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Updated: Jul 24, 2025

A Comprehensive Procedure to Evaluate the In Vivo Performance of Cancer Nanomedicines
Published on: March 4, 2017
Autophagy inhibitors for cancer therapy: Small molecules and nanomedicines
Jian-Li Chen1, Xuan Wu1, Dan Yin1
1State Key Laboratory of Quality Research in Chinese Medicine, Macau Institute for Applied Research in Medicine and Health, Macau University of Science and Technology, Taipa, Macau SAR, China.
Abstract:
Autophagy is a conserved process in which the cytosolic materials are degraded and eventually recycled for cellular metabolism to maintain homeostasis. The dichotomous role of autophagy in pathogenesis is complicated. Accumulating reports have suggested that cytoprotective autophagy is responsible for tumor growth and progression. Autophagy inhibitors, such as chloroquine (CQ) and hydroxychloroquine (HCQ), are promising for treating malignancies or overcoming drug resistance in chemotherapy. With the rapid development of nanotechnology, nanomaterials also show autophagy-inhibitory effects or are reported as the carriers delivering autophagy inhibitors. In this review, we summarize the small-molecule compounds and nanomaterials inhibiting autophagic flux as well as the mechanisms involved. The nanocarrier-based drug delivery systems for autophagy inhibitors and their distinct advantages are also described. The progress of autophagy inhibitors for clinical applications is finally introduced, and their future perspectives are discussed.
Insights
Autophagy, a cellular recycling process, plays a complex role in disease. This review covers autophagy inhibitors, including small molecules and nanomaterials, for cancer therapy and drug resistance.
Area of Science:
- Cell Biology
- Biochemistry
- Oncology
Background:
- Autophagy is a fundamental cellular process for degrading and recycling cytoplasmic components, crucial for maintaining cellular homeostasis.
- The role of autophagy in disease, particularly cancer, is complex, with cytoprotective autophagy often promoting tumor growth and progression.
- Autophagy inhibitors like chloroquine (CQ) and hydroxychloroquine (HCQ) show promise in cancer treatment and overcoming chemotherapy resistance.
Purpose of the Study:
- To review small-molecule compounds and nanomaterials that inhibit autophagic flux.
- To describe the mechanisms by which these agents affect autophagy.
- To discuss nanocarrier-based drug delivery systems for autophagy inhibitors and their clinical applications and future perspectives.
Main Methods:
- Literature review of small-molecule compounds and nanomaterials with autophagy-inhibitory effects.
- Analysis of mechanisms underlying autophagy inhibition by various agents.
- Examination of nanocarrier systems for delivering autophagy inhibitors.
- Review of current clinical progress and future outlook for autophagy inhibitors in cancer therapy.
Main Results:
- Small molecules (e.g., CQ, HCQ) and various nanomaterials can inhibit autophagic flux.
- Nanomaterials can act as direct inhibitors or as effective carriers for autophagy inhibitors.
- Nanocarrier-based delivery systems offer advantages for enhancing the efficacy and targeting of autophagy inhibitors.
Conclusions:
- Autophagy inhibition is a viable strategy for cancer treatment and overcoming drug resistance.
- Nanotechnology offers novel approaches for developing and delivering autophagy inhibitors.
- Further research and clinical trials are needed to fully realize the therapeutic potential of autophagy inhibitors.
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