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
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
L-685,458, an Aspartyl Protease Transition State Mimic, Is a Potent Inhibitor of Amyloid β-Protein Precursor γ-Secretase Activity
Shearman, Mark S, Beher, Dirk, Clarke, Earl E, Lewis, Huw D, Harrison, Tim, Hunt, Peter, Nadin, Alan, Smith, Adrian L, Stevenson, Graeme, Castro, José L
Published in Biochemistry (Easton) (01.08.2000)
Published in Biochemistry (Easton) (01.08.2000)
Get full text
Journal Article
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
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
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
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
Involvement of Caspases in Proteolytic Cleavage of Alzheimer’s Amyloid-β Precursor Protein and Amyloidogenic Aβ Peptide Formation
Gervais, François G., Xu, Daigen, Robertson, George S., Vaillancourt, John P., Zhu, Yanxia, Huang, JingQi, LeBlanc, Andréa, Smith, David, Rigby, Michael, Shearman, Mark S., Clarke, Earl E., Zheng, Hui, Van Der Ploeg, Leonardus H.T., Ruffolo, Salvatore C., Thornberry, Nancy A., Xanthoudakis, Steve, Zamboni, Robert J., Roy, Sophie, Nicholson, Donald W.
Published in Cell (30.04.1999)
Published in Cell (30.04.1999)
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
Intra- or Intercomplex Binding to the γ-Secretase Enzyme
Earl E. Clarke, Ian Churcher, Semantha Ellis, Jonathan D. J. Wrigley, Huw D. Lewis, Timothy Harrison, Mark S. Shearman, Dirk Beher
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 γ-Secretase at a Novel Site
Dirk Beher, Earl E. Clarke, Jonathan D. J. Wrigley, Agnes C. L. Martin, Alan Nadin, Ian Churcher, Mark S. Shearman
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
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
Functional Overexpression of γ-Secretase Reveals Protease-independent Trafficking Functions and a Critical Role of Lipids for Protease Activity
Jonathan D. J. Wrigley, Irina Schurov, Emma J. Nunn, Agnes C. L. Martin, Earl E. Clarke, Semantha Ellis, Timothy P. Bonnert, Mark S. Shearman, Dirk Beher
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