Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Earl E. Clarke"'
Autor:
Mohamed Shaimi, Jayesh Mistry, Huw D. Lewis, Jonathan D. Best, Christopher J. Welch, Andrew Madin, Michael Reilly, Fraser Murray, Timothy Harrison, Jonathan D.J. Wrigley, Ian Collins, Mark S. Shearman, Laura Catherine Cooper, Earl E. Clarke, Linda Elizabeth Keown
Publikováno v:
Journal of Medicinal Chemistry. 52:3441-3444
The development of potent gamma-secretase inhibitors having substituted heterocycles attached to a benzobicyclo[4.2.1]nonane core is described. This work led to the identification of [6S,9R,11R]-2',3',4',5,5',6,7,8,9,10-decahydro-2-(5-(4-fluorophenyl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a063e44deb50d5be29f0d0a39011301
https://doi.org/10.1021/jm900056p
https://doi.org/10.1021/jm900056p
Autor:
Andrew Madin, Tim Sparey, Timothy Harrison, Joanne Clare Hannam, Mark S. Shearman, Earl E. Clarke, Bindi Sohal
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:375-379
Bridgehead substituted derivatives of bicyclo[4.2.1]nonanes were synthesized and shown to be potent inhibitors of gamma-secretase. Two related series were synthesized to explore the SARs. More potent compounds were found in the non-benzofused series
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa77a32ef0f4f62ac1a6451f03f7c206
https://doi.org/10.1016/j.bmcl.2007.10.057
https://doi.org/10.1016/j.bmcl.2007.10.057
Autor:
Ian Churcher, Earl E. Clarke, Tim Harrison, Semantha Ellis, Jonathan D.J. Wrigley, Mark S. Shearman, Huw D. Lewis, Dirk Beher
Publikováno v:
Journal of Biological Chemistry. 281:31279-31289
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::111d9b65647ba519ac1b052e09d3f34e
https://doi.org/10.1016/s0021-9258(19)84040-1
https://doi.org/10.1016/s0021-9258(19)84040-1
Autor:
Earl E. Clarke, Timothy Harrison, Jonathan D. Best, Bindi Sohal, Mirlinda Biba, Mark S. Shearman, Christopher J. Welch, Andrew Madin, Jonathan D.J. Wrigley, Huw D. Lewis, José L. Castro, Joanne Clare Hannam, Dirk Beher, Nancy N. Tsou, Tim Sparey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4212-4216
A novel series of N-alkyl-substituted cyclic sulfamides were developed from a screening hit. Chemistries were developed which allowed surveys of N-alkyl groups and amines resulting in the identification of N-trifluoroethyl-substituted cyclic sulfamid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::24d8ea2266ac589e3f3e4a96128239e5
https://doi.org/10.1016/j.bmcl.2005.06.084
https://doi.org/10.1016/j.bmcl.2005.06.084
Autor:
Alan Nadin, Dirk Beher, Ian Churcher, Jonathan D.J. Wrigley, Mark S. Shearman, Agnes C.L. Martin, Earl E. Clarke
Publikováno v:
Journal of Biological Chemistry. 279:43419-43426
γ-Secretase is a multi-component enzyme complex that performs an intramembranous cleavage, releasing amyloid-β (Aβ) peptides from processing intermediates of the β-amyloid precursor protein. Because Aβ peptides are thought to be causative for Al
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8e92ec0f13d24ead051b7e0c53abea59
https://doi.org/10.1074/jbc.m404937200
https://doi.org/10.1074/jbc.m404937200
Autor:
Bart De Strooper, Jonathan D.J. Wrigley, Mark S. Shearman, Emma J. Nunn, Omar Nyabi, Dirk Beher, Earl E. Clarke, Alan Nadin, Peter W. Hunt
Publikováno v:
Journal of Neurochemistry. 90:1312-1320
Gamma-secretase performs the final processing step in the generation of amyloid-beta (Abeta) peptides, which are believed to be causative for Alzheimer's disease. Presenilins (PS) are required for gamma-secretase activity and the presence of two esse
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::20a9fc35349fb54751f79c24937ec3ea
https://doi.org/10.1111/j.1471-4159.2004.02596.x
https://doi.org/10.1111/j.1471-4159.2004.02596.x
Autor:
Dirk Beher, Alan Nadin, Timothy Harrison, Colin L. Masters, Michael Fricker, Earl E. Clarke, Janetta G. Culvenor, Mark S. Shearman, Jonathan D.J. Wrigley, Yue-Ming Li
Publikováno v:
Biochemistry. 42:8133-8142
Gamma-secretase is the enzyme activity releasing the amyloid-beta peptide from membrane-bound processing intermediates derived from the beta-amyloid precursor protein. Cellular release and subsequent aggregation of the amyloid-beta peptide is thought
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e416f43fea3b3d26ab43b8e7ecc3c2f
https://doi.org/10.1021/bi034045z
https://doi.org/10.1021/bi034045z
Autor:
Sonia Kerrad, Timothy Harrison, Ian Churcher, Susie Williams, Yui S. Tang, Dirk Beher, Earl E. Clarke, José L. Castro, Wensheng Liu, Mark S. Shearman, Huw D. Lewis, Jonathan D.J. Wrigley
Publikováno v:
Journal of Medicinal Chemistry. 46:2275-2278
Novel benzodiazepine-containing gamma-secretase inhibitors for potential use in Alzheimer's disease have been designed that incorporate a substituted hydrocinnamide C-3 side chain. A syn combination of alpha-alkyl or aryl and beta-hydroxy or hydroxym
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8ace8806549107cc0385af07cda58fb6
https://doi.org/10.1021/jm034058a
https://doi.org/10.1021/jm034058a
Autor:
Earl E. Clarke, Mark S. Shearman
Publikováno v:
Journal of Neuroscience Methods. 102:61-68
Many of the recent advances in the understanding of the pathological processes underlying Alzheimer's disease have come about as a result of the development of assays that can specifically quantitate in biological milieu amyloid-beta (A beta) peptide
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78229d6ba55911a89d1b02aa14142268
https://doi.org/10.1016/s0165-0270(00)00280-6
https://doi.org/10.1016/s0165-0270(00)00280-6
Autor:
Semantha Ellis, Timothy Harrison, Huw D. Lewis, Dirk Beher, Ian Churcher, Jonathan D.J. Wrigley, Mark S. Shearman, Earl E. Clarke
Publikováno v:
The Journal of biological chemistry. 281(42)
Gamma-secretase is one of the critical enzymes required for the generation of amyloid-beta peptides from the beta-amyloid precursor protein. Because amyloid-beta peptides are generally accepted to play a key role in Alzheimer disease, gamma-secretase
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::35b91f96061c43196a95c8476c5d1887
https://pubmed.ncbi.nlm.nih.gov/16899457
https://pubmed.ncbi.nlm.nih.gov/16899457