Retinoic acid synthesis by NG2 expressing cells promotes a permissive environment for axonal outgrowth
Goncalves, Maria B., Wu, Yue, Trigo, Diogo, Clarke, Earl, Malmqvist, Tony, Grist, John, Hobbs, Carl, Carlstedt, Thomas P., Corcoran, Jonathan P.T.
Published in Neurobiology of disease (01.03.2018)
Published in Neurobiology of disease (01.03.2018)
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C286, an orally available retinoic acid receptor β agonist drug, regulates multiple pathways to achieve spinal cord injury repair
Goncalves, Maria B, Wu, Yue, Clarke, Earl, Grist, John, Moehlin, Julien, Mendoza-Parra, Marco Antonio, Hobbs, Carl, Kalindjian, Barret, Fok, Henry, Mander, Adrian P, Hassanin, Hana, Bendel, Daryl, Täubel, Jörg, Mant, Tim, Carlstedt, Thomas, Jack, Julian, Corcoran, Jonathan P T
Published in Frontiers in molecular neuroscience (20.08.2024)
Published in Frontiers in molecular neuroscience (20.08.2024)
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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)
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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)
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RARβ Agonist Drug (C286) Demonstrates Efficacy in a Pre-clinical Neuropathic Pain Model Restoring Multiple Pathways via DNA Repair Mechanisms
Goncalves, Maria B., Moehlin, Julien, Clarke, Earl, Grist, John, Hobbs, Carl, Carr, Antony M., Jack, Julian, Mendoza-Parra, Marco Antonio, Corcoran, Jonathan P.T.
Published in iScience (25.10.2019)
Published in iScience (25.10.2019)
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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)
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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)
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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)
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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)
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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)
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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)
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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)
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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)
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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)
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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)
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Drug repurposing for Alzheimer's disease based on transcriptional profiling of human iPSC-derived cortical neurons
Williams, Gareth, Gatt, Ariana, Clarke, Earl, Corcoran, Jonathan, Doherty, Patrick, Chambers, David, Ballard, Clive
Published in Translational psychiatry (06.09.2019)
Published in Translational psychiatry (06.09.2019)
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Phase 1 safety, tolerability, pharmacokinetics and pharmacodynamic results of KCL‐286, a novel retinoic acid receptor‐β agonist for treatment of spinal cord injury, in male healthy participants
Goncalves, Maria B., Mant, Tim, Täubel, Jörg, Clarke, Earl, Hassanin, Hana, Bendel, Daryl, Fok, Henry, Posner, John, Holmes, Jane, Mander, Adrian P., Corcoran, Jonathan P. T.
Published in British journal of clinical pharmacology (01.12.2023)
Published in British journal of clinical pharmacology (01.12.2023)
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Neuronal RARβ Signaling Modulates PTEN Activity Directly in Neurons and via Exosome Transfer in Astrocytes to Prevent Glial Scar Formation and Induce Spinal Cord Regeneration
Goncalves, Maria B, Malmqvist, Tony, Clarke, Earl, Hubens, Chantal J, Grist, John, Hobbs, Carl, Trigo, Diogo, Risling, Mårten, Angeria, Maria, Damberg, Peter, Carlstedt, Thomas P, Corcoran, Jonathan P T
Published in The Journal of neuroscience (25.11.2015)
Published in The Journal of neuroscience (25.11.2015)
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