Search Results - "Summerfield, G."

Examining the Uptake of Central Nervous System Drugs and Candidates across the Blood-Brain Barrier by Summerfield, Scott G, Zhang, Yanyan, Liu, Houfu

“…Assessing the equilibration of the unbound drug concentrations across the blood-brain barrier (Kp,uu) has progressively replaced the partition coefficient…”
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Treatment of hyperthyroidism with antithyroid drugs corrects mild neutropenia in Graves' disease by Aggarwal, N., Tee, S. A., Saqib, W., Fretwell, T., Summerfield, G.P., Razvi, S.

“…Summary Context Neutropenia secondary to antithyroid drug (ATD) therapy in Graves' disease (GD) is well recognized. However, the effect of hyperthyroidism,…”
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Central nervous system drug disposition: the relationship between in situ brain permeability and brain free fraction by Summerfield, Scott G, Read, Kevin, Begley, David J, Obradovic, Tanja, Hidalgo, Ismael J, Coggon, Sara, Lewis, Ann V, Porter, Rod A, Jeffrey, Phil

“…The dispositions of 50 marketed central nervous system (CNS) drugs into the brain have been examined in terms of their rat in situ (P) and in vitro apparent…”
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Prediction of brain:blood unbound concentration ratios in CNS drug discovery employing in silico and in vitro model systems by Liu, Houfu, Dong, Kelly, Zhang, Wandong, Summerfield, Scott G., Terstappen, Georg C.

“…[Display omitted] •Increase in Kp,uu,br/CLint translates into higher drug brain unbound exposure•The performance of current in silico Kp,uu,br models is…”
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Improving the in vitro prediction of in vivo central nervous system penetration: integrating permeability, P-glycoprotein efflux, and free fractions in blood and brain by Summerfield, Scott G, Stevens, Alexander J, Cutler, Leanne, del Carmen Osuna, Maria, Hammond, Beverley, Tang, Sac-Pham, Hersey, Ann, Spalding, David J, Jeffrey, Phil

“…This work examines the inter-relationship between the unbound drug fractions in blood and brain homogenate, passive membrane permeability, P-glycoprotein (Pgp)…”
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Combining PET Biodistribution and Equilibrium Dialysis Assays to Assess the Free Brain Concentration and BBB Transport of CNS Drugs by Gunn, Roger N, Summerfield, Scott G, Salinas, Cristian A, Read, Kevin D, Guo, Qi, Searle, Graham E, Parker, Christine A, Jeffrey, Phil, Laruelle, Marc

“…The passage of drugs in and out of the brain is controlled by the blood—brain barrier (BBB), typically, using either passive diffusion across a concentration…”
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Influence of Secondary Structure on the Fragmentation of Protonated Peptides by Tsaprailis, George, Nair, Hari, Somogyi, Árpád, Wysocki, Vicki H, Zhong, Wenqing, Futrell, Jean H, Summerfield, Scott G, Gaskell, Simon J

“…The influence of acid−base interactions on the gas-phase dissociation of a series of protonated peptides was investigated. Peptides containing both acidic…”
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Common variation at 12q24.13 (OAS3) influences chronic lymphocytic leukemia risk by Sava, G P, Speedy, H E, Di Bernardo, M C, Dyer, M J S, Holroyd, A, Sunter, N J, Marr, H, Mansouri, L, Deaglio, S, Karabon, L, Frydecka, I, Jamroziak, K, Woszczyk, D, Juliusson, G, Smedby, K E, Jayne, S, Majid, A, Wang, Y, Dearden, C, Hall, A G, Mainou-Fowler, T, Jackson, G H, Summerfield, G, Harris, R J, Pettitt, A R, Allsup, D J, Bailey, J R, Pratt, G, Pepper, C, Fegan, C, Rosenquist, R, Catovsky, D, Allan, J M, Houlston, R S

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Characterization of three diaminopyrimidines as potent and selective antagonists of P2X3 and P2X2/3 receptors with in vivo efficacy in a pain model by Ballini, E, Virginio, C, Medhurst, SJ, Summerfield, SG, Aldegheri, L, Buson, A, Carignani, C, Chen, YH, Giacometti, A, Lago, I, Powell, AJ, Jarolimek, W

“…BACKGROUND AND PURPOSE P2X3 and P2X2/3 receptors are highly localized on the peripheral and central pathways of nociceptive signal transmission. The discovery…”
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Free Drug Theory – No Longer Just a Hypothesis? by Summerfield, Scott G., Yates, James W. T., Fairman, David A.

“…The Free Drug Hypothesis is a well-established concept within the scientific lexicon pervading many areas of Drug Discovery and Development, and yet it is…”
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Inhibition of colonic motility and defecation by RS‐127445 suggests an involvement of the 5‐HT2B receptor in rodent large bowel physiology by Bassil, AK, Taylor, CM, Bolton, VJN, Gray, KM, Brown, JD, Cutler, L, Summerfield, SG, Bruton, G, Winchester, WJ, Lee, K, Sanger, GJ

“…Background:  5‐HT2B receptors are localized within the myenteric nervous system, but their functions on motor/sensory neurons are unclear. To explore the role…”
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Cutaneous features of intravascular lymphoma by Wahie, S., Dayala, S., Husain, A., Summerfield, G., Hervey, V., Langtry, J. A. A.

“…Summary Intravascular lymphoma (IVL) is a subset of extranodal non‐Hodgkin lymphoma, with an estimated incidence of < 1 case per million people. It is…”
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Perspectives on gender parity in bioanalysis: an interview with Scott Summerfield by Summerfield, Scott G

“…Having studied for a PhD and postdoctoral fellowship in proteomics Scott moved into the field of regulated Bioanalysis in 1997 when joining SmithKline Beecham…”
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The GSK Bioanalytical Hub model in bioanalysis: maximizing the synergies of co-locating various platforms in support of regulated and nonregulated study end points by Summerfield, Scott G, Tang, Huaping, Decman, Vilma, Abberley, Lee, Gunn, George, Yang, Eric

“…The term “bioanalytical” encompasses a much greater breadth of analytical deliverables than ever before. Circulating drug concentration data are complemented…”
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The cyclooxygenase-2 inhibitor GW406381X [2-(4-ethoxyphenyl)-3-[4-(methylsulfonyl)phenyl]-pyrazolo[1,5-b]pyridazine] is effective in animal models of neuropathic pain and central sensitization by Bingham, Sharon, Beswick, Paul J, Bountra, Chas, Brown, Terry, Campbell, Ian B, Chessell, Iain P, Clayton, Nick, Collins, Sue D, Davey, Philip T, Goodland, Helen, Gray, Norman, Haslam, Claudine, Hatcher, Jonathan P, Hunter, A Jacqueline, Lucas, Fiona, Murkitt, Graham, Naylor, Alan, Pickup, Elizabeth, Sargent, Becky, Summerfield, Scott G, Stevens, Alexander, Stratton, Sharon C, Wiseman, Joanne

“…The pathogenic form of the cyclooxygenase (COX) enzyme, COX-2, is also constitutively present in the spinal cord and has been implicated in chronic pain states…”
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Variant IRF4/MUM1 associates with CD38 status and treatment-free survival in chronic lymphocytic leukaemia by Allan, J M, Sunter, N J, Bailey, J R, Pettitt, A R, Harris, R J, Pepper, C, Fegan, C, Hall, A G, Deignan, L, Bacon, C M, Pointon, J C, Houlston, R S, Broderick, P, Mainou-Fowler, T, Jackson, G H, Summerfield, G, Evans, P A, Strefford, J C, Parker, A, Oscier, D, Pratt, G, Allsup, D J

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Integrating in Silico and in Vitro Approaches To Predict Drug Accessibility to the Central Nervous System by Zhang, Yan-Yan, Liu, Houfu, Summerfield, Scott G, Luscombe, Christopher N, Sahi, Jasminder

“…Estimation of uptake across the blood–brain barrier (BBB) is key to designing central nervous system (CNS) therapeutics. In silico approaches ranging from…”
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Investigation into the role of P2X(3)/P2X(2/3) receptors in neuropathic pain following chronic constriction injury in the rat: an electrophysiological study by Sharp, Caroline J, Reeve, Alison J, Collins, Sue D, Martindale, Jo C, Summerfield, Scott G, Sargent, Becky S, Bate, Simon T, Chessell, Iain P

“…1. Two P2X(3)/P2X(2/3) receptor antagonists with different potencies were profiled electrophysiologically in a rat model of nerve injury. 2. A-317491 has poor…”
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Rapid bioavailability and disposition protocol: A novel higher throughput approach to assess pharmacokinetics and steady-state tissue disstribution using fewer animals by Fu, Tingting, Gao, Ruina, Scott-Stevens, Paul, Chen, Yan, Zhang, Chalmers, Wang, Jianfei, Summerfield, Scott G., Damian, Valeriu, Sahi, Jasminder

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Incurred sample reanalysis at GSK: what have we learned? by Summerfield, Scott G, Barfield, Matthew, White, Stephen A

“…Outcomes of incurred sample reanalysis (ISR) studies have been reviewed from a decade of internally supported bioanalysis. From over 1000 bioanalytical…”
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