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Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor.
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.
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: bissegger l.
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.
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A high affinity pan-PI3K binding module supports selective targeted protein degradation of PI3Kα.
Jauslin WT, Schild M, Schaefer T, Borsari C, Orbegozo C, Bissegger L, Zhanybekova S, Ritz D, Schmidt A, Wymann M, Gillingham D.
Jauslin WT, et al. Among authors: bissegger l.
Chem Sci. 2023 Dec 12;15(2):683-691. doi: 10.1039/d3sc04629j. eCollection 2024 Jan 3.
Chem Sci. 2023.
PMID: 38179525
Free PMC article.
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Correction: A high affinity pan-PI3K binding module supports selective targeted protein degradation of PI3Kα.
Jauslin WT, Schild M, Schaefer T, Borsari C, Orbegozo C, Bissegger L, Zhanybekova S, Ritz D, Schmidt A, Wymann M, Gillingham D.
Jauslin WT, et al. Among authors: bissegger l.
Chem Sci. 2024 Jan 15;15(4):1520. doi: 10.1039/d4sc90011a. eCollection 2024 Jan 24.
Chem Sci. 2024.
PMID: 38274068
Free PMC article.
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