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Modulation of autophagy by the novel mitochondrial complex I inhibitor Authipyrin.

Abstract：

:Autophagy ensures cellular homeostasis by the degradation of long-lived proteins, damaged organelles and pathogens. This catabolic process provides essential cellular building blocks upon nutrient deprivation. Cellular metabolism, especially mitochondrial respiration, has a significant influence on autophagic flux, and complex I function is required for maximal autophagy. In Parkinson's disease mitochondrial function is frequently impaired and autophagic flux is altered. Thus, dysfunctional organelles and protein aggregates accumulate and cause cellular damage. In order to investigate the interdependency between mitochondrial function and autophagy, novel tool compounds are required. Herein, we report the discovery of a structurally novel autophagy inhibitor (Authipyrin) using a high content screening approach. Target identification and validation led to the discovery that Authipyrin targets mitochondrial complex I directly, leading to the potent inhibition of mitochondrial respiration as well as autophagy.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Kaiser N,Corkery D,Wu Y,Laraia L,Waldmann H

doi

10.1016/j.bmc.2019.02.028

subject

Has Abstract

pub_date

2019-06-15 00:00:00

pages

2444-2448

issue

12

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(19)30139-7

journal_volume

27

pub_type

杂志文章

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