Search Results - "Neduvelil, Joseph G."

Photoactivated γ-secretase inhibitors directed to the active site covalently label presenilin 1 by Gardell, Stephen J, Li, Yue-Ming, Xu, Min, Lai, Ming-Tain, Huang, Qian, Castro, José L, DiMuzio-Mower, Jillian, Harrison, Timothy, Lellis, Colin, Nadin, Alan, Neduvelil, Joseph G, Register, R. Bruce, Sardana, Mohinder K, Shearman, Mark S, Smith, Adrian L, Shi, Xiao-Ping, Yin, Kuo-Chang, Shafer, Jules A

“…Cleavage of amyloid precursor protein (APP) by the β- and γ-secretases generates the amino and carboxy termini, respectively, of the Aβ amyloidogenic peptides…”
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HOLE: A program for the analysis of the pore dimensions of ion channel structural models by Smart, Oliver S., Neduvelil, Joseph G., Wang, Xiaonan, Wallace, B.A., Sansom, Mark S.P.

“…A method (HOLE) that allows the analysis of the dimensions of the pore running through a structural model of an ion channel is presented. The algorithm uses a…”
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A novel series of potent γ-secretase inhibitors based on a benzobicyclo[4.2.1]nonane core by Lewis, Stephen J., Smith, Adrian L., Neduvelil, Joseph G., Stevenson, Graeme I., Lindon, Matthew J., Jones, A. Brian, Shearman, Mark S., Beher, Dirk, Clarke, Earl, Best, Jonathan D., Peachey, James E., Harrison, Timothy, Castro, J. Luis

“…[Display omitted] A new series of γ-secretase inhibitors was developed from an in-house screening hit based on a benzobicyclo[4.2.1]nonane core. Lead…”
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γ-Secretase: characterization and implication for Alzheimer disease therapy by MIN XU, LAI, Ming-Tain, GARDELL, Stephen J, LI, Yue-Ming, QIAN HUANG, DIMUZIO-MOWER, Jillian, CASTRO, José L, HARRISON, Timothy, NADIN, Alan, NEDUVELIL, Joseph G, SHEARMAN, Mark S, SHAFER, Jules A

“…gamma-Secretase is a membrane-bound protease that cleaves within the transmembrane region of amyloid precursor protein to generate the C-termini of the Abeta…”
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High-Affinity and Potent, Water-Soluble 5-Amino-1,4-benzodiazepine CCKB/Gastrin Receptor Antagonists Containing a Cationic Solubilizing Group by Showell, Graham A, Bourrain, Sylvie, Neduvelil, Joseph G, Fletcher, Stephen R, Baker, Raymond, Watt, Alan P, Fletcher, Alan E, Freedman, Stephen B, Kemp, John A

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2-Aryl tryptamines : Selective high-affinity antagonists for the h5-HT2A receptor by STEVENSON, Graeme I, SMITH, Adrian L, LEWIS, Stephen, MICHIE, Stephen G, NEDUVELIL, Joseph G, PATEL, Smita, MARWOOD, Rosemarie, PATEL, Shil, CASTRO, José L

“…A series of 2-aryl tryptamines have been identified as high-affinity h5-HT2A antagonists. Structure-activity relationship studies have shown that h5-HT2A…”
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A stereocontrolled synthesis of 2 R -benzyl-5 S - tert -butoxycarbonylamino-4 R -( tert -butyldimethylsilanyloxy)-6-phenyl-hexanoic acid (Phe–Phe hydroxyethylene dipeptide isostere) by Nadin, Alan, Sánchez López, José M, Neduvelil, Joseph G, Thomas, Steven R

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Substituted pyrazoles as novel selective ligands for the human dopamine D4 receptor by Bourrain, S, Collins, I, Neduvelil, J G, Rowley, M, Leeson, P D, Patel, S, Emms, F, Marwood, R, Chapman, K L, Fletcher, A E, Showell, G A

“…Two novel series of 3-(heterocyclylmethyl)pyrazoles have been synthesised and evaluated as ligands for the human dopamine D4 receptor. Compounds in series I…”
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Substituted pyrazoles as novel selective ligands for the human dopamine D 4 receptor by Bourrain, Sylvie, Collins, Ian, Neduvelil, Joseph G., Rowley, Michael, Leeson, Paul D., Patel, Smita, Patel, Shil, Emms, Frances, Marwood, Rosemarie, Chapman, Kerry L., Fletcher, Alan E., Showell, Graham A.

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4-Hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1 H-indol-3-yl)propyl]piperidines: Selective h5-HT 1D agonists for the treatment of migraine by Bourrain, Sylvie, Neduvelil, Joseph G., Beer, Margaret S., Stanton, Josephine A., Showell, Graham A., MacLeod, Angus M.

“…A series of 4-hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1 H-indol-3-yl)propyl] piperidines was investigated as potential selective h5-HT 1D agonists for the…”
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2-Aryl tryptamines: selective high-affinity antagonists for the h5-HT 2A receptor by Stevenson, Graeme I, Smith, Adrian L, Lewis, Stephen, Michie, Stephen G, Neduvelil, Joseph G, Patel, Smita, Marwood, Rosemarie, Patel, Shil, Castro, José L

“…A series of 2-aryl tryptamines have been identified as high-affinity h5-HT 2A antagonists. Structure–activity relationship studies have shown that h5-HT 2A…”
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4-Hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl]piperidines : Selective h5-HT1D agonists for the treatment of migraine by BOURRAIN, S, NEDUVELIL, J. G, BEER, M. S, STANTON, J. A, SHOWELL, G. A, MACLEOD, A. M

“…A series of 4-hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl] piperidines was investigated as potential selective h5-HT1D agonists for the treatment…”
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C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists by Showell, Graham A., Bourrain, Sylvie, Fletcher, Stephen R., Neduvelil, Joseph G., Fletcher, Alan E., Freedman, Stephen B., Patel, Smita, Smith, Alison J., Marshall, George R., Graham, Michael I., Sohal, Bindi, Matassa, Victor G.

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Biological properties of the benzodiazepine amidine derivative L-740,093, a cholecystokinin-B/gastrin receptor antagonist with high affinity in vitro and high potency in vivo by Patel, S, Smith, A J, Chapman, K L, Fletcher, A E, Kemp, J A, Marshall, G R, Hargreaves, R J, Ryecroft, W, Iversen, L L, Iversen, S D

“…A novel series of 5-amino-1,4-benzodiazepin-2-one derivatives (amidines), which contain a cationic solubilizing group and which are antagonists for the…”
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C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCK B/gastrin receptor antagonists by Showell, Graham A., Bourrain, Sylvie, Fletcher, Stephen R., Neduvelil, Joseph G., Fletcher, Alan E., Freedman, Stephen B., Patel, Smita, Smith, Alison J., Marshall, George R., Graham, Michael I., Sohal, Bindi, Matassa, Victor G.

“…A novel series of potent, water-soluble benzodiazepine based CCK B/gastrin antagonists has been prepared which incorporate an N-methylpiperazine group at the…”
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