M
Michael Hennig
Researcher at Hoffmann-La Roche
Publications - 106
Citations - 5957
Michael Hennig is an academic researcher from Hoffmann-La Roche. The author has contributed to research in topics: Binding site & Carnitine. The author has an hindex of 39, co-authored 102 publications receiving 5451 citations. Previous affiliations of Michael Hennig include University of Cologne & University of Göttingen.
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Journal ArticleDOI
1,3-Disubstituted 4-Aminopiperidines as Useful Tools in the Optimization of the 2-Aminobenzo[A]Quinolizine Dipeptidyl Peptidase Iv Inhibitors.
Thomas Lübbers,Markus Bohringer,Luca Gobbi,Michael Hennig,Daniel Hunziker,Bernd Kuhn,Bernd Michael Löffler,Patrizio Mattei,Robert Narquizian,Jens-Uwe Peters,Yves Ruff,Hans Peter Wessel,Pierre C. Wyss +12 more
TL;DR: In a search for novel DPP-IV inhibitors, 2-aminobenzo[a]quinolizines were identified as submicromolar HTS hits and the developed synthetic methodology and the SAR could be transferred to the 1,3-disubstituted 4-aminopiperidines series, leading to highly active DPP -IV inhibitors.
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Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors.
Markus Boehringer,Holger Fischer,Michael Hennig,Daniel Hunziker,Joerg Huwyler,Bernd Kuhn,Bernd Michael Loeffler,Thomas Luebbers,Patrizio Mattei,Robert Narquizian,Elena Sebokova,Urs Sprecher,Hans Peter Wessel +12 more
TL;DR: Synthesis and SAR are described for a structurally distinct class of DPP-IV inhibitors based on aminobenzo[a]quinolizines bearing (hetero-)aromatic substituents in the S1 specificity pocket that displays excellent in vivo activity and superior drug-like properties.
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Mapping the conformational space accessible to BACE2 using surface mutants and cocrystals with Fab fragments, Fynomers and Xaperones
David Banner,Bernard Gsell,Jörg Benz,Julian Bertschinger,Dominique Burger,Simon Brack,Simon Cuppuleri,Maja Debulpaep,Alain Gast,Dragan Grabulovski,Michael Hennig,Hans Hilpert,Walter Huber,Andreas Kuglstatter,Eric Kusznir,Toon Laeremans,Hugues Matile,Christian Miscenic,Arne C. Rufer,Daniel Schlatter,Jan Steyaert,Martine Stihle,Ralf Thoma,Martin Weber,Armin Ruf +24 more
TL;DR: The different strategies used for raising and selecting BACE2 binders for cocrystallization are described and the crystallization success, crystal quality and the time and resources needed to obtain suitable crystals are compared.
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Novel Hexahydrospiro[piperidine-4,1‘-pyrrolo[3,4-c]pyrroles]: Highly Selective Small-Molecule Nociceptin/Orphanin FQ Receptor Agonists
Sabine Kolczewski,Geo Adam,Cesura Andrea,Francois Jenck,Michael Hennig,Thomas Oberhauser,Sonia Poli,Felix Rössler,Stephan Röver,Jürgen Wichmann,Frank M. Dautzenberg +10 more
TL;DR: Results indicate that (+)-5a is a highly selective and potent small-molecule full agonist of the NOP receptor.
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Structure-Assisted Discovery of an Aminothiazole Derivative as a Lead Molecule for Inhibition of Bacterial Fatty-Acid Synthesis.
TL;DR: A structure-based biophysical screening approach has identified for the first time a synthetic small molecule, 2-phenylamino-4-methyl-5-acetylthiazole, that binds to the active site of the β-Ketoacyl-ACP synthase.