High Throughput Screening for Drug Discovery of Autophagy Modulators

Author(s): Chih-Wen Shu, Pei-Feng Liu, Chun-Ming Huang

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Volume 15 , Issue 9 , 2012

Become EABM
Become Reviewer

Abstract:

Autophagy is an evolutionally conserved process in cells for cleaning abnormal proteins and organelles in a lysosome dependent manner. Growing studies have shown that defects or induced autophagy contributes to many diseases including aging, neurodegeneration, pathogen infection, and cancer. However, the precise involvement of autophagy in health and disease remains controversial because the theories are built on limited assays and chemical modulators, indicating that the role of autophagy in diseases may require further verification. Many food and drug administration (FDA) approved drugs modulate autophagy signaling, suggesting that modulation of autophagy with pharmacological agonists or antagonists provides a potential therapy for autophagy-related diseases. This suggestion raises an attractive issue on drug discovery for exploring chemical modulators of autophagy. High throughput screening (HTS) is becoming a powerful tool for drug discovery that may accelerate screening specific autophagy modulators to clarify the role of autophagy in diseases. Herein, this review lays out current autophagy assays to specifically measure autophagy components such as LC3 (mammalian homologue of yeast Atg8) and Atg4. These assays are feasible or successful for HTS with certain chemical libraries, which might be informative for this intensively growing field as research tools and hopefully developing new drugs for autophagy-related diseases.

Keywords: Autophagy, drug discovery, high throughput screening, chemical modulators, pharmacological agonists, assay development, Atg4, LC3, mammalian homologue, antagonists

Rights & PermissionsPrintExport Cite as

Article Details

VOLUME: 15
ISSUE: 9
Year: 2012
Page: [721 - 729]
Pages: 9
DOI: 10.2174/138620712803519734
Price: $65

Article Metrics

PDF: 51