Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Xavier Pelle"'
Autor:
Xavier Pelle, Pierre Nimsgern, Pascale Fille, Yves Ruff, Frederic Berst, Maxim Ratnikov, Roberto Martinez
Publikováno v:
ACS Combinatorial Science. 22:120-128
The use of DNA-encoded libraries has emerged as a powerful hit generation technology. Combining the power of combinatorial chemistry to enumerate large compound collections with the efficiency of affinity selection in pools, the methodology makes it
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17d85bb9dafd6f294d55d76f8a65e945
https://doi.org/10.1021/acscombsci.9b00164
https://doi.org/10.1021/acscombsci.9b00164
Autor:
Margaret E Brousseau, Kevin B Clairmont, Glen Spraggon, Alec N Flyer, Andrei A Golosov, Philipp Grosche, Jérôme André, Shari Caplan, Guanjing Chen, Li Fan, Raphael Gattlen, Alexander Koch, Ian Lewis, Jingzhou Li, Eugene Liu, Danuta Lubicka, Andreas Marzinzik, Katsumasa Nakajima, David Nettleton, Johannes Ottl, Meihui Pan, Tajesh Patel, Stephanie Pickett, Jennifer Poirier, Patrick C Reid, Xavier Pelle, Vanitha Subramanian, Victoria Vera, Mei Xu, Lihua Yang, Qing Yang, jinghua yu, Guoming Zhu, Lauren G Monovich
Publikováno v:
Circulation. 144
Elevated LDL-C is a major risk factor for atherosclerotic cardiovascular disease, the leading cause of death worldwide. Proprotein convertase subtilisin/kexin type 9 (PCSK9) has pronounced effects on LDL-C levels via its modulation of hepatic LDL rec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4c41fa5183540594ef99cce950597f62
https://doi.org/10.1161/circ.144.suppl_1.10516
https://doi.org/10.1161/circ.144.suppl_1.10516
Autor:
Katsumasa Nakajima, David Nettleton, Guoming Zhu, Debra Burdick, Alexander W. Koch, Qing Yang, Glen Spraggon, Margaret E. Brousseau, Guanjing Chen, Lisa Ames, Raphael Gattlen, Flyer Alec, Jennifer Poirier, Jingzhou Li, Mohindra Seepersaud, Dawn Kelly-Sullivan, Stephanie Pickett, Xavier Pelle, Lauren Perry, Raj Chopra, Jakal Amin, Jerome Andre, Danuta Lubicka, Victoria Vera, Philipp Grosche, Patel Tajesh Jayprakash, Ian Lewis, Lihua Yang, Eugene Liu, Andrei Golosov, jinghua yu, Li Fan, Patrick C. Reid, Lauren G. Monovich, Shari L. Caplan, Meihui Pan, Diana Dubiel, Vanitha Subramanian, Kevin B. Clairmont, Johannes Ottl, Mei Xu, Andreas Marzinzik
Publikováno v:
Cell Chemical Biology. 29:249-258.e5
Summary Proprotein convertase subtilisin/kexin type 9 (PCSK9) regulates plasma low-density lipoprotein cholesterol (LDL-C) levels by promoting hepatic LDL receptor (LDLR) degradation. Therapeutic antibodies that disrupt PCSK9-LDLR binding reduce LDL-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9b646053b683b9aba0f84b9efef17df
https://doi.org/10.1016/j.chembiol.2021.08.012
https://doi.org/10.1016/j.chembiol.2021.08.012
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1
Autor:
Sandra W. Cowan-Jacob, A.A. Wylie, Bahaa Salem, J.M. Groell, Franco Lombardo, Peter Drueckes, Gabriele Rummel, Paul W. Manley, G. Berellini, Robert Martin Grotzfeld, Alice Loo, Markus Warmuth, Chrystelle Henry, Andreas Marzinzik, A.Q. Hassan, Xavier Pelle, V. Iyer, Stephanie Kay Dodd, Joseph Schoepfer, Simona Cotesta, Pascal Furet, Darryl Brynley Jones, Doriano Fabbro, Tobias Gabriel, Wolfgang Jahnke, S. Buonamici, Thomas Zoller
Publikováno v:
Journal of Medicinal Chemistry. 61:8120-8135
Chronic myelogenous leukemia (CML) arises from the constitutive activity of the BCR-ABL1 oncoprotein. Tyrosine kinase inhibitors (TKIs) that target the ATP-binding site have transformed CML into a chronic manageable disease. However, some patients de
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d43ca6c11f830ca5a00d41dc4c6b7d49
https://doi.org/10.1021/acs.jmedchem.8b01040
https://doi.org/10.1021/acs.jmedchem.8b01040
Autor:
Hans Bitter, Sandra W. Cowan-Jacob, A. Quamrul Hassan, Silvia Buonamici, Andreas Marzinzik, Wolfgang Jahnke, Sanjeev Thohan, Jerry Donovan, Timothy P. Hughes, Wenjing Zhu, Andrew Wylie, Pascal Furet, Michael Palmer, Lilli Petruzzelli, Xavier Pelle, Susan Branford, Joseph Schoepfer, William R. Sellers, K. Gary Vanasse, Alice Loo, Nicholas Keen, Francesco Hofmann, Franco Lombardo, David M. Ross, Giuliano Berellini, Markus Warmuth, Stephanie Kay Dodd, Varsha Iyer
Publikováno v:
Nature. 543:733-737
Chronic myeloid leukaemia (CML) is driven by the activity of the BCR-ABL1 fusion oncoprotein. ABL1 kinase inhibitors have improved the clinical outcomes for patients with CML, with over 80% of patients treated with imatinib surviving for more than 10
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f07354b900e8232f5f55b603e546d48
https://doi.org/10.1038/nature21702
https://doi.org/10.1038/nature21702
Autor:
Xavier Pellerin Le Bas, Laurent Froideval, Adan Mouko, Christophe Conessa, Laurent Benoit, Laurent Perez
Publikováno v:
Remote Sensing, Vol 16, Iss 16, p 2891 (2024)
This study introduces a new software, cLASpy_T, that helps design models for the automatic 3D point cloud classification of coastal environments. This software is based on machine learning algorithms from the scikit-learn library and can classify poi
Externí odkaz:
https://doaj.org/article/cd266bb6cc85460caa4bb36f54da48ff
Autor:
Andreas Marzinzik, Silvio Ofner, Jean-Michel Rondeau, Wolfgang Jahnke, Chrystelle Henry, S. Lehmann, E. Bourgier, Xavier Pelle, Jonathan Green, J. Constanze D. Hartwieg, Rene Hemmig, Simona Cotesta, Guido Bold, Frédéric Stauffer
Publikováno v:
Angewandte Chemie. 127:14783-14787
Die Wirksamkeit und Vertraglichkeit eines Medikaments kann verbessert werden, indem dieses gezielt an den gewunschten Wirkungsort gebracht wird. Bisphosphonate sind Prototypen derartiger Medikamente; allerdings ist ihre Affinitat zum Knochen eher zu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::87792e19609ec7716e6908d3d507899a
https://doi.org/10.1002/ange.201507064
https://doi.org/10.1002/ange.201507064
Autor:
Francisco Adrian, Janis Liebetanz, André Strauss, Sandra W. Cowan-Jacob, Andreas Marzinzik, Xavier Pelle, Pascal Furet, Frederic Berst, Jürgen Mestan, Paul W. Manley, Gabriele Fendrich, Robert Martin Grotzfeld, Nathanael S. Gray, Markus Warmuth, Doriano Fabbro, Jianming Zhang, Alexandra Szyttenholm, Wolfgang Jahnke
Publikováno v:
Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics. 1804:454-462
The ATP-competitive inhibitors dasatinib and nilotinib, which bind to catalytically different conformations of the Abl kinase domain, have recently been approved for the treatment of imatinib-resistant CML. These two new drugs, albeit very efficient
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5cb61c5abe9c391126e4268635db9538
https://doi.org/10.1016/j.bbapap.2009.12.009
https://doi.org/10.1016/j.bbapap.2009.12.009
Autor:
Jean-Michel Rondeau, E. Bourgier, Marjo Götte, Johann Zimmermann, Armin Widmer, Steven J. Stout, Andreas Marzinzik, René Amstutz, Wolfgang Jahnke, S. Lehmann, Xavier Pelle, Christelle Henry, Frédéric Stauffer, Silvio Ofner, Simona Cotesta, Guido Bold, Thomas Zoller, J. Fraser Glickman, Thomas P. Roddy, J. Constanze D. Hartwieg
Publikováno v:
ChemMedChem. 10(11)
Farnesyl pyrophosphate synthase (FPPS) is an established target for the treatment of bone diseases, but also shows promise as an anticancer and anti-infective drug target. Currently available anti-FPPS drugs are active-site-directed bisphosphonate in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38093a983a2bffe41ce36a8d35f93526
https://pubmed.ncbi.nlm.nih.gov/26381451
https://pubmed.ncbi.nlm.nih.gov/26381451
Autor:
Frédéric Stauffer, Jean-Michel Rondeau, Simona Cotesta, Jonathan Green, Rene Hemmig, J. Constanze D. Hartwieg, Guido Bold, Andreas Marzinzik, Xavier Pelle, Silvio Ofner, E. Bourgier, Chrystelle Henry, Wolfgang Jahnke, S. Lehmann
Publikováno v:
Angewandte Chemie (International ed. in English). 54(48)
Targeting drugs to their desired site of action can increase their safety and efficacy. Bisphosphonates are prototypical examples of drugs targeted to bone. However, bisphosphonate bone affinity is often considered too strong and cannot be significan
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a912087c34e094acec2b0ff6e6e3263
https://pubmed.ncbi.nlm.nih.gov/26457482
https://pubmed.ncbi.nlm.nih.gov/26457482