Hypertension is a risk factor for myocardial infarction, stroke, renal failure, heart failure, and peripheral vascular disease. One feature of hypertension is a hyperresponsiveness to contractile agents, and inhibition of vasoconstriction forms the b... Read More about The extracellular signal-regulated kinase (ERK) pathway: a potential therapeutic target in hypertension.

Fluorescence correlation spectroscopy, combined with bimolecular fluorescence complementation, reveals the effects of β-arrestin complexes and endocytic targeting on the membrane mobility of neuropeptide Y receptors (2012)
Journal Article
Kilpatrick, L. E., Briddon, S. J., & Holliday, N. D. (2012). Fluorescence correlation spectroscopy, combined with bimolecular fluorescence complementation, reveals the effects of β-arrestin complexes and endocytic targeting on the membrane mobility of neuropeptide Y receptors. Biochimica et Biophysica Acta (BBA) - Molecular Cell Research, 1823(6),

Fluorescence correlation spectroscopy (FCS) and photon counting histogram (PCH) analysis are powerful ways to study mobility and stoichiometry of G protein coupled receptor complexes, within microdomains of single living cells. However, relating thes... Read More about Fluorescence correlation spectroscopy, combined with bimolecular fluorescence complementation, reveals the effects of β-arrestin complexes and endocytic targeting on the membrane mobility of neuropeptide Y receptors.

Fluoxetine counteracts the cognitive and cellular effects of 5-Fluorouracil in the rat hippocampus by a mechanism of prevention rather than recovery (2012)
Journal Article
Lyons, L., ELBeltagy, M., Bennett, G., & Wigmore, P. (2012). Fluoxetine counteracts the cognitive and cellular effects of 5-Fluorouracil in the rat hippocampus by a mechanism of prevention rather than recovery. PLoS ONE, 7(1), Article e30010. https://doi.org/10.1371/journal.pone.0030010

5-Fluorouracil (5-FU) is a cytostatic drug associated with chemotherapy-induced cognitive impairments that many cancer patients experience after treatment. Previous work in rodents has shown that 5-FU reduces hippocampal cell proliferation, a possi... Read More about Fluoxetine counteracts the cognitive and cellular effects of 5-Fluorouracil in the rat hippocampus by a mechanism of prevention rather than recovery.