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Potent, selective, and orally bioavailable inhibitors of VPS34 provide chemical tools to modulate autophagy in vivo

Honda, Ayako and Harrington, Edmund and Furet, Pascal and Knapp, Mark and Triantafellow, Ellen and Hamann, Lawrence and Firestone, Brant and Murphy, Leon and Keaney, Erin (2016) Potent, selective, and orally bioavailable inhibitors of VPS34 provide chemical tools to modulate autophagy in vivo. ACS Medicinal Chemistry Letters, 7 (1). pp. 72-76. ISSN 1948-58751948-5875

Abstract

Autophagy is a dynamic process that regulates lysosomal-dependent degradation of cellular components. Until recently the study of autophagy has been hampered by the lack of reliable pharmacological tools but selective inhib-itors are now available to modulate the PI 3-kinase VPS34 which is required for autophagy. Here we describe the discovery of potent and selective VPS34 inhibitors, their pharmacokinetic (PK) properties, and ability to inhibit autophagy in cellular and mouse models.

Item Type: Article
Date Deposited: 26 Apr 2016 23:45
Last Modified: 26 Apr 2016 23:45
URI: https://oak.novartis.com/id/eprint/26727

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