Molecular Design in Practice: A Review of Selected Projects in a French Research Institute That Illustrates the Link between Chemical Biology and Medicinal Chemistry

Autor: Benoit Deprez, Damien Bosc, Julie Charton, Cyril Couturier, Rebecca Deprez-Poulain, Marion Flipo, Florence Leroux, Baptiste Villemagne, Nicolas Willand

Publikováno v: Molecules, Vol 26, Iss 19, p 6083 (2021)

Chemical biology and drug discovery are two scientific activities that pursue different goals but complement each other. The former is an interventional science that aims at understanding living systems through the modulation of its molecular compone

Externí odkaz: https://doaj.org/article/3139cdf061794c5db887520979edb00b

Identification of indole-based activators of insulin degrading enzyme

Autor: Julie Charton, Clara Maillard, Chau Phi Dinh, Adrien Herledan, Florence Leroux, Catherine Piveteau, Benoit Deprez, Isabelle Duplan, Nicolas Kraupner, Nathalie Hennuyer, Xiaoan Wen, Rebecca Deprez-Poulain, Damien Bosc, Sandrine Warenghem, Bart Staels, Valérie Landry

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, 2021, pp.113982. ⟨10.1016/j.ejmech.2021.113982⟩
European Journal of Medicinal Chemistry, Elsevier, 2021, pp.113982. ⟨10.1016/j.ejmech.2021.113982⟩

International audience; Insulin degrading enzyme (IDE) is a zinc metalloprotease that cleaves numerous substrates among which amyloid-β and insulin. It has been linked through genetic studies to the risk of type-2 diabetes (T2D) or Alzheimer's disea

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15ed5fe0bfb1f46856b4bc660d9fb3a7
https://hal.science/hal-03430475

Multi-Component Reaction for the Preparation of 1,5-Disubstituted 1,2,3-Triazoles by In-Situ Generation of Azides and Nickel-Catalyzed Azide-Alkyne Cycloaddition

Autor: Damien Bosc, Nour Bou Karroum, Nicolas Kraupner, Rebecca Deprez-Poulain, Virgyl Camberlein, Emmanuelle Lipka, Benoit Deprez

Publikováno v: Tetrahedron Letters
Tetrahedron Letters, Elsevier, In press, ⟨10.1016/j.tetlet.2021.153131⟩
Tetrahedron Letters, In press, ⟨10.1016/j.tetlet.2021.153131⟩

International audience; An efficient one-pot procedure combining bromide conversion into azide followed by NiAAC for the preparation of 1,5-disubstituted 1,2,3-triazoles has been developed. This procedure prevents the use of isolated azides, which ar

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4073d9cbef3a3c5810b360cb55da35f4
https://hal.archives-ouvertes.fr/hal-03207833/file/Bosc_TetLett_revised.pdf

Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening

Autor: Valérie Landry, Valentin Guillaume, Julie Charton, Florence Leroux, Wei-Jen Tang, Terence Beghyn, Sandrine Warenghem, Wenguang G. Liang, Sarah Urata, Virginie Pottiez, Paul Hermant, Li Sheng, Rebecca Deprez-Poulain, Damien Bosc, Adrien Herledan, Benoit Deprez

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, 2019, 179, pp.557-566. ⟨10.1016/j.ejmech.2019.06.057⟩
European Journal of Medicinal Chemistry, Elsevier, 2019, 179, pp.557-566. ⟨10.1016/j.ejmech.2019.06.057⟩
Eur J Med Chem

International audience; Insulin-degrading enzyme, IDE, is a metalloprotease implicated in the metabolism of key peptides such as insulin, glucagon, β-amyloid peptide. Recent studies have pointed out its broader role in the cell physiology. In order

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3d8372949902200aa76e63f083a7335
https://hal.science/hal-03243182

A new quinoline-based chemical probe inhibits the autophagy-related cysteine protease ATG4B

Autor: Marcel B. Bally, Fan Zhang, Nancy Erro Go, Steven J.M. Jones, Jing Xu, A. M. Hannigan, Lubomir Vezenkov, Courtney Choutka, Kevin C. Yang, R. N. Guay-Ross, S. Loo, Wieslawa H. Dragowska, Damien Bosc, Sharon M. Gorski, Tom A. Pfeifer, Nicolette S. Honson, Suzana Kovacic, Martin E. Gleave, Guoying Chen, Jianghong An, Robert N. Young, Svetlana Bortnik, Ada W. Y. Leung, P. G. K. Clark

Publikováno v: Scientific Reports
Scientific Reports, Vol 8, Iss 1, Pp 1-17 (2018)
Scientific Reports, Nature Publishing Group, 2018, 8 (1), pp.11653. ⟨10.1038/s41598-018-29900-x⟩

The cysteine protease ATG4B is a key component of the autophagy machinery, acting to proteolytically prime and recycle its substrate MAP1LC3B. The roles of ATG4B in cancer and other diseases appear to be context dependent but are still not well under

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ec4c1e5752a839a23a75f0139971545
http://europepmc.org/articles/PMC6076261