Intra- or Intercomplex Binding to the γ-Secretase Enzyme: A MODEL TO DIFFERENTIATE INHIBITOR CLASSES
Clarke, Earl E, Churcher, Ian, Ellis, Semantha, Wrigley, Jonathan D.J, Lewis, Huw D, Harrison, Timothy, Shearman, Mark S, Beher, Dirk
Published in The Journal of biological chemistry (20.10.2006)
Published in The Journal of biological chemistry (20.10.2006)
Get full text
Journal Article
Selected non-steroidal anti-inflammatory drugs and their derivatives target gamma-secretase at a novel site. Evidence for an allosteric mechanism
Beher, Dirk, Clarke, Earl E, Wrigley, Jonathan D J, Martin, Agnes C L, Nadin, Alan, Churcher, Ian, Shearman, Mark S
Published in The Journal of biological chemistry (15.10.2004)
Published in The Journal of biological chemistry (15.10.2004)
Get full text
Journal Article
Generation of C‐terminally truncated amyloid‐β peptides is dependent on γ‐secretase activity
Beher, Dirk, Wrigley, Jonathan D. J., Owens, Andrew P., Shearman, Mark S.
Published in Journal of neurochemistry (01.08.2002)
Published in Journal of neurochemistry (01.08.2002)
Get full text
Journal Article
4-Substituted cyclohexyl sulfones as potent, orally active γ-secretase inhibitors
Churcher, Ian, Beher, Dirk, Best, Jonathan D., Castro, José L., Clarke, Earl E., Gentry, Amy, Harrison, Timothy, Hitzel, Laure, Kay, Euan, Kerrad, Sonia, Lewis, Huw D., Morentin-Gutierrez, Pablo, Mortishire-Smith, Russell, Oakley, Paul J., Reilly, Michael, Shaw, Duncan E., Shearman, Mark S., Teall, Martin R., Williams, Susie, Wrigley, Jonathan D.J.
Published in Bioorganic & medicinal chemistry letters (15.01.2006)
Published in Bioorganic & medicinal chemistry letters (15.01.2006)
Get full text
Journal Article
Novel Orally Bioavailable γ-Secretase Inhibitors with Excellent in Vivo Activity
Keown, Linda E, Collins, Ian, Cooper, Laura C, Harrison, Timothy, Madin, Andrew, Mistry, Jayesh, Reilly, Michael, Shaimi, Mohamed, Welch, Christopher J, Clarke, Earl E, Lewis, Huw D, Wrigley, Jonathan D. J, Best, Jonathan D, Murray, Fraser, Shearman, Mark S
Published in Journal of medicinal chemistry (11.06.2009)
Published in Journal of medicinal chemistry (11.06.2009)
Get full text
Journal Article
Pharmacological knock-down of the presenilin 1 heterodimer by a novel gamma -secretase inhibitor: implications for presenilin biology
Beher, D, Wrigley, J D, Nadin, A, Evin, G, Masters, C L, Harrison, T, Castro, J L, Shearman, M S
Published in The Journal of biological chemistry (30.11.2001)
Published in The Journal of biological chemistry (30.11.2001)
Get full text
Journal Article
In Vitro Characterization of the Presenilin-Dependent γ-Secretase Complex Using a Novel Affinity Ligand
Beher, Dirk, Fricker, Michael, Nadin, Alan, Clarke, Earl E, Wrigley, Jonathan D. J, Li, Yue-Ming, Culvenor, Janetta G, Masters, Colin L, Harrison, Timothy, Shearman, Mark S
Published in Biochemistry (Easton) (15.07.2003)
Published in Biochemistry (Easton) (15.07.2003)
Get full text
Journal Article
Design and Synthesis of Highly Potent Benzodiazepine γ-Secretase Inhibitors: Preparation of (2S,3R)-3-(3,4- Difluorophenyl)-2-(4-fluorophenyl)-4- hydroxy-N-((3S)-1-methyl-2-oxo-5- phenyl-2,3-dihydro-1H-benzo[e][1,4]- diazepin-3-yl)butyramide by Use of an Asymmetric Ireland−Claisen Rearrangement
Churcher, Ian, Williams, Susie, Kerrad, Sonia, Harrison, Timothy, Castro, José L, Shearman, Mark S, Lewis, Huw D, Clarke, Earl E, Wrigley, Jonathan D. J, Beher, Dirk, Tang, Yui S, Liu, Wensheng
Published in Journal of medicinal chemistry (05.06.2003)
Published in Journal of medicinal chemistry (05.06.2003)
Get full text
Journal Article
Functional Overexpression of γ-Secretase Reveals Protease-independent Trafficking Functions and a Critical Role of Lipids for Protease Activity
Wrigley, Jonathan D.J., Schurov, Irina, Nunn, Emma J., Martin, Agnes C.L., Clarke, Earl E., Ellis, Semantha, Bonnert, Timothy P., Shearman, Mark S., Beher, Dirk
Published in The Journal of biological chemistry (01.04.2005)
Published in The Journal of biological chemistry (01.04.2005)
Get full text
Journal Article
Peripherin/rds influences membrane vesicle morphology. Implications for retinopathies
Wrigley, J D, Ahmed, T, Nevett, C L, Findlay, J B
Published in The Journal of biological chemistry (05.05.2000)
Published in The Journal of biological chemistry (05.05.2000)
Get full text
Journal Article
Intra- or Intercomplex Binding to the γ-Secretase Enzyme
Clarke, Earl E., Churcher, Ian, Ellis, Semantha, Wrigley, Jonathan D.J., Lewis, Huw D., Harrison, Timothy, Shearman, Mark S., Beher, Dirk
Published in The Journal of biological chemistry (20.10.2006)
Published in The Journal of biological chemistry (20.10.2006)
Get full text
Journal Article
The geminal dimethyl analogue of Flurbiprofen as a novel Aβ42 inhibitor and potential Alzheimer's disease modifying agent
STOCK, Nicholas, MUNOZ, Benito, ST-JACQUES, René, PRASIT, Peppi, WRIGLEY, Jonathan D. J, SHEARMAN, Mark S, BEHER, Dirk, PEACHEY, James, WILLIAMSON, Toni L, BAIN, Gretchen, WEICHAO CHEN, XIAOHUI JIANG
Published in Bioorganic & medicinal chemistry letters (15.04.2006)
Published in Bioorganic & medicinal chemistry letters (15.04.2006)
Get full text
Journal Article
A new series of potent benzodiazepine γ-secretase inhibitors
Churcher, Ian, Ashton, Kate, Butcher, John W., Clarke, Earl E., Harrison, Timothy, Lewis, Huw D., Owens, Andrew P., Teall, Martin R., Williams, Susie, Wrigley, Jonathan D.J.
Published in Bioorganic & medicinal chemistry letters (20.01.2003)
Published in Bioorganic & medicinal chemistry letters (20.01.2003)
Get full text
Journal Article
3-Substituted gem-cyclohexane sulfone based γ-secretase inhibitors for Alzheimer’s disease: Conformational analysis and biological activity
Jelley, Richard A., Elliott, Jason, Gibson, Karl R., Harrison, Timothy, Beher, Dirk, Clarke, Earl E., Lewis, Huw D., Shearman, Mark, Wrigley, Jonathan D.J.
Published in Bioorganic & medicinal chemistry letters (15.07.2006)
Published in Bioorganic & medicinal chemistry letters (15.07.2006)
Get full text
Journal Article
High affinity, bioavailable 3-Amino-1,4-benzodiazepine-Based γ-Secretase inhibitors
Owens, Andrew P., Nadin, Alan, Talbot, Adam C., Clarke, Earl E., Harrison, Timothy, Lewis, Huw D., Reilly, Michael, Wrigley, Jonathan D.J., Castro, José L.
Published in Bioorganic & medicinal chemistry letters (17.11.2003)
Published in Bioorganic & medicinal chemistry letters (17.11.2003)
Get full text
Journal Article
Conserved residues within the putative active site of γ‐secretase differentially influence enzyme activity and inhibitor binding
Wrigley, Jonathan D. J., Nunn, Emma J., Nyabi, Omar, Clarke, Earl E., Hunt, Peter, Nadin, Alan, De Strooper, Bart, Shearman, Mark S., Beher, Dirk
Published in Journal of neurochemistry (01.09.2004)
Published in Journal of neurochemistry (01.09.2004)
Get full text
Journal Article
Selected Non-steroidal Anti-inflammatory Drugs and Their Derivatives Target γ-Secretase at a Novel Site
Beher, Dirk, Clarke, Earl E., Wrigley, Jonathan D.J., Martin, Agnes C.L., Nadin, Alan, Churcher, Ian, Shearman, Mark S.
Published in The Journal of biological chemistry (01.10.2004)
Published in The Journal of biological chemistry (01.10.2004)
Get full text
Journal Article
S2-03-02: Mechanistic differences in targeting γ-secretase with inhibitors
Beher, Dirk, Clarke, Earl E., Wrigley, Jonathan D.J., Churcher, Ian, Ellis, Semantha, Lewis, Huw D., Harrison, Timothy, Shearman, Mark S.
Published in Alzheimer's & dementia (01.07.2006)
Published in Alzheimer's & dementia (01.07.2006)
Get full text
Journal Article
Methionine-rich repeat proteins: a family of membrane-associated proteins which contain unusual repeat regions
Weiss, Jamie L., Evans, Nicholas A., Ahmed, Tanweer, Wrigley, Jonathan D.J., Khan, Shukria, Wright, Charles, Keen, Jeffrey N., Holzenburg, Andreas, Findlay, John B.C.
Published in Biochimica et biophysica acta (01.03.2005)
Published in Biochimica et biophysica acta (01.03.2005)
Get full text
Journal Article
The geminal dimethyl analogue of Flurbiprofen as a novel Aβ 42 inhibitor and potential Alzheimer’s disease modifying agent
Stock, Nicholas, Munoz, Benito, Wrigley, Jonathan D.J., Shearman, Mark S., Beher, Dirk, Peachey, James, Williamson, Toni L., Bain, Gretchen, Chen, Weichao, Jiang, Xiaohui, St-Jacques, René, Prasit, Peppi
Published in Bioorganic & medicinal chemistry letters (2006)
Published in Bioorganic & medicinal chemistry letters (2006)
Get full text
Journal Article