Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 7, Issue 1, Pages 72-76Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00335
Keywords
VPS34; autophagy; phosphoinositide 3-kinase
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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 inhibitors 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.
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