Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Stephan, Krapp"'
Autor:
Norma Rogers, Stephan Krapp, Faika Mseeh, Richard T. Lewis, Keith Mikule, Michelle Han, Jay Theroff, Yongying Jiang, Keith M. Wilcoxen, Cross Jason, Dana Pfaffinger, Michael J. Soth, Paul G. Leonard, Philip Jones, Pijus K. Mandal, Angela L. Harris, Martin R. Tremblay, Simon S. Yu, Jason P Burke, Connor A. Parker, Barbara Czako, Alessia Petrocchi, Naphtali J. Reyna, Joseph R. Marszalek, Matthew M. Hamilton, Timothy McAfoos, Brett W. Virgin-Downey, Graham Trevitt, Alfred Lammens, Alan Xu
Publikováno v:
Journal of Medicinal Chemistry. 64:11302-11329
Indoleamine 2,3-dioxygenase 1 (IDO1), a heme-containing enzyme that mediates the rate-limiting step in the metabolism of l-tryptophan to kynurenine, has been widely explored as a potential immunotherapeutic target in oncology. We developed a class of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec33cf6551a670d4d40eaab2894a6f60
https://doi.org/10.1021/acs.jmedchem.1c00679
https://doi.org/10.1021/acs.jmedchem.1c00679
Autor:
Ruth Geiss-Friedlander, Walter Littmann, Stephan Krapp, Breyan Ross, Robert Huber, Reiner Kiefersauer
Publikováno v:
Journal of Applied Crystallography
A novel aerosol device for protein crystal complexation using ultrasonic vibrations is described.
Soaking of macromolecular crystals allows the formation of complexes via diffusion of molecules into a preformed crystal for structural analysis. S
Soaking of macromolecular crystals allows the formation of complexes via diffusion of molecules into a preformed crystal for structural analysis. S
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e09416c1c0558ab300da4d8b1cbe0ff
Autor:
Sevan Habeshian, Lukas Lercher, Ying Zhang, John W. Cuozzo, Yanbin Liu, Xia Tian, Martin Augustin, Andreas Bergmann, Stephan Krapp, Michael Mrosek, Alfred Lammens, Paolo A. Centrella, Archna Archna, Maike Däther, Marie-Aude Guié, Debora L. Konz Makino, Klaus Pflügler, Reiner Kiefersauer, Julie Liu, Klaus Maskos, John P. Guilinger, Anthony D. Keefe, Heather A. Thomson, Matthew A. Clark, Markus Siegert
Publikováno v:
Bioorganic & Medicinal Chemistry. 42:116223
Libraries of DNA-Encoded small molecules created using combinatorial chemistry and synthetic oligonucleotides are being applied to drug discovery projects across the pharmaceutical industry. The majority of reported projects describe the discovery of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ef4f8e3b428396e039274205268b549
https://doi.org/10.1016/j.bmc.2021.116223
https://doi.org/10.1016/j.bmc.2021.116223
Autor:
Daniel Ysselstein, Dimitri Krainc, Richard B. Silverman, Jianbin Zheng, Renato T. Skerlj, Neil L. Kelleher, Peter T. Lansbury, Long Chen, Stephan Krapp, Michael Mrosek, Ursula Heunisch, Joel Charrow, Jonathan P. Remis, Michael Schwake, Owen S. Skinner
Publikováno v:
Journal of the American Chemical Society. 140(18)
β-Glucocerebrosidase (GCase) mutations cause Gaucher’s disease and are a high risk factor in Parkinson’s disease. The implementation of a small molecule modulator is a strategy to restore proper folding and lysosome delivery of degradation-prone
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1b64c2dcc14d094ae3065b55955506ad
https://pubmed.ncbi.nlm.nih.gov/29676907
https://pubmed.ncbi.nlm.nih.gov/29676907
Autor:
Stefan Gerhardt, William McCoull, Jane E. Moore, John Revill, Martin J. Packer, Stephan Krapp, James S. Scott, Nicholas John Newcombe, Derek Ogg, Elaine Kilgour, Amanda Rees, Stefan Steinbacher, Nidhal Selmi, Martin Augustin, Caroline Blake, Anne Ertan, Paul Robert Owen Whittamore
Publikováno v:
Med. Chem. Commun.. 5:57-63
3,3-Di-methyl-azetidin-2-ones were identified as potent and selective 11β-HSD1 inhibitors against the human and mouse forms of the enzyme. Structure guided optimisation of LLE was conducted, utilising a key polar interaction and identifying stereoch
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d5ec1d9e811431313f5ae29a9b1caaaf
https://doi.org/10.1039/c3md00234a
https://doi.org/10.1039/c3md00234a
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:
Stefan Gerhardt, Andrew David Morley, Peter W. Kenny, Hannes Simader, Emma V. Jones, Galith Karoutchi, Stephan Krapp, Neil Rankine, Keith Oldham, Paul A. Bethel, Stefan Steinbacher, Martin Augustin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4622-4625
A number of molecular recognition features have been exploited in structure-based design of selective Cathepsin inhibitors.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b5e987a8e0f4a810fd0d5bfae2d2508
https://doi.org/10.1016/j.bmcl.2009.06.090
https://doi.org/10.1016/j.bmcl.2009.06.090
Autor:
Neil Rankine, Linda J. Wood, Galith Karoutchi, Michelle Coulson, Keith Oldham, Emma V. Jones, Paul A. Bethel, Stephan Krapp, Susannah J. Ford, Stefan Gerhardt, David Ryan, Matthew Grist, Peter W. Kenny, Hannes Simader, Andrew David Morley, Stuart L. Wells, Gordon A. Hamlin, Stefan Steinbacher, Jack E. Dawson, Nabil Asaad, Martin Augustin, Michael James
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4280-4283
A series of potent Cathepsin L inhibitors with good selectivity with respect to other cysteine Cathepsins is described and SAR is discussed with reference to the crystal structure of a protein-ligand complex.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca39a993160acd7584b90a963ada1ade
https://doi.org/10.1016/j.bmcl.2009.05.071
https://doi.org/10.1016/j.bmcl.2009.05.071
Autor:
Gleb Bourenkov, Thomas Steiner, Stephan Krapp, Rita Gerardy-Schahn, Robert Huber, Petra Hess, Uwe Jacob, Anne-Christin Lamerz, Constanze Breithaupt
Publikováno v:
Journal of Biological Chemistry. 282:13003-13010
Uridine diphosphate-glucose pyrophosphorylase (UGPase) represents a ubiquitous enzyme, which catalyzes the formation of UDP-glucose, a key metabolite of the carbohydrate pathways of all organisms. In the protozoan parasite Leishmania major, which cau
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e2486ea4b2b6e8c2e57aa7baa14bc63
https://doi.org/10.1074/jbc.m609984200
https://doi.org/10.1074/jbc.m609984200