Small molecule inhibitors of fungal Δ(9) fatty acid desaturase as antifungal agents against Candida auris

Autor: Faiza Tebbji, Anagha C. T. Menon, Inès Khemiri, Daniel J. St-Cyr, Louis Villeneuve, Antony T. Vincent, Adnane Sellam

Publikováno v: Frontiers in Cellular and Infection Microbiology, Vol 14 (2024)

Candida auris has emerged as a significant healthcare-associated pathogen due to its multidrug-resistant nature. Ongoing constraints in the discovery and provision of new antifungals create an urgent imperative to design effective remedies to this pr

Externí odkaz: https://doaj.org/article/73cef9d33bd7416eadc09e75b2872689

Probing Anti-inflammatory Properties Independent of NF-κB Through Conformational Constraint of Peptide-Based Interleukin-1 Receptor Biased Ligands

Autor: Azade Geranurimi, Colin W. H. Cheng, Christiane Quiniou, Tang Zhu, Xin Hou, José Carlos Rivera, Daniel J. St-Cyr, Kim Beauregard, Vadim Bernard-Gauthier, Sylvain Chemtob, William D. Lubell

Publikováno v: Frontiers in Chemistry, Vol 7 (2019)

Interleukin-1β (IL-1β) binds to the IL-1 receptor (IL-1R) and is a key cytokine mediator of inflammasome activation. IL-1β signaling leads to parturition in preterm birth (PTB) and contributes to the retinal vaso-obliteration characteristic of oxy

Externí odkaz: https://doaj.org/article/edf58270e86449f8bba2c5225df6cecb

Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4

Autor: Chetan K. Chana, Pierre Maisonneuve, Ganna Posternak, Nicolas G.A. Grinberg, Juline Poirson, Samara M. Ona, Derek F. Ceccarelli, Pavel Mader, Daniel J. St-Cyr, Victor Pau, Igor Kurinov, Xiaojing Tang, Dongjing Deng, Weiren Cui, Wenji Su, Letian Kuai, Richard Soll, Mike Tyers, Hannes L. Röst, Robert A. Batey, Mikko Taipale, Anne-Claude Gingras, Frank Sicheri

Publikováno v: Journal of Medicinal Chemistry. 65:12725-12746

Targeted protein degradation (TPD) strategies exploit bivalent small molecules to bridge substrate proteins to an E3 ubiquitin ligase to induce substrate degradation. Few E3s have been explored as degradation effectors due to a dearth of E3-binding s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e9bd44e2ad315c9a8487c6d1e86a88a
https://doi.org/10.1021/acs.jmedchem.2c00509

Head-to-tail cyclization of side chain-protected linear peptides to recapitulate genetically-encoded cyclized peptides

Autor: Samir Bouayad‐Gervais, Daniel J. St‐Cyr, Mathieu Courcelles, Éric Bonneil, Florence H. Gohard, Pierre Thibault, William C. Earnshaw, Mike Tyers

Publikováno v: Bouayad Gervais, S, St-Cyr, D J, Courcelles, M, Bonneil, É, Gohard, F, Thibault, P, Earnshaw, W C & Tyers, M 2022, ' Head-to-tail cyclization of side chain-protected linear peptides to recapitulate genetically-encoded cyclized peptides ', Peptide Science, vol. 114, no. 3, e24254 . https://doi.org/10.1002/pep2.24254

Genetically-encoded cyclic peptide libraries allow rapid in vivo screens for inhibitors of any target protein of interest. In particular, the Split Intein Circular Ligation of Protein and Peptides (SICLOPPS) system exploits spontaneous protein splici

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ad92d8339c869333e6076dad0bae100
https://pubmed.ncbi.nlm.nih.gov/35864841

E2 enzyme inhibition by stabilization of a low-affinity interface with ubiquitin

Autor: Frank Sicheri, Anne Marinier, Stephen Orlicky, Sachdev S. Sidhu, Mike Tyers, Hao Huang, Derek F. Ceccarelli, Pankaj Garg, Amy Ziemba, Serge Plamondon, Daniel J. St-Cyr, Gary Kleiger, Manfred Auer

Publikováno v: Nature chemical biology
Nature Chemical Biology

Weak protein interactions between ubiquitin and the ubiquitin-proteasome system (UPS) enzymes that mediate its covalent attachment to substrates serve to position ubiquitin for optimal catalytic transfer. We show that a small molecule inhibitor of th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f1bedc9c8886ba2ff9f4214a09b599f6
https://doi.org/10.1038/nchembio.1412