Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Anja Jestel"'
Autor:
Dylan J. Taatjes, Andrei V. Krivtsov, Alexander Arefolov, Ge Zou, Ioana Nitulescu, Anupong Tangpeerachaikul, Nancy E. Kohl, Olugbeminiyi O Fadeyi, Roderick T. Bronson, Andrew G. Myers, Andrew L. Kung, Scott A. Armstrong, Henry E. Pelish, Brian B. Liau, Diogo H. Da Silva, Karrie Du, E.V. Schneider, Amanda L. Christie, Madeleine E. Lemieux, Zachary C. Poss, Matthew D. Shair, Deepti Banka, Brittany T. Caruso, Chong Si, Christopher C. Ebmeier, Anja Jestel
Publikováno v:
Nature
Super-enhancers (SEs), which are composed of large clusters of enhancers densely loaded with the Mediator complex, transcription factors and chromatin regulators, drive high expression of genes implicated in cell identity and disease, such as lineage
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b0f5a8dd31ffaa438c4711e420afca94
https://doi.org/10.1038/nature14904
https://doi.org/10.1038/nature14904
Autor:
Stephan Krapp, James J. Crawford, Lyn Rosenbrier Ribeiro, Andrew David Morley, Jonathan E. Finlayson, Calum Cook, Caroline Smith, Jonathan Bowyer, Anja Jestel, Julian A. Hudson, Stefan Steinbacher, Benjamin P. McDermott, Thomas M. McGuire, Adrian John Highton, Alexander G. Dossetter, Ken Page, Peter W. Kenny, Morris Jeffrey James, Christine Heyes, Philip A. MacFaul, Helen Sawney, Scott W. Martin
Publikováno v:
Journal of Medicinal Chemistry. 55:8827-8837
Rational structure-based design has yielded highly potent inhibitors of cathepsin K (Cat K) with excellent physical properties, selectivity profiles, and pharmacokinetics. Compounds with a 3,4-(CH₃O)₂Ph motif, such as 31, were found to have excel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10c9fe76f9dfd359a75bdb8ca7448118
https://doi.org/10.1021/jm301119s
https://doi.org/10.1021/jm301119s
Autor:
Anja Jestel, Stephan Krapp, Maureen Dempster, Xavier Fradera, Susanna Nagel, Emma Carswell, Andrew J. Cooke, William Hamilton, Bert Kazemier, Arthur Oubrie
Publikováno v:
Acta Crystallographica Section F Structural Biology and Crystallization Communications. 68:404-408
Factor XI (FXI) is a key enzyme in the coagulation pathway and an attractive target for the development of anticoagulant drugs. A small number of high-resolution crystal structures of FXIa in complex with small synthetic inhibitors have been publishe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fbb9445d69885ca908101db6115fb6f4
https://doi.org/10.1107/s1744309112009037
https://doi.org/10.1107/s1744309112009037
Autor:
Wolfram Bode, Peter Reinemer, Luis Moroder, Sergio A. Cadamuro, Peter Goettig, Holger Steuber, Marion G. Götz, Michael Willem, Christian Renner, Tanja Kohler, Anja Jestel, Alessandra Barazza
Publikováno v:
ChemBioChem. 8:2078-2091
Minimal sequence requirements for binding of substrate-derived statine peptides to the aspartyl enzyme were established on the basis of the X-ray cocrystal structure of the hydroxyethylene-octapeptide OM00-3 in complexation with BACE-1. With this inf
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9b8d2185df743b60e3862174f2a7ac8b
https://doi.org/10.1002/cbic.200700383
https://doi.org/10.1002/cbic.200700383
Autor:
Christian Benda, Hans Brandstetter, Albrecht Messerschmidt, Milko Velarde, Mathias Bädeker, Michael Blaesse, Anja Jestel, Sofia Macieira, Torsten Neuefeind
Publikováno v:
Journal of Molecular Biology. 352:918-931
Atypical protein kinases C (aPKCs) play critical roles in signaling pathways that control cell growth, differentiation and survival. Therefore, they constitute attractive targets for the development of novel therapeutics against cancer. The crystal s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::73eff0ab811bfa5637eb9134db8ef266
https://doi.org/10.1016/j.jmb.2005.07.060
https://doi.org/10.1016/j.jmb.2005.07.060
Autor:
Megumi Ikemori-Kawada, Atsushi Inoue, Anja Jestel, Konstanze von König, Akihiko Tsuruoka, Tomohiro Matsushima, Junji Matsui, Kiyoshi Okamoto, Yasuhiro Funahashi
Publikováno v:
ACS medicinal chemistry letters. 6(1)
Lenvatinib is an oral multikinase inhibitor that selectively inhibits vascular endothelial growth factor (VEGF) receptors 1 to 3 and other proangiogenic and oncogenic pathway-related receptor tyrosine kinases. To elucidate the origin of the potency o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f8b6d716ea9bbf7c1c1422d98fe44e1b
https://pubmed.ncbi.nlm.nih.gov/25589937
https://pubmed.ncbi.nlm.nih.gov/25589937
Autor:
Ken Page, Peter W. Kenny, Morris Jeffrey James, Stephan Krapp, Christine Heyes, Calum Cook, Helen Sawney, Lyn Rosenbrier Ribeiro, Andrew David Morley, Jonathan Bowyer, Adrian John Highton, Julian A. Hudson, Stefan Steinbacher, Anja Jestel, Scott W. Martin, Madeleine Vickers, Thomas M. McGuire, Philip A. MacFaul, Alexander G. Dossetter, Jonathan E. Finlayson, Nicola Murdoch Heron, Pablo Morentin Gutierrez, Howard H Beeley, James J. Crawford, Caroline Smith
Publikováno v:
Journal of medicinal chemistry. 55(14)
Directed screening of nitrile compounds revealed 3 as a highly potent cathepsin K inhibitor but with cathepsin S activity and very poor stability to microsomes. Synthesis of compounds with reduced molecular complexity, such as 7, revealed key SAR and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::affa107536bbdb5700a7b53c64d0f5a7
https://pubmed.ncbi.nlm.nih.gov/22742641
https://pubmed.ncbi.nlm.nih.gov/22742641
Autor:
Jonathan Bowyer, Anja Jestel, Adrian John Highton, Philip A. MacFaul, Stephan Krapp, Alexander G. Dossetter, Thomas M. McGuire, Helen Sawney, Jonathan E. Finlayson, Morris Jeffrey James, Stefan Steinbacher, Caroline Smith, Christine Heyes, Andrew David Morley, Calum Cook, Nicola Murdoch Heron, Julian A. Hudson, James J. Crawford, Lyn Rosenbrier Ribeiro, Ken Page
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(17)
The discovery of nitrile compound 4, a potent inhibitor of Cathepsin K (Cat K) with good bioavailability in dog is described. The compound was used to demonstrate target engagement and inhibition of Cat K in an in vivo dog PD model. The margin to hER
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e0f37a66cacb75592dfb15ed0b0c6dd
https://pubmed.ncbi.nlm.nih.gov/22858142
https://pubmed.ncbi.nlm.nih.gov/22858142
Autor:
Jark, Böttcher, Anja, Jestel, Reiner, Kiefersauer, Stephan, Krapp, Susanna, Nagel, Stefan, Steinbacher, Holger, Steuber
Publikováno v:
Methods in enzymology. 493
In the past two decades, fragment-based approaches have evolved as a predominant strategy in lead discovery. The availability of structural information on the interaction geometries of binding fragments is key to successful structure-guided fragment-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::65627bf5a5baadb9bec81258db81f3c1
https://pubmed.ncbi.nlm.nih.gov/21371587
https://pubmed.ncbi.nlm.nih.gov/21371587
Autor:
Susanna Nagel, Reiner Kiefersauer, Stephan Krapp, Anja Jestel, Holger Steuber, Stefan Steinbacher, Jark Böttcher
In the past two decades, fragment-based approaches have evolved as a predominant strategy in lead discovery. The availability of structural information on the interaction geometries of binding fragments is key to successful structure-guided fragment-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e907d555f1c82043d788754c8cac4cbe
https://doi.org/10.1016/b978-0-12-381274-2.00003-0
https://doi.org/10.1016/b978-0-12-381274-2.00003-0
