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Covalent Proximity Scanning of a Distal Cysteine to Target PI3Kα.
Borsari C, Keles E, McPhail JA, Schaefer A, Sriramaratnam R, Goch W, Schaefer T, De Pascale M, Bal W, Gstaiger M, Burke JE, Wymann MP. Borsari C, et al. Among authors: de pascale m. J Am Chem Soc. 2022 Apr 13;144(14):6326-6342. doi: 10.1021/jacs.1c13568. Epub 2022 Mar 30. J Am Chem Soc. 2022. PMID: 35353516 Free PMC article.
4-(Difluoromethyl)-5-(4-((3R,5S)-3,5-dimethylmorpholino)-6-((R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders.
Borsari C, Keles E, Rageot D, Treyer A, Bohnacker T, Bissegger L, De Pascale M, Melone A, Sriramaratnam R, Beaufils F, Hamburger M, Hebeisen P, Löscher W, Fabbro D, Hillmann P, Wymann MP. Borsari C, et al. Among authors: de pascale m. J Med Chem. 2020 Nov 25;63(22):13595-13617. doi: 10.1021/acs.jmedchem.0c00620. Epub 2020 Nov 9. J Med Chem. 2020. PMID: 33166139 Free article.
Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor.
De Pascale M, Bissegger L, Tarantelli C, Beaufils F, Prescimone A, Mohamed Seid Hedad H, Kayali O, Orbegozo C, Raguž L, Schaefer T, Hebeisen P, Bertoni F, Wymann MP, Borsari C. De Pascale M, et al. Eur J Med Chem. 2023 Feb 15;248:115038. doi: 10.1016/j.ejmech.2022.115038. Epub 2022 Dec 28. Eur J Med Chem. 2023. PMID: 36634458 Free article.
Synthesis of Pyridoclax Analogues: Insight into Their Druggability by Investigating Their Physicochemical Properties and Interactions with Membranes.
De Pascale M, Iacopetta D, Since M, Corvaisier S, Vie V, Paboeuf G, Hennequin D, Perato S, De Giorgi M, Sinicropi MS, Sopkova-De Oliveira Santos J, Voisin-Chiret AS, Malzert-Freon A. De Pascale M, et al. Among authors: de giorgi m. ChemMedChem. 2020 Jan 7;15(1):136-154. doi: 10.1002/cmdc.201900542. Epub 2019 Nov 26. ChemMedChem. 2020. PMID: 31743599 Free article.
Structure-guided design of pyridoclax derivatives based on Noxa / Mcl-1 interaction mode.
Hedir S, De Giorgi M, Fogha J, De Pascale M, Weiswald LB, Brotin E, Marekha B, Denoyelle C, Denis C, Suzanne P, Gautier F, Juin P, Ligat L, Lopez F, Carlier L, Legay R, Bureau R, Rault S, Poulain L, Oliveira Santos JS, Voisin-Chiret AS. Hedir S, et al. Among authors: de pascale m, de giorgi m. Eur J Med Chem. 2018 Nov 5;159:357-380. doi: 10.1016/j.ejmech.2018.10.003. Epub 2018 Oct 4. Eur J Med Chem. 2018. PMID: 30308410
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