Zobrazeno 1 - 10
of 70
pro vyhledávání: '"J.C.M. Uitdehaag"'
Autor:
Helma van den Hurk, Jan J. M. van Groningen, Jos de Man, Johan Friesen, J.C.M. Uitdehaag, Guido J.R. Zaman, Yvonne Grobben, Nicole Willemsen-Seegers, Rogier C. Buijsman
Publikováno v:
SLAS Discovery. 25:1018-1025
Arginase-1, which converts the amino acid L-arginine into L-ornithine and urea, is a promising new drug target for cancer immunotherapy, as it has a role in the regulation of T-cell immunity in the tumor microenvironment. To enable the discovery of s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9196233de65aa40a9f091093779243b6
https://doi.org/10.1177/2472555220919340
https://doi.org/10.1177/2472555220919340
Autor:
Hortense Deronzier, Cecile Dorleans, John Waller, Laurent Saniere, Andre Fouquet, Fiona Elizabeth Andrews, Mark Baugh, J.C.M. Uitdehaag, George McGarry, Phil Jones, Ann Mitchell, Emma Kinghorn, Eric Nicolai, Wilson Caulfield, Zoran Rankovic, Dominique Potin, Mario van Zeeland, Wullie Arbuckle, Jennifer Kerr, Jiaqiang Cai, Mark Wheaton Anderson, Iain Martin, Maureen Dempster, Ashvin Mistry, François Chevallier, William Finlay, Clive Long, Robinson John E, Xavier Fradera, Paul Westwood, Iain Cumming
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6237-6241
Several structure-guided optimisation strategies were explored in order to improve the hERG selectivity profile of cathepsin K inhibitor 1 , whilst maintaining its otherwise excellent in vitro and in vivo profile. Ultimately, attenuation of c log P a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dbcfb747e700da9944dc50d293047fcc
https://doi.org/10.1016/j.bmcl.2010.08.101
https://doi.org/10.1016/j.bmcl.2010.08.101
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:
J.C.M. Uitdehaag, Rogier C. Buijsman, Guido J.R. Zaman, Martine B.W. Prinsen, Jeffrey J. Kooijman, Jos de Man, Jeroen A.D.M. de Roos, Judith R.F. de Vetter, Suzanne J.C. van Gerwen, Nicole Willemsen-Seegers, Jelle Dylus
Publikováno v:
Cancer Research. 78:4907-4907
Profiling of new drug candidates on cancer cell line panels is an important tool to identify candidate drug response biomarkers for clinical studies. We have set up a platform, called Oncolines™, that comprises 102 genetically well-characterized ce
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::10781ef5affbfa549ee824f5c87f3c27
https://doi.org/10.1158/1538-7445.am2018-4907
https://doi.org/10.1158/1538-7445.am2018-4907
Autor:
R.C. Buijsman, Martine B.W. Prinsen, Jelle Dylus, S.J.C. Van Gerwen, Jeffrey J. Kooijman, J.A.D.M. De Roos, J. de Man, J.C.M. Uitdehaag, G.J.R. Zaman, J.R.F. De Vetter
Publikováno v:
ESMO Open. 3:A201
Introduction Profiling of drugs on cancer cell line panels can uncover new insights into the mechanisms of drug response. We have established a panel of 102 genetically well-characterised cell lines from distinct tumour origins, called Oncolines. Ear
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::517de969e323dd0343ab41208ccd79cc
https://doi.org/10.1136/esmoopen-2018-eacr25.477
https://doi.org/10.1136/esmoopen-2018-eacr25.477
Akademický článek
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Autor:
J.C.M. Uitdehaag
Publikováno v:
Drug Discovery Today. 16:369-371
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dd0a796b5424ae937c8dd68d6dea109a
https://doi.org/10.1016/j.drudis.2011.02.013
https://doi.org/10.1016/j.drudis.2011.02.013
Autor:
R.C. Buijsman, G.J.R. Zaman, J. de Man, Nicole Willemsen-Seegers, Martine B.W. Prinsen, Masaaki Sawa, J.R.F. De Vetter, J.C.M. Uitdehaag, Yusuke Kawase
Publikováno v:
European Journal of Cancer. 69:S79
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3d8acde9154dfa37e7bea9f8b34b1312
https://doi.org/10.1016/s0959-8049(16)32830-1
https://doi.org/10.1016/s0959-8049(16)32830-1
Autor:
J.R.F. De Vetter, Martine B.W. Prinsen, Nicole Willemsen-Seegers, Jelle Dylus, S.J.C. Van Gerwen, Jeffrey J. Kooijman, R.C. Buijsman, J.A.D.M. De Roos, Masaaki Sawa, A.M. Van Doornmalen, G.J.R. Zaman, J. de Man, J.C.M. Uitdehaag
Publikováno v:
European Journal of Cancer. 69:S24
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::28b9fcda145b876f2acb824ebbd531bb
https://doi.org/10.1016/s0959-8049(16)32652-1
https://doi.org/10.1016/s0959-8049(16)32652-1