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Autophagy. 2013 Apr;9(4):595-603. doi: 10.4161/auto.23641. Epub 2013 Feb 14.

Synthesis and screening of 3-MA derivatives for autophagy inhibitors.

Author information

1
State Key Laboratory of Biomembrane and Membrane Biotechnology, Tsinghua University-Peking University Joint Center for Life Sciences, School of Life Sciences, Tsinghua University, Beijing, China.

Abstract

Autophagy is a conserved degradation process, which plays important pathophysiological roles. The lack of effective inhibitors of autophagy has been an obstacle in both basic research and understanding the physiological role of autophagy in disease manifestation. The most widely used inhibitor, 3-methyladenine (3-MA), is poorly soluble at room temperature and is effective only at high concentrations. In this study, we synthesized a library of small compounds by chemically modifying 3-MA and screened this library for autophagy inhibitors. Three 3-MA derivatives generated through this approach showed improved solubility and effectiveness in inhibiting autophagy. We demonstrated that chemical modification of an existing autophagy inhibitor is an effective method to generate improved autophagy inhibitors.

KEYWORDS:

3-MA; autophagy; derivatives; inhibitor; synthesis

PMID:
23412639
PMCID:
PMC3627673
DOI:
10.4161/auto.23641
[Indexed for MEDLINE]
Free PMC Article

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