The Nuclear Transport Protein Importin-5: A Promising Target in Oncology and Virology

Autor: Rémi Patouret

Publikováno v: CHIMIA, Vol 75, Iss 4, Pp 319-322 (2021)

Cellular homeostasis importantly relies on the correct nucleoplasmic distribution of a large number of RNA molecules and proteins, which are shuttled by specialized transport receptors. The nuclear import receptor importin-5, also called IPO5, RanBP5

Externí odkaz: https://doaj.org/article/a2d86a5cddae47b0bca044222ea64409

HDX-MS reveals structural determinants for RORγ hyperactivation by synthetic agonists

Autor: Timothy S Strutzenberg, Ruben D Garcia-Ordonez, Scott J Novick, HaJeung Park, Mi Ra Chang, Christelle Doebellin, Yuanjun He, Rémi Patouret, Theodore M Kamenecka, Patrick R Griffin

Publikováno v: eLife, Vol 8 (2019)

Members of the nuclear receptor (NR) superfamily regulate both physiological and pathophysiological processes ranging from development and metabolism to inflammation and cancer. Synthetic small molecules targeting NRs are often deployed as therapeuti

Externí odkaz: https://doaj.org/article/7598ee1869b74d83a7b3c7b8c0a9b36c

HDX-MS reveals structural determinants for RORγ hyperactivation by synthetic agonists

Autor: HaJeung Park, Theodore M. Kamenecka, Timothy S. Strutzenberg, Patrick R. Griffin, Scott J. Novick, Ruben D. Garcia-Ordonez, Christelle Doebellin, Yuanjun He, Mi Ra Chang, Rémi Patouret

Publikováno v: eLife
eLife, Vol 8 (2019)

Members of the nuclear receptor (NR) superfamily regulate both physiological and pathophysiological processes ranging from development and metabolism1 to inflammation2 and cancer3. As ligand-gated transcription factors, synthetic small molecules targ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b52a22f3dc0c32b6255b7e27bdc41dbb

Identification of potent RORβ modulators: Scaffold variation

Autor: Scott J. Novick, Ruben D. Garcia-Ordonez, Mi Ra Chang, Venkatasubramanian Dharmarajan, Sean Campbell, Rémi Patouret, Anthony Ciesla, Theodore M. Kamenecka, Laura A. Solt, Patrick R. Griffin, Christelle Doebelin

Publikováno v: Bioorganicmedicinal chemistry letters. 28(19)

We sought to develop RORβ-selective probe molecules in order to investigate the function of the receptor in vitro and in vivo and its role in the pathophysiology of disease. To accomplish this, we modified a potent dual RORβ/RORγ inverse agonist f

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::95debe5d3c8c2418a75e2024fc194c33
https://pubmed.ncbi.nlm.nih.gov/30143422

Substituted α-mercaptoketones, new types of specific neprilysin inhibitors

Autor: Simon Leiris, Rémi Patouret, Marie-Claude Fournie-Zaluski, Tanja Ouimet, Hervé Poras, Bernard P. Roques

Publikováno v: Bioorganic & Medicinal Chemistry Letters
Bioorganic & Medicinal Chemistry Letters, 2017, 27 (16), pp.3883-3890. ⟨10.1016/j.bmcl.2017.06.050⟩

International audience; New neprilysin inhibitors containing an alpha-mercaptoketone HSC((RR2)-R-1)CO group, as zinc ligand were designed. Two parameters were explored for potency optimization: the size of the inhibitor which could interact with the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9411e861939bab86b816c14d00b9419
https://pubmed.ncbi.nlm.nih.gov/28676269