Related Experiment Video
Updated: Apr 17, 2026

Author Spotlight: A Selective Luciferase-Based Assay for Monitoring ATG4B 27 Activity in Cells
Published on: June 30, 2023
Untangling knots between autophagic targets and candidate drugs, in cancer therapy
Tao Xie1, Si-Jia Li, Ming-Rui Guo
1State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, 610041, China.
Abstract:
Autophagy is an evolutionarily conserved lysosomal mechanism implicated in a wide variety of pathological processes, such as cancer. Autophagy can be regulated by a limited number of autophagy-related genes (Atgs) such as oncogenic Bcl-2/Bcl-XL , mTORC1, Akt and PI3KCI, and tumour suppressive proteins PI3KCIII, Beclin-1, Bif-1, p53, DAPKs, PTEN and UVRAG, which play their crucial roles in regulating autophagy-related cancer. As autophagy has a dual role in cancer cells, with tumour-promoting and tumour-suppressing properties, it has become an attractive target for a series of emerging small molecule drugs. In this review, we reveal new discoveries of related small molecules or chemical compounds that can regulate autophagic pathways and lead to pro-death or pro-survival autophagy, in different types of cancer. We discuss the knots between autophagic targets and candidate drugs, in the hope of shedding new light on exploiting new anti-tumour small molecule drugs for future cancer therapy.
Insights
Autophagy, a cellular process, plays a dual role in cancer. This review explores small molecules targeting autophagy for novel anti-cancer drug development.
Area of Science:
- Molecular Biology
- Cell Biology
- Oncology
Background:
- Autophagy is a conserved lysosomal degradation pathway crucial in cellular homeostasis.
- Dysregulation of autophagy is implicated in various pathologies, notably cancer.
- Key autophagy-related genes (Atgs) and regulatory proteins influence cancer development.
Purpose of the Study:
- To review recent discoveries of small molecules modulating autophagy in cancer.
- To explore the dual role of autophagy (tumor-promoting and tumor-suppressing) in cancer cells.
- To identify potential therapeutic strategies targeting autophagy for cancer treatment.
Main Methods:
- Literature review of small molecules and chemical compounds affecting autophagy.
- Analysis of regulatory pathways involving oncogenes, tumor suppressors, and autophagy.
- Discussion of the link between autophagic targets and drug candidates.
Main Results:
- Small molecules can induce either pro-death or pro-survival autophagy.
- Autophagy's role in cancer is context-dependent, offering therapeutic opportunities.
- Specific molecular targets within autophagy pathways are being identified for drug development.
Conclusions:
- Targeting autophagy with small molecules presents a promising avenue for anti-cancer drug discovery.
- Understanding the intricate regulation of autophagy is key to developing effective cancer therapies.
- Further research into the interplay between autophagy and candidate drugs can illuminate new treatment strategies.
Related Concept Videos
Targeted Cancer Therapies
There are several types of targeted therapies against...
Targeted Cancer Therapies
Autophagy
An autophagic pathway consists of a series of signaling events activated in response to diverse stress and physiological conditions such as food deprivation,...
Delivery Pathways to the Lysosome
Endocytosis
In endocytosis, the cell membrane takes up macromolecules and particles from the surrounding medium. Clathrin-mediated...
Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Autophagic Cell Death
Autophagy and Apoptosis
Autophagy can activate apoptosis. In normal conditions, the autophagy activating protein Beclin-1 and...

