Abstract LBA004: Identification of GSPT1-directed molecular glue degrader (MGD) for the treatment of Myc-driven breast cancer

Autor: Gerald Gavory, Bernhard Fasching, Debora Bonenfant, Amine Sadok, Ambika Singh, Martin Schillo, Vittoria Massafra, Anne-Cecile d’Alessandro, John Castle, Mahmoud Ghandi, Agustin Chicas, Frederic Delobel, Alexander Flohr, Giorgio Ottaviani, Thomas Ryckmans, Anne-Laure Laine, Oliv Eidam, Hannah Wang, Ilona Bernett, Laura Chan, Chiara Gorrini, Theo Roumiliotis, Jyoti Choudhary, Yann-Vai LeBihan, Marc Cabry, Mark Stubbs, Rosemary Burke, Rob Van Montfort, John Caldwell, Rajesh Chopra, Ian Collins, Silvia Buonamici

Publikováno v: Molecular Cancer Therapeutics. 20:LBA004-LBA004

The Myc family of transcription factors is a well-established driver of human cancers. However, despite being amongst the most frequently mutated, translocated and overexpressed oncogenes, no therapy directly targeting the Myc family members has been

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::440831d4043db94d06301e979ed876c1
https://doi.org/10.1158/1535-7163.targ-21-lba004

Covalent Docking of Large Libraries for the Discovery of Chemical Probes

Autor: Lucie Gibold, Kenji Uchida, Richard Bonnet, John J. Irwin, Rand M. Miller, Nir London, Shyam Krishnan, Jack Taunton, Oliv Eidam, Brian K. Shoichet, Peter Cimermancic

Publikováno v: Nature chemical biology
Nature Chemical Biology
Nature Chemical Biology, Nature Publishing Group, 2014, 10 (12), pp.1066-1072. ⟨10.1038/nchembio.1666⟩
Nature Chemical Biology, 2014, 10 (12), pp.1066-1072. ⟨10.1038/nchembio.1666⟩

International audience; Chemical probes that form a covalent bond with a protein target often show enhanced selectivity, potency and utility for biological studies. Despite these advantages, protein-reactive compounds are usually avoided in high-thro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::473495585156175379aa3c7084dd9aeb
http://europepmc.org/articles/PMC4232467

Fragment-guided design of subnanomolar β-lactamase inhibitors active in vivo

Autor: Oliv Eidam, Sarah Barelier, Emilia Caselli, Brian K. Shoichet, Chiara Romagnoli, Fabio Prati, Guillaume Dalmasso, R. Bonnet

Publikováno v: Proceedings of the National Academy of Sciences of the United States of America
Proceedings of the National Academy of Sciences of the United States of America, National Academy of Sciences, 2012, 109 (43), pp.17448-17453. ⟨10.1073/pnas.1208337109⟩
Proceedings of the National Academy of Sciences of the United States of America, vol 109, iss 43
Proceedings of the National Academy of Sciences of the United States of America, 2012, 109 (43), pp.17448-17453. ⟨10.1073/pnas.1208337109⟩

Fragment-based design was used to guide derivatization of a lead series of β-lactamase inhibitors that had heretofore resisted optimization for in vivo activity. X-ray structures of fragments overlaid with the lead suggested new, unanticipated funct

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec4d141dc108ab1d5399214b95935574
https://doi.org/10.1073/pnas.1208337109

Design, Synthesis, Crystal Structures, and Antimicrobial Activity of Sulfonamide Boronic Acids as β-Lactamase Inhibitors

Autor: Oliv Eidam, Kerim Babaoglu, Richard Bonnet, Emilia Caselli, Brian K. Shoichet, Denise Teotico Pohlhaus, Fabio Prati, Joel Karpiak, Chiara Romagnoli

Publikováno v: Journal of Medicinal Chemistry. 53:7852-7863

We investigated a series of sulfonamide boronic acids that resulted from the merging of two unrelated AmpC β-lactamase inhibitor series. The new boronic acids differed in the replacement of the canonical carboxamide, found in all penicillin and ceph

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::48e6aaaa2b14ea4a8cb9eeda868942e6
https://doi.org/10.1021/jm101015z

Homologous ligands accommodated by discrete conformations of a buried cavity

Autor: Oliv Eidam, Matthew Merski, Trent E. Balius, Marcus Fischer, Brian K. Shoichet

Publikováno v: Proceedings of the National Academy of Sciences of the United States of America, vol 112, iss 16

Conformational change in protein–ligand complexes is widely modeled, but the protein accommodation expected on binding a congeneric series of ligands has received less attention. Given their use in medicinal chemistry, there are surprisingly few su

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::29b622ff9f62a76e408431bca6112bdb
https://escholarship.org/uc/item/98j260f3