Diversity-oriented synthesis encoded by deoxyoligonucleotides

Autor: Liam Hudson, Jeremy W. Mason, Matthias V. Westphal, Matthieu J. R. Richter, Jonathan R. Thielman, Bruce K. Hua, Christopher J. Gerry, Guoqin Xia, Heather L. Osswald, John M. Knapp, Zher Yin Tan, Praveen Kokkonda, Ben I. C. Tresco, Shuang Liu, Andrew G. Reidenbach, Katherine S. Lim, Jennifer Poirier, John Capece, Simone Bonazzi, Christian M. Gampe, Nichola J. Smith, James E. Bradner, Connor W. Coley, Paul A. Clemons, Bruno Melillo, C. Suk-Yee Hon, Johannes Ottl, Christoph E. Dumelin, Jonas V. Schaefer, Ann Marie E. Faust, Frédéric Berst, Stuart L. Schreiber, Frédéric J. Zécri, Karin Briner

Publikováno v: Nature Communications, Vol 14, Iss 1, Pp 1-15 (2023)

Abstract Diversity-oriented synthesis (DOS) is a powerful strategy to prepare molecules with underrepresented features in commercial screening collections, resulting in the elucidation of novel biological mechanisms. In parallel to the development of

Externí odkaz: https://doaj.org/article/36c9d05209eb47b1b03cc9fce00df87d

Cannabinoid CB2 Receptors Modulate Microglia Function and Amyloid Dynamics in a Mouse Model of Alzheimer’s Disease

Autor: Samuel Ruiz de Martín Esteban, Irene Benito-Cuesta, Itziar Terradillos, Ana M. Martínez-Relimpio, M. Andrea Arnanz, Gonzalo Ruiz-Pérez, Claudia Korn, Catarina Raposo, Roman C. Sarott, Matthias V. Westphal, Izaskun Elezgarai, Erick M. Carreira, Cecilia J. Hillard, Uwe Grether, Pedro Grandes, M. Teresa Grande, Julián Romero

Publikováno v: Frontiers in Pharmacology, Vol 13 (2022)

The distribution and roles of the cannabinoid CB2 receptor in the CNS are still a matter of debate. Recent data suggest that, in addition to its presence in microglial cells, the CB2 receptor may be also expressed at low levels, yet biologically rele

Externí odkaz: https://doaj.org/article/971c3ccb7b28416a96223192611a4cd6

DNA-encoded library (DEL)-enabled discovery of proximity-inducing small molecules

Autor: Jeremy W. Mason, Liam Hudson, Matthias V. Westphal, Antonin Tutter, Gregory Michaud, Wei Shu, Xiaolei Ma, Connor W. Coley, Paul A. Clemons, Simone Bonazzi, Frédéric Berst, Frédéric J. Zécri, Karin Briner, Stuart L. Schreiber

Molecular glues and bifunctional compounds that induce protein–protein associations provide a powerful and general mechanism to modulate cell circuitry. We sought to develop a platform for the direct discovery of compounds able to induce associatio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::353823b77fa8f321be337dcdf45df150
https://doi.org/10.1101/2022.10.13.512184

Water-Compatible Cycloadditions of Oligonucleotide-Conjugated Strained Allenes for DNA-Encoded Library Synthesis

Autor: Karin Briner, Liam Hudson, Johan A Pradeilles, Matthias V Westphal, Jeremy W Mason, Stuart L. Schreiber, Frédéric Zecri

Publikováno v: J Am Chem Soc

DNA-encoded libraries of small molecules are being explored extensively for the identification of binders in early drug-discovery efforts. Combinatorial syntheses of such libraries require water- and DNA-compatible reactions, and the paucity of these

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8f0d19cdfb83e29c8e85a274dcbd595
https://doi.org/10.1021/jacs.9b13186

Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe

Autor: Thais Gazzi, Benjamin Brennecke, Kenneth Atz, Claudia Korn, David Sykes, Gabriel Forn-Cuni, Patrick Pfaff, Roman C. Sarott, Matthias V. Westphal, Yelena Mostinski, Leonard Mach, Malgorzata Wasinska-Kalwa, Marie Weise, Bradley L. Hoare, Tamara Miljuš, Maira Mexi, Nicolas Roth, Eline J. Koers, Wolfgang Guba, André Alker, Arne C. Rufer, Eric A. Kusznir, Sylwia Huber, Catarina Raposo, Elisabeth A. Zirwes, Anja Osterwald, Anto Pavlovic, Svenja Moes, Jennifer Beck, Matthias Nettekoven, Irene Benito-Cuesta, Teresa Grande, Faye Drawnel, Gabriella Widmer, Daniela Holzer, Tom van der Wel, Harpreet Mandhair, Michael Honer, Jürgen Fingerle, Jörg Scheffel, Johannes Broichhagen, Klaus Gawrisch, Julián Romero, Cecilia J. Hillard, Zoltan V. Varga, Mario van der Stelt, Pal Pacher, Jürg Gertsch, Christoph Ullmer, Peter J. McCormick, Sergio Oddi, Herman P. Spaink, Mauro Maccarrone, Dmitry B. Veprintsev, Erick M. Carreira, Uwe Grether, Marc Nazaré

Publikováno v: Gazzi, Thais; Brennecke, Benjamin; Atz, Kenneth; Korn, Claudia; Sykes, David; Forn-Cuni, Gabriel; Pfaff, Patrick; Sarott, Roman C; Westphal, Matthias V; Mostinski, Yelena; Mach, Leonard; Wasinska-Kalwa, Malgorzata; Weise, Marie; Hoare, Bradley L; Miljuš, Tamara; Mexi, Maira; Roth, Nicolas; Koers, Eline J; Guba, Wolfgang; Alker, André; ... (2022). Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe. Chemical Science, 13(19), pp. 5539-5545. The Royal Society of Chemistry 10.1039/d1sc06659e
Chemical Science, 13(19), 5539-5545
Chemical Science

Despite its essential role in the (patho)physiology of several diseases, CB2R tissue expression profiles and signaling mechanisms are not yet fully understood. We report the development of a highly potent, fluorescent CB2R agonist probe employing str

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69e61ac61b6e5b29da1ceeb545f2c056
http://hdl.handle.net/11697/192023