Zobrazeno 1 - 10
of 19
pro vyhledávání: '"John Bruin"'
Autor:
John Bruin, William Hamilton, Emma Kinghorn, Kenneth S. Cameron, Paul Westwood, Jiaqiang Cai, Kathryn Everett, Clive Long, Maureen Dempster, Chris Claxton, Xavier Fradera, D. Jonathan Bennett, Robinson John E, Simone Belshaw, Philip Jones, Wullie Arbuckle, Mark Baugh, Iain Martin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:932-935
Based on the theoretical understanding of the in vivo lysosomotropism, by adjusting the pka of basic nitrogen containing cathepsin S inhibitors, a set of compounds with pka 6–8 were identified to have excellent cell based Lip10 activity, yet avoidi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::476635684754e9aff8bc8031c6950b59
https://doi.org/10.1016/j.bmcl.2010.12.065
https://doi.org/10.1016/j.bmcl.2010.12.065
Autor:
D. Jonathan Bennett, Kenneth S. Cameron, John Bruin, Mario van Zeeland, Xavier Fradera, J.C.M. Uitdehaag, Emma Kinghorn, Jiaqiang Cai, Maureen Dempster, Paul Westwood, Lucy Popplestone, Mark Baugh, Robinson John E, William Hamilton, Clive Long
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4507-4510
Using computer aided modelling studies, a new extended P2/S2 interaction was identified. This extended region can accommodate a variety of functional groups, such as aryls and basic amines. It was discovered that the N3 nitrogen of the pyrimidine-2-c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b6a4ef389f50e29987f14e5b21317077
https://doi.org/10.1016/j.bmcl.2010.06.043
https://doi.org/10.1016/j.bmcl.2010.06.043
Autor:
T.M. Meulemans, Jonathan Gillespie, D. Jonathan Bennett, Darcey Black, Ann Mitchell, Kenneth S. Cameron, J.C.M. Uitdehaag, Maurice Maidment, Mario van Zeeland, Fiona Elizabeth Andrews, Sylviane Boucharens, Allard Kaptein, Maureen Dempster, Emma Kinghorn, Mark Baugh, Jiaqiang Cai, Philip Jones, Zoran Rankovic, Paul Westwood, Martijn Bastiani, Iain Martin, Iain Cumming, Leon van Berkom, Paul Vink, Paul Scullion, Xavier Fradera, John Bruin, Robinson John E, William Hamilton, Clive Long
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4350-4354
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile analogues were identified as potent and selective cathepsin S inhibitor against both purified enzyme and in human JY cell based cellular assays. This core has a very stable thio-trapping nitrile war-h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78adb9c4a5619dc58c16a256a3eb3516
https://doi.org/10.1016/j.bmcl.2010.06.072
https://doi.org/10.1016/j.bmcl.2010.06.072
Autor:
Eric Nicolai, Clive Long, Ann Mitchell, Maureen Dempster, William Hamilton, Jennifer Kerr, Cecile Dorleans, Iain Martin, Paul Scullion, Hortense Deronzier, John Bruin, Emma Hamilton, Zoran Rankovic, Andre Fouquet, John Robinson, John Waller, Laurent Saniere, Mark Baugh, Fiona Andrews, Jiaqiang Cai, Joost C.M. Uitdehaag, Wilson Caulfield, Dominique Potin, Ashvin Mistry, François Chevallier, Paul Westwood, Emma Kinghorn, George McGarry, Iain Cumming, Mario van Zeeland, X. Fradera
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1524-1527
Morphing structural features of HTS-derived chemotypes led to the discovery of novel 2-cyano-pyrimidine inhibitors of cathepsin K with good pharmacokinetic profiles, for example, compound 20 showed high catK potency (IC(50)=4nM), >580-fold selectivit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c3024221a3f1580ea5f971d2c310f2b7
https://doi.org/10.1016/j.bmcl.2010.01.100
https://doi.org/10.1016/j.bmcl.2010.01.100
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2351-2354
The first solid-phase synthesis of zatebradine 1 and its analogues is reported. This has resulted in the preparation of compounds with increased ability to reduce the spontaneous beating of isolated guinea-pig atria in a concentration-dependent manne
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c525e8d7dcbf21a394c806372ab0b0ea
https://doi.org/10.1016/s0960-894x(01)00424-3
https://doi.org/10.1016/s0960-894x(01)00424-3
Autor:
John Bruin
Publikováno v:
Symposium. 3:93-117
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5665536b64de8982099602a9f8cb6a38
https://doi.org/10.5840/symposium1999316
https://doi.org/10.5840/symposium1999316
Autor:
John Bruin
Publikováno v:
Symposium. 3:296-301
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9a22adbda6430765a0685ae3bc3dce8e
https://doi.org/10.5840/symposium19993226
https://doi.org/10.5840/symposium19993226
Autor:
John Bruin
Publikováno v:
The Modern Schoolman. 70:143-152
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f04cceb5cdb1f6525b0a1629af407f46
https://doi.org/10.5840/schoolman199370216
https://doi.org/10.5840/schoolman199370216
Autor:
Leontien den Hoed, A. Mieke H. Boots, Ethan Grant, Heather J. McKinnon, Kieran McGregor, Monika Gorecka, Jonathan Bennett, Mark Baugh, John Bruin, William Hamilton, Christopher Robert James Claxton, Paul Vink, M. David Percival, Kalpit A. Vora, Clive Long, Marie-Jose van Lierop, Maureen Dempster, Emma Kinghorn, Darcey Black, Jiaqiang Cai, Paul Westwood
Publikováno v:
Journal of autoimmunity. 36(3-4)
The purpose of the study was to examine the potential of inhibition of cathepsin S as a treatment for autoimmune diseases. A highly selective cathepsin S inhibitor, CSI-75, was shown to upregulate levels of the cathepsin S substrate, invariant chain
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db16e71cb07694b02b87aee329b6e8ba
https://pubmed.ncbi.nlm.nih.gov/21439785
https://pubmed.ncbi.nlm.nih.gov/21439785
Autor:
Peter van Rijnsbergen, Kathryn Everett, Simone Belshaw, D. Jonathan Bennett, Wullie Arbuckle, Maureen Dempster, Emma Kinghorn, Xavier Fradera, Mark Baugh, Jiaqiang Cai, Zoran Rankovic, Paul Westwood, John Bruin, William Hamilton, Clive Long, T.M. Meulemans, Philip Jones, Mario van Zeeland, Jennifer Kerr, J.C.M. Uitdehaag, Lucy Popplestone, Leon van Berkom, Iain Martin, Robinson John E
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(23)
The trifluoromethylphenyl P2 motif from previously reported heteroarylnitrile series has been successfully applied for the design and synthesis of highly potent novel ketoamide-based cathepsin S inhibitors. The key in this process is the change of th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b3a43d1f132eeef39158411039e24986
https://pubmed.ncbi.nlm.nih.gov/21030256
https://pubmed.ncbi.nlm.nih.gov/21030256