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Updated: Jan 2, 2026

MAME Models for 4D Live-cell Imaging of Tumor: Microenvironment Interactions that Impact Malignant Progression
Published on: February 17, 2012
Targeting Tumor Microenvironment by Small-Molecule Inhibitors
Shangwei Zhong1, Ji-Hak Jeong2, Zhikang Chen3
1The Hunan Provincial Key Lab of Precision Diagnosis and Treatment for Gastrointestinal Tumor, Xiangya Hospital, Central South University, Hunan, 410008, China; Department of Molecular Medicine, The Scripps Research Institute, Jupiter, FL 33458, USA.
Abstract:
The tumor microenvironment (TME) is a hypoxic, acidic, and immune/inflammatory cell-enriched milieu that plays crucial roles in tumor development, growth, progression, and therapy resistance. Targeting TME is an attractive strategy for the treatment of solid tumors. Conventional cancer chemotherapies are mostly designed to directly kill cancer cells, and the effectiveness is always compromised by their penetration and accessibility to cancer cells. Small-molecule inhibitors, which exhibit good penetration and accessibility, are widely studied, and many of them have been successfully applied in clinics for cancer treatment. As TME is more penetrable and accessible than tumor cells, a lot of efforts have recently been made to generate small-molecule inhibitors that specifically target TME or the components of TME or develop special drug-delivery systems that release the cytotoxic drugs specifically in TME. In this review, we briefly summarize the recent advances of small-molecule inhibitors that target TME for the tumor treatment.
Insights
Targeting the tumor microenvironment (TME) with small-molecule inhibitors offers a promising strategy for cancer treatment. These inhibitors show improved penetration and accessibility, enhancing efficacy against solid tumors.
Area of Science:
- Oncology
- Pharmacology
Background:
- The tumor microenvironment (TME) is characterized by hypoxia, acidity, and immune cell infiltration, significantly influencing tumor progression and treatment resistance.
- Conventional chemotherapy often struggles with penetration and accessibility to cancer cells within the TME.
- Targeting the TME presents a viable strategy for improving solid tumor treatment outcomes.
Purpose of the Study:
- To review recent advancements in small-molecule inhibitors designed to target the TME for cancer therapy.
- To highlight strategies focusing on TME-specific targeting or drug delivery systems.
Main Methods:
- Literature review of recent research on small-molecule inhibitors and TME-targeting strategies.
- Analysis of studies focusing on drug penetration, accessibility, and TME component targeting.
Main Results:
- Small-molecule inhibitors demonstrate superior penetration and accessibility compared to conventional chemotherapies.
- Emerging strategies involve developing inhibitors that specifically target TME components or utilize TME-responsive drug delivery systems.
Conclusions:
- Small-molecule inhibitors targeting the TME represent a significant advancement in cancer treatment.
- Further research into TME-specific therapies holds great potential for overcoming treatment resistance and improving patient outcomes.
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