Michael Schaefer
Novartis
13 Papers
153 Citations
Michael Schaefer is an academic researcher from Novartis. The author has contributed to research in topics: COP9 signalosome & NEDD8. The author has an hindex of 9, co-authored 13 publications.
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Papers
Targeted inhibition of the COP9 signalosome for treatment of cancer.
Anita Schlierf,Eva Altmann,Jean Quancard,Anne B. Jefferson,Rene Assenberg,Martin Renatus,Matthew Jones,Ulrich Hassiepen,Michael Schaefer,Michael Kiffe,Andreas Weiss,Christian Wiesmann,Richard Sedrani,Jörg Eder,Bruno Martoglio +14 more
TL;DR: CSN5i-3 is described, a potent, selective and orally available inhibitor of CSN5, the proteolytic subunit ofCSN, the largest enzyme family of the ubiquitin–proteasome system in humans, which provides insights into how CSN regulates CRLs and suggests that CSN 5 inhibition has potential for anti-tumour therapy.
A natural ligand for the orphan receptor GPR15 modulates lymphocyte recruitment to epithelia
Thomas Suply,Sébastien Hannedouche,Nathalie Carte,Jianping Li,Bianka L. Grosshans,Michael Schaefer,Layla Raad,Valerie Beck,Solange Vidal,Agnès Hiou-Feige,Noemie Beluch,Samuel Barbieri,Johann Wirsching,Nadine Lageyre,Frank Hillger,Corinne Debon,Janet Dawson,Philip Smith,Vincent Lannoy,Michel Detheux,Francis Bitsch,Rocco Falchetto,Tewis Bouwmeester,Jeffrey A. Porter,Birgit Baumgarten,Keith Mansfield,José M. Carballido,Klaus Seuwen,Frederic Bassilana +28 more
TL;DR: The purification from porcine colonic tissue extracts of an agonistic ligand for GPR15 and its functional characterization identifies a receptor-ligand pair that is required for immune homeostasis at epithelia and whose modulation may represent an alternative approach to treating conditions affecting the skin such as psoriasis.
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Patent
Oxazine derivatives and their use in the treatment of neurological disorders
Sangamesh Badiger,Murali Chebrolu,Mathias Frederiksen,Philipp Holzer,Konstanze Hurth,Lei Li,Hui Liu,Rainer Martin Lueoend,Rainer Machauer,Henrik Moebitz,Ulf Neumann,Rita Ramos,Heinrich Rueeger,Michael Schaefer,Marina Tintelnot-Blomley,Siem Jacob Veenstra,Markus Voegtle,Xin Xiong +17 more
- 13 Jul 2011
TL;DR: In this paper, the oxazine derivatives of formula (I) having BACE inhibitory activity have been defined in free form or in salt form, their preparation methods, their medical use and medicaments comprising them.
55
Patent
Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders
Sangamesh Badiger,Murali Chebrolu,Mathias Frederiksen,Philipp Holzer,Konstanze Hurth,Rainer Martin Lueoend,Rainer Machauer,Henrik Moebitz,Ulf Neumann,Rita Ramos,Heinrich Rueeger,Marina Tintelnot-Blomley,Siem Jacob Veenstra,Markus Voegtle,Michael Schaefer +14 more
- 23 Jul 2010
TL;DR: In this paper, the authors describe a novel heterocyclic compounds of the formula (I) in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, and their medical use as BACE inhibitors for the treatment of Alzheimer and to medicaments comprising them.
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Hemoglobin Bohr effects: atomic origin of the histidine residue contributions.
TL;DR: The contributions to the pKa shift calculated by means of the linear response approximation show that the salt bridge involving His146 plays an important role in the alkaline Bohr effect, as suggested by Perutz but that other interactions are significant as well.
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