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Pharmacological enhancement of leg and muscle microvascular blood flow does not augment anabolic responses in skeletal muscle of young men under fed conditions (2013)
Journal Article
Phillips, B. E., Atherton, P. J., Varadhan, K., Wilkinson, D. J., Limb, M. C., Selby, A. L., …Williams, J. P. (2014). Pharmacological enhancement of leg and muscle microvascular blood flow does not augment anabolic responses in skeletal muscle of young men under fed conditions. AJP - Endocrinology and Metabolism, 306(2), Article E168-E176. https://doi.org/10.1152/ajpendo.00440.2013

Skeletal muscle anabolism associated with postprandial plasma aminoacidemia and insulinemia is contingent upon amino acids (AA) and insulin crossing the microcirculation-myocyte interface. In this study, we hypothesized that increasing muscle microva... Read More about Pharmacological enhancement of leg and muscle microvascular blood flow does not augment anabolic responses in skeletal muscle of young men under fed conditions.

The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledgebase of drug targets and their ligands (2013)
Journal Article
Pawson, A. J., Sharman, J. L., Benson, H. E., Faccenda, E., Alexander, S. P., Buneman, O. P., …Harmar, A. J. (2014). The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledgebase of drug targets and their ligands. Nucleic Acids Research, 42(D1), Article D1098-D1106. https://doi.org/10.1093/nar/gkt1143

The International Union of Basic and Clinical Pharmacology/British Pharmacological Society (IUPHAR/BPS) Guide to PHARMACOLOGY (http://www.guidetopharmacology.org) is a new open access resource providing pharmacological, chemical, genetic, functional... Read More about The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledgebase of drug targets and their ligands.

Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human ?1-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 ?1-adrenoceptor. PLoS ONE, 8(11), https://doi.org/10.1371/journal.pone.0077582

?-blockers are widely used to improve symptoms and prolong life in heart disease primarily by inhibiting the actions of endogenous catecholamines at the ?1-adrenoceptor. There are two common naturally occurring polymorphisms within the human ?1-adren... Read More about Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human ?1-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 ?1-Selective ?-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 ?1-Selective ?-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 ?1-Selective ?-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 ?-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 ?-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 ?-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.

Predicting in vivo cardiovascular properties of ?-blockers from cellular assays: a quantative comparison of cellular and cardiovascular pharmacological responses (2011)
Journal Article
Baker, J. G., Kemp, P., March, J., Fretwell, L., Hill, S. J., & Gardiner, S. M. (2011). Predicting in vivo cardiovascular properties of ?-blockers from cellular assays: a quantative comparison of cellular and cardiovascular pharmacological responses. FASEB Journal, 25(12), https://doi.org/10.1096/fj.11-192435

?-Adrenoceptor antagonists differ in their degree of partial agonism. In vitro assays have provided information on ligand affinity, selectivity, and intrinsic efficacy. However, the extent to which these properties are manifest in vivo is less clear.... Read More about Predicting in vivo cardiovascular properties of ?-blockers from cellular assays: a quantative comparison of cellular and cardiovascular pharmacological responses.

Dimerization of ABCG2 analysed by bimolecular fluorescence complementation (2011)
Journal Article
Haider, A. J., Briggs, D., Self, T. J., Chilvers, H. L., Holliday, N. D., & Kerr, I. D. (2011). Dimerization of ABCG2 analysed by bimolecular fluorescence complementation. PLoS ONE, 6(10), Article e25818. https://doi.org/10.1371/journal.pone.0025818

ABCG2 is one of three human ATP binding cassette transporters that are functionally capable of exporting a diverse range of substrates from cells. The physiological consequence of ABCG2 multidrug transport activity in leukaemia, and some solid tumour... Read More about Dimerization of ABCG2 analysed by bimolecular fluorescence complementation.

Knockdown of embryonic myosin heavy chain reveals an essential role in the morphology and function of the developing heart (2011)
Journal Article
Rutland, C. S., Polo-Parada, L., Ehler, E., Alibhai, A., Thorpe, A., Suren, S., …Loughna, S. (2011). Knockdown of embryonic myosin heavy chain reveals an essential role in the morphology and function of the developing heart. Development, 138(18), https://doi.org/10.1242/dev.059063

The expression and function of embryonic myosin heavy chain (eMYH) has not been investigated within the early developing heart. This is despite the knowledge that other structural proteins, such as alpha and beta myosin heavy chains and cardiac alpha... Read More about Knockdown of embryonic myosin heavy chain reveals an essential role in the morphology and function of the developing heart.

Functional network construction in Arabidopsis using rule-based machine learning on large-scale data sets (2011)
Journal Article
Bassel, G. W., Glaab, E., Marquez, J., Holdsworth, M. J., & Barcardit, J. (2011). Functional network construction in Arabidopsis using rule-based machine learning on large-scale data sets. Plant Cell, 23(9), https://doi.org/10.1105/tpc.111.088153

The meta-analysis of large-scale postgenomics data sets within public databases promises to provide important novel biological knowledge. Statistical approaches including correlation analyses in coexpression studies of gene expression have emerged as... Read More about Functional network construction in Arabidopsis using rule-based machine learning on large-scale data sets.

SUMO conjugation of STAT1 protects cells from hyperresponsiveness to IFN? (2011)
Journal Article
Begitt, A., Droescher, M., Knobeloch, K., & Vinkemeier, U. (2011). SUMO conjugation of STAT1 protects cells from hyperresponsiveness to IFN?. Blood, 118(4), https://doi.org/10.1182/blood-2011-04-347930

The biologic effects of IFNγ are mediated by the transcription factor STAT1. The activity of STAT1 is inhibited by small ubiquitin-like modifier (SUMO) conjugation. This occurs both directly through decreasing STAT1 tyrosine phosphorylation and indir... Read More about SUMO conjugation of STAT1 protects cells from hyperresponsiveness to IFN?.

STAT1 signaling is not regulated by a phosphorylation-acetylation switch (2011)
Journal Article
Antunes, F., Marg, A., & Vinkemeier, U. (2011). STAT1 signaling is not regulated by a phosphorylation-acetylation switch. Molecular and Cellular Biology, 31(14), https://doi.org/10.1128/MCB.05300-11

The treatment of cells with histone deacetylase inhibitors (HDACi) was reported to reveal the acetylation of STAT1 at lysine 410 and lysine 413 (O. H. Kra¨mer et al., Genes Dev. 20:473–485, 2006). STAT1 acetylation was proposed to regulate apoptosi... Read More about STAT1 signaling is not regulated by a phosphorylation-acetylation switch.

H-NS mediates the dissociation of a refractory protein–DNA complex during Tn10/IS10 transposition (2011)
Journal Article
Liu, D., Haniford, D. B., & Chalmers, R. (2011). H-NS mediates the dissociation of a refractory protein–DNA complex during Tn10/IS10 transposition. Nucleic Acids Research, 39(15), https://doi.org/10.1093/nar/gkr309

Tn10/IS10 transposition takes place in the context of a protein–DNA complex called a transpososome. During the reaction, the transpososome undergoes several conformational changes. The host proteins IHF and H-NS, which also are global regulators of g... Read More about H-NS mediates the dissociation of a refractory protein–DNA complex during Tn10/IS10 transposition.