M
Matthias Westphal
Researcher at ETH Zurich
Publications - 17
Citations - 316
Matthias Westphal is an academic researcher from ETH Zurich. The author has contributed to research in topics: Biology & Cannabinoid receptor. The author has an hindex of 5, co-authored 13 publications receiving 209 citations. Previous affiliations of Matthias Westphal include Hoffmann-La Roche.
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Journal ArticleDOI
Evaluation of tert-Butyl Isosteres: Case Studies of Physicochemical and Pharmacokinetic Properties, Efficacies, and Activities
TL;DR: In this paper, physicochemical data of two series of drug analogues of bosentan and vercirnon are documented as part of a comparative study of tert-butyl, pentafluorosulfanyl, trifluoromethyl, bicyclo[1.1]pentanyl, and cyclopropyl-trifluorsulfyl substituents.
Journal ArticleDOI
Synthesis of Photoswitchable Δ9-Tetrahydrocannabinol Derivatives Enables Optical Control of Cannabinoid Receptor 1 Signaling
Matthias Westphal,Michael A. Schafroth,Roman C. Sarott,Michael A. Imhof,Christian P. Bold,Philipp Leippe,Amey Dhopeshwarkar,Jessica M. Grandner,Vsevolod Katritch,Ken Mackie,Dirk Trauner,Dirk Trauner,Erick M. Carreira,James A. Frank +13 more
TL;DR: Efficient asymmetric syntheses of four photoswitchable Δ9-tetrahydrocannabinol derivatives (azo-THCs) from a central building block 3-Br-THC enable CB1-mediated optical control of inwardly rectifying potassium channels, as well as adenylyl cyclase.
Journal ArticleDOI
Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CB2 Receptor Expression and Ligand Engagement in Human Cells
Marjolein Soethoudt,Sara C. Stolze,Matthias Westphal,Luuk van Stralen,Andrea Martella,Eva J. van Rooden,Wolfgang Guba,Zoltán Varga,Hui Deng,Sander I. van Kasteren,Uwe Grether,Adriaan P. IJzerman,Pal Pacher,Erick M. Carreira,Herman S. Overkleeft,Andreea Ioan-Facsinay,Laura H. Heitman,Mario van der Stelt +17 more
TL;DR: The development of LEI121 as a photoreactive probe to study the type 2 cannabinoid receptor (CB2R), a promising GPCR to treat tissue injury and inflammatory diseases and hold promise as biomarkers in translational drug discovery is reported.
Journal ArticleDOI
Development of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells
Roman C. Sarott,Matthias Westphal,Patrick Pfaff,Claudia Korn,David A. Sykes,David A. Sykes,Thais Gazzi,Benjamin Brennecke,Kenneth Atz,Marie Weise,Yelena Mostinski,Pattarin Hompluem,Pattarin Hompluem,Eline J. Koers,Eline J. Koers,Tamara Miljuš,Tamara Miljuš,Nicolas J. Roth,Hermon Asmelash,Man C Vong,Man C Vong,Jacopo Piovesan,Jacopo Piovesan,Wolfgang Guba,Arne C. Rufer,Eric Kusznir,Sylwia Huber,Catarina Raposo,Elisabeth A. Zirwes,Anja Osterwald,Anto Pavlovic,Svenja Moes,Jennifer Beck,Irene Benito-Cuesta,Teresa Grande,Samuel Ruiz de Martín Esteban,Alexei Yeliseev,Faye M. Drawnel,Gabriella Widmer,Daniela Holzer,Tom van der Wel,Harpreet Mandhair,Cheng-Yin Yuan,William R. Drobyski,Yurii Saroz,Natasha L. Grimsey,Michael Honer,Jürgen Fingerle,Klaus Gawrisch,Julián Romero,Cecilia J. Hillard,Zoltán Varga,Zoltán Varga,Mario van der Stelt,Pal Pacher,Jürg Gertsch,Peter J. McCormick,Christoph Ullmer,Sergio Oddi,Mauro Maccarrone,Dmitry B. Veprintsev,Dmitry B. Veprintsev,Marc Nazaré,Uwe Grether,Erick M. Carreira +64 more
TL;DR: A versatile ligand platform for the modular design of a collection of highly specific CB2R fluorescent probes, used successfully across ap-plications, species and cell types are reported for the first time.
Journal ArticleDOI
Highly Selective, Amine-Derived Cannabinoid Receptor 2 Probes.
Matthias Westphal,Roman C. Sarott,Elisabeth A. Zirwes,Anja Osterwald,Wolfgang Guba,Christoph Ullmer,Uwe Grether,Erick M. Carreira +7 more
TL;DR: The design and synthesis of CB2 R-selective cannabinoids along with their in vitro pharmacological characterization (binding and functional studies) are reported, which combine structural features of HU-308 and AM841 to give chimeric ligands that emerge as potentCB2 R agonists with high selectivity over the closely related cannabinoid receptor 1 (CB1 R).