Search Results - "Astles, C"

Experimental investigation of short-term warming on arsenic flux from contaminated sediments of two well-oxygenated subarctic lakes by Astles, Brittany C, Chételat, John, Palmer, Michael J, Vermaire, Jesse C

“…Legacy arsenic (As) contamination from past mining operations remains an environmental concern in lakes of the Yellowknife area (Northwest Territories, Canada)…”
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Unique pharmacology of heteromeric α7β2 nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes by Zwart, Ruud, Strotton, Merrick, Ching, Jennifer, Astles, Peter C., Sher, Emanuele

“…α7β2 is a novel type of nicotinic acetylcholine receptor shown to be uniquely expressed in cholinergic neurons of the basal forebrain and in hippocampal…”
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Selective Cannabinoid Receptor Type 2 (CB2) Agonists: Optimization of a Series of Purines Leading to the Identification of a Clinical Candidate for the Treatment of Osteoarthritic Pain by Hollinshead, Sean P, Tidwell, Michael W, Palmer, John, Guidetti, Rossella, Sanderson, Adam, Johnson, Michael P, Chambers, Mark G, Oskins, Jennifer, Stratford, Robert, Astles, Peter C

“…A focused screening strategy identified thienopyrimidine 12 as a cannabinoid receptor type 2 agonist (hCB2) with moderate selectivity over the hCB1 receptor…”
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Discovery and optimization of novel purines as potent and selective CB2 agonists by Hollinshead, Sean P., Astles, Peter C., Chambers, Mark G., Johnson, Michael P., Palmer, John, Tidwell, Michael W.

“…A focused screening strategy identified thienopyrimidine 1 as a hCB2 cannabinoid receptor agonist with moderate selectivity over the hCB1 receptor. This…”
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Managing complex respiratory patients in the community: an evaluation of a pilot integrated respiratory care service by Gillett, K, Lippiett, K, Astles, C, Longstaff, J, Orlando, R, Lin, S X, Powell, A, Roberts, C, Chauhan, A J, Thomas, M, Wilkinson, T M

“…IntroductionIn the UK, there is significant variation in respiratory care and outcomes. An integrated approach to the management of high-risk respiratory…”
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Discovery of a Series of Orally Bioavailable Androgen Receptor Degraders for the Treatment of Prostate Cancer by Bagal, Sharan K., Astles, Peter C., Diène, Coura, Argyrou, Argyrides, Crafter, Claire, Cassar, Doyle J., Fallan, Charlene, Hock, Andreas, Jones, Thomas, Moreau, Kevin, Lamont, Gillian M., Lamont, Scott, Michaloglou, Chrysiis, Packer, Martin J., Pike, Andy, Ramos-Montoya, Antonio, Scott, James S., Shaw, Joseph, Shologu, Ziyanda

“…Androgen receptor (AR) signaling plays a key role in the progression of prostate cancer. This study describes the discovery and optimization of a novel series…”
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Identification of Novel Potent NSD2-PWWP1 Ligands Using Structure-Based Design and Computational Approaches by Carlino, Luca, Astles, Peter C., Ackroyd, Bryony, Ahmed, Afshan, Chan, Christina, Collie, Gavin W., Dale, Ian L., O’Donovan, Daniel H., Fawcett, Caroline, di Fruscia, Paolo, Gohlke, Andrea, Guo, Xiaoxiao, Hao-Ru Hsu, Jessie, Kaplan, Bethany, Milbradt, Alexander G., Northall, Sarah, Petrović, Dušan, Rivers, Emma L., Underwood, Elizabeth, Webb, Alice

“…Dysregulation of histone methyl transferase nuclear receptor-binding SET domain 2 (NSD2) has been implicated in several hematological and solid malignancies…”
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An Anomaly in Intercept Time for Short Range Ballistic Re-Entry Vehicles by Nguyen, P. Bao U., Amyot-Bourgeois, Maude, Astles, Brittany C.

“…This paper documents an anomaly in intercept time of a ballistic re-entry vehicle (RV) by a ballistic interceptor. Intuitively, it is expected that as soon as…”
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A Practical Synthesis of (±)-α-Isosparteine from a Tetraoxobispidine Core by Blakemore, Paul R, Kilner, Colin, Norcross, Neil R, Astles, Peter C

“…The title alkaloid was synthesized in racemic form from 3,7-diallyl-2,4,6,8-tetraoxo-3,7-diazabicyclo[3.3.1]nonane (7) by a regioselective diallylation…”
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The SAR development of substituted purine derivatives as selective CB2 agonists for the treatment of chronic pain by Guidetti, Rossella, Astles, Peter C, Sanderson, Adam J, Hollinshead, Sean P, Johnson, Michael P, Chambers, Mark G

“…Osteoarthritis (OA) and the associated joint pain are highly prevalent and a leading cause of disability. We have previously reported the identification of a…”
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Selective ETA Antagonists. 5. Discovery and Structure−Activity Relationships of Phenoxyphenylacetic Acid Derivatives by Astles, Peter C, Brown, Thomas J, Halley, Frank, Handscombe, Caroline M, Harris, Neil V, Majid, Tahir N, McCarthy, Clive, McLay, Iain M, Morley, Andrew, Porter, Barry, Roach, Alan G, Sargent, Carol, Smith, Christopher, Walsh, Roger J. A

“…The fifth paper in this series describes the culmination of our investigations into the development of a potent and selective ETA receptor antagonist for the…”
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Diamine containing VLA-4 antagonists by Astles, Peter C., Harris, Neil V., Morley, Andrew D.

“…Design and synthesis of a library as potential VLA-4 antagonists has been accomplished, based around a proposed pharmacophoric model. Compounds possessing…”
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Total synthesis of furanocembranolides. 3. A concise convergent route to acerosolide by Paquette, Leo A, Astles, Peter C

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Selective Endothelin A Receptor Antagonists. 3. Discovery and Structure−Activity Relationships of a Series of 4-Phenoxybutanoic Acid Derivatives by Astles, Peter C, Brealey, Clive, Brown, Thomas J, Facchini, Vincenzo, Handscombe, Caroline, Harris, Neil V, McCarthy, Clive, McLay, Iain M, Porter, Barry, Roach, Alan G, Sargent, Carol, Smith, Christopher, Walsh, Roger J. A

“…The third in this series of papers describes our further progress into the discovery of a potent and selective endothelin A (ETA) receptor antagonist for the…”
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Total synthesis of furanocembranolides. 2. Macrocyclization studies culminating in the synthesis of a dihydropseudopterolide and gorgiacerone. Related furanocembranolide interconversions by Rayner, Christopher M, Astles, Peter C, Paquette, Leo A

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Total Synthesis of (±)-α-Isosparteine, (±)-β-Isosparteine, and (±)-Sparteine from a Common Tetraoxobispidine Intermediate by Norcross, Neil R, Melbardis, John P, Solera, Margarita Ferris, Sephton, Mark A, Kilner, Colin, Zakharov, Lev N, Astles, Peter C, Warriner, Stuart L, Blakemore, Paul R

“…The three title alkaloids were separately prepared in stereocontrolled fashion from a common tetraoxobispidine precursor,…”
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A Stereocontrolled Synthesis of (±)-β-Isosparteine by R. Blakemore, Paul, R. Norcross, Neil, L. Warriner, Stuart, C. Astles, Peter

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Selective Endothelin A Receptor Antagonists. 4. Discovery and Structure−Activity Relationships of Stilbene Acid and Alcohol Derivatives by Astles, Peter C, Brown, Thomas J, Halley, Frank, Handscombe, Caroline M, Harris, Neil V, McCarthy, Clive, McLay, Iain M, Lockey, Peter, Majid, Tahir, Porter, Barry, Roach, Alan G, Smith, Christopher, Walsh, Roger

“…This publication describes the synthesis and optimization of a novel series of stilbene endothelin antagonists. Analysis of the SAR established for previous…”
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Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) Inhibitors. 2. 2-(1,3-Dioxan-2-yl)-4,5-diphenyl-1H-imidazoles as Potent Inhibitors of ACAT by Astles, Peter C, Ashton, Michael J, Bridge, Andrew W, Harris, Neil V, Hart, Terrance W, Parrott, David P, Porter, Barry, Riddell, David, Smith, Christopher, Williams, Robert J

“…The second in this series of papers concerns our further investigations into the search for a potent bioavailable acyl-CoA:cholesterol O-acyltransferase (ACAT)…”
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Selective endothelin A receptor ligands. 1. Discovery and structure-activity of 2,4-disubstituted benzoic acid derivatives by Astles, PC, Brown, TJ, Handscombe, CM, Harper, MF, Harris, NV, Lewis, RA, Lockey, PM, McCarthy, C, McLay, IM, Porter, B, Roach, AG, Smith, C, Walsh, RJA

“…This paper describes the discovery of a new non-peptide endothelin A (ET A) selective ligand, 2,4-dibenzyloxybenzoic acid 3, which inhibits the binding of […”
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