Search Results - "Day, H E"

Is specialization an evolutionary dead end? Testing for differences in speciation, extinction and trait transition rates across diverse phylogenies of specialists and generalists by Day, E. H., Hua, X., Bromham, L.

“…Specialization has often been claimed to be an evolutionary dead end, with specialist lineages having a reduced capacity to persist or diversify. In a…”
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Hypothalamic Pituitary Adrenal Axis Responses to Low-Intensity Stressors are Reduced After Voluntary Wheel Running in Rats by Campeau, S., Nyhuis, T. J., Sasse, S. K., Kryskow, E. M., Herlihy, L., Masini, C. V., Babb, J. A., Greenwood, B. N., Fleshner, M., Day, H. E. W.

“…Regular physical exercise is beneficial for both physical and mental health. By contrast, stress is associated with deleterious effects on health and there is…”
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Expression of fibroblast growth factor-2 and brain-derived neurotrophic factor mRNA in the medial prefrontal cortex and hippocampus after uncontrollable or controllable stress by Bland, S.T, Tamlyn, J.P, Barrientos, R.M, Greenwood, B.N, Watkins, L.R, Campeau, S, Day, H.E, Maier, S.F

“…Abstract Neurotrophic factors, including basic fibroblast growth factor (FGF-2) and brain-derived neurotrophic factor (BDNF) are known to be affected by…”
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Acute Glucocorticoid Pretreatment Suppresses Stress-Induced Hypothalamic-Pituitary-Adrenal Axis Hormone Secretion and Expression of Corticotropin-Releasing Hormone hnRNA but Does Not Affect c-fos mRNA or Fos Protein Expression in the Paraventricular Nucleus of the Hypothalamus by Ginsberg, A. B., Campeau, S., Day, H. E., Spencer, R. L.

“…Corticosterone regulates both basal and stress‐induced hypothalamic‐pituitary‐adrenal (HPA) axis activity in a negative‐feedback fashion. However, the cellular…”
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Evidence for a lack of phasic inhibitory properties of habituated stressors on HPA axis responses in rats by Masini, C.V, Day, H.E.W, Gray, T, Crema, L.M, Nyhuis, T.J, Babb, J.A, Campeau, S

“…Abstract This experiment tested the hypothesis that habituation to repeated stressor exposures is produced by phasic inhibitory influence on the neural…”
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Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X‑Linked Inhibitor of Apoptosis Protein (XIAP) by Tamanini, Emiliano, Buck, Ildiko M, Chessari, Gianni, Chiarparin, Elisabetta, Day, James E. H, Frederickson, Martyn, Griffiths-Jones, Charlotte M, Hearn, Keisha, Heightman, Tom D, Iqbal, Aman, Johnson, Christopher N, Lewis, Edward J, Martins, Vanessa, Peakman, Torren, Reader, Michael, Rich, Sharna J, Ward, George A, Williams, Pamela A, Wilsher, Nicola E

“…XIAP and cIAP1 are members of the inhibitor of apoptosis protein (IAP) family and are key regulators of anti-apoptotic and pro-survival signaling pathways…”
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Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP by Chessari, Gianni, Buck, Ildiko M, Day, James E. H, Day, Philip J, Iqbal, Aman, Johnson, Christopher N, Lewis, Edward J, Martins, Vanessa, Miller, Darcey, Reader, Michael, Rees, David C, Rich, Sharna J, Tamanini, Emiliano, Vitorino, Marc, Ward, George A, Williams, Pamela A, Williams, Glyn, Wilsher, Nicola E, Woolford, Alison J.-A

“…Inhibitor of apoptosis proteins (IAPs) are important regulators of apoptosis and pro-survival signaling pathways whose deregulation is often associated with…”
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Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2 by Heightman, Tom D, Berdini, Valerio, Braithwaite, Hannah, Buck, Ildiko M, Cassidy, Megan, Castro, Juan, Courtin, Aurélie, Day, James E. H, East, Charlotte, Fazal, Lynsey, Graham, Brent, Griffiths-Jones, Charlotte M, Lyons, John F, Martins, Vanessa, Muench, Sandra, Munck, Joanne M, Norton, David, O’Reilly, Marc, Palmer, Nick, Pathuri, Puja, Reader, Michael, Rees, David C, Rich, Sharna J, Richardson, Caroline, Saini, Harpreet, Thompson, Neil T, Wallis, Nicola G, Walton, Hugh, Wilsher, Nicola E, Woolford, Alison J.-A, Cooke, Michael, Cousin, David, Onions, Stuart, Shannon, Jonathan, Watts, John, Murray, Christopher W

“…Aberrant activation of the MAPK pathway drives cell proliferation in multiple cancers. Inhibitors of BRAF and MEK kinases are approved for the treatment of…”
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Sex differences in activated corticotropin-releasing factor neurons within stress-related neurocircuitry and hypothalamic–pituitary–adrenocortical axis hormones following restraint in rats by Babb, J.A, Masini, C.V, Day, H.E.W, Campeau, S

“…Highlights ► Similar qualitative stress-induced neurocircuitry activation in male and female brain. ► Females have higher activation of PVN, BST, and MPOA…”
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Remote CB1 receptor antagonist administration reveals multiple sites of tonic and phasic endocannabinoid neuroendocrine regulation by Newsom, R.J., Garcia, R.J., Stafford, J., Osterlund, C., O’Neill, C.E., Day, H.E.W., Campeau, S.

“…•This study assessed the contributions of CB1 receptors in the modulation of basal and stress-induced neural and HPA axis activities.•CB1R antagonism induced…”
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Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors by Murray, Christopher W, Berdini, Valerio, Buck, Ildiko M, Carr, Maria E, Cleasby, Anne, Coyle, Joseph E, Curry, Jayne E, Day, James E. H, Day, Phillip J, Hearn, Keisha, Iqbal, Aman, Lee, Lydia Y. W, Martins, Vanessa, Mortenson, Paul N, Munck, Joanne M, Page, Lee W, Patel, Sahil, Roomans, Susan, Smith, Kirsten, Tamanini, Emiliano, Saxty, Gordon

“…The DDR1 and DDR2 receptor tyrosine kinases are activated by extracellular collagen and have been implicated in a number of human diseases including cancer. We…”
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Targeting the Hsp90 Chaperone: Synthesis of Novel Resorcylic Acid Macrolactone Inhibitors of Hsp90 by Day, James E. H., Sharp, Swee Y., Rowlands, Martin G., Aherne, Wynne, Workman, Paul, Moody, Christopher J.

“…A series of benzo‐macrolactones has been prepared by chemical synthesis, and evaluated as inhibitors of heat shock protein 90 (Hsp90), an emerging attractive…”
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Cannabinoid receptor type 1 antagonism significantly modulates basal and loud noise induced neural and hypothalamic-pituitary-adrenal axis responses in male Sprague–Dawley rats by Newsom, R.J, Osterlund, C, Masini, C.V, Day, H.E, Spencer, R.L, Campeau, S

“…Abstract Altered regulation of the hypothalamic-pituitary-adrenal (HPA) axis is associated with stress-induced changes in cognitive, emotional, and physical…”
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Targeting the Hsp90 Molecular Chaperone with Novel Macrolactams. Synthesis, Structural, Binding, and Cellular Studies by Day, James E. H, Sharp, Swee Y, Rowlands, Martin G, Aherne, Wynne, Hayes, Angela, Raynaud, Florence I, Lewis, William, Roe, S. Mark, Prodromou, Chrisostomos, Pearl, Laurence H, Workman, Paul, Moody, Christopher J

“…A series of resorcylic acid macrolactams, nitrogen analogues of the naturally occurring macrolactone radicicol, have been prepared by chemical synthesis and…”
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Inhibition of Hsp90 with Resorcylic Acid Macrolactones: Synthesis and Binding Studies by Day, James E. H., Sharp, Swee Y., Rowlands, Martin G., Aherne, Wynne, Lewis, William, Roe, S. Mark, Prodromou, Chrisostomos, Pearl, Laurence H., Workman, Paul, Moody, Christopher J.

“…A series of resorcylic acid macrolactones, analogues of the natural product radicicol has been prepared by chemical synthesis, and evaluated as inhibitors of…”
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Acute and chronic effects of ferret odor exposure in Sprague–Dawley rats by Campeau, S., Nyhuis, T.J., Sasse, S.K., Day, H.E.W., Masini, C.V.

“…This manuscript describes several behavioral and functional studies evaluating the capacity of ferret odors to elicit a number of acute and long-term responses…”
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Anatomy of an Endogenous Antagonist: Relationship between Agouti-Related Protein and Proopiomelanocortin in Brain by Bagnol, Didier, Lu, Xin-Yun, Kaelin, Christopher B, Day, Heidi E. W, Ollmann, Michael, Gantz, Ira, Akil, Huda, Barsh, Gregory S, Watson, Stanley J

“…Agouti-related protein (AGRP) is a recently discovered orexigenic neuropeptide that inhibits the binding and action of alpha-melanocyte-stimulating hormone…”
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Fragment-Based Discovery of Allosteric Inhibitors of SH2 Domain-Containing Protein Tyrosine Phosphatase‑2 (SHP2) by Day, James E. H., Berdini, Valerio, Castro, Joan, Chessari, Gianni, Davies, Thomas G., Day, Philip J., St. Denis, Jeffrey D., Fujiwara, Hideto, Fukaya, Satoshi, Hamlett, Christopher C. F., Hearn, Keisha, Hiscock, Steven D., Holvey, Rhian S., Ito, Satoru, Kandola, Navrohit, Kodama, Yasuo, Liebeschuetz, John W., Martins, Vanessa, Matsuo, Kenichi, Mortenson, Paul N., Muench, Sandra, Nakatsuru, Yoko, Ochiiwa, Hiroaki, Palmer, Nicholas, Peakman, Torren, Price, Amanda, Reader, Michael, Rees, David C., Rich, Sharna J., Shah, Alpesh, Shibata, Yoshihiro, Smyth, Tomoko, Twigg, David G., Wallis, Nicola G., Williams, Glyn, Wilsher, Nicola E., Woodhead, Andrew, Shimamura, Tadashi, Johnson, Christopher N.

“…The ubiquitously expressed protein tyrosine phosphatase SHP2 is required for signaling downstream of receptor tyrosine kinases (RTKs) and plays a role in…”
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A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660) by Johnson, Christopher N, Ahn, Jong Sook, Buck, Ildiko M, Chiarparin, Elisabetta, Day, James E H, Hopkins, Anna, Howard, Steven, Lewis, Edward J, Martins, Vanessa, Millemaggi, Alessia, Munck, Joanne M, Page, Lee W, Peakman, Torren, Reader, Michael, Rich, Sharna J, Saxty, Gordon, Smyth, Tomoko, Thompson, Neil T, Ward, George A, Williams, Pamela A, Wilsher, Nicola E, Chessari, Gianni

“…Inhibitor of apoptosis proteins (IAPs) are promising anticancer targets, given their roles in the evasion of apoptosis. Several peptidomimetic IAP antagonists,…”
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Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2 by Heightman, Tom D, Berdini, Valerio, Bevan, Luke, Buck, Ildiko M, Carr, Maria G, Courtin, Aurélie, Coyle, Joseph E, Day, James E H, East, Charlotte, Fazal, Lynsey, Griffiths-Jones, Charlotte M, Howard, Steven, Kucia-Tran, Justyna, Martins, Vanessa, Muench, Sandra, Munck, Joanne M, Norton, David, O'Reilly, Marc, Palmer, Nicholas, Pathuri, Puja, Peakman, Torren M, Reader, Michael, Rees, David C, Rich, Sharna J, Shah, Alpesh, Wallis, Nicola G, Walton, Hugh, Wilsher, Nicola E, Woolford, Alison J-A, Cooke, Michael, Cousin, David, Onions, Stuart, Shannon, Jonathan, Watts, John, Murray, Christopher W

“…Aberrant activation of the mitogen-activated protein kinase pathway frequently drives tumor growth, and the ERK1/2 kinases are positioned at a key node in this…”
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