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Small-molecule modulators of tumor immune microenvironment
Jing Zhang1, Jia Yu1, Meijing Liu1
1Institute of Pharmacy and Pharmacology, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hengyang Medical School, University of South China, Hengyang, Hunan 421001, China.
Bioorganic Chemistry
|March 5, 2024
Summary
Small-molecule drugs offer unique advantages in tumor immunotherapy, complementing antibody-based immune checkpoint inhibitors. This review analyzes small-molecule modulators and their structure-activity relationships for novel cancer treatment development.
Area of Science:
- Oncology
- Immunology
- Pharmacology
Background:
- Tumor immunotherapy enhances anti-cancer immune responses and reduces immunosuppression.
- Immune checkpoint blocking (ICB) using monoclonal antibodies (mAbs) is a primary therapeutic strategy.
- Small-molecule drugs present distinct advantages over biologics in cancer immunotherapy.
Purpose of the Study:
- To review the mechanisms of tumor immunotherapy.
- To analyze the current research status of small-molecule immunomodulators.
- To discuss the structure-activity relationships (SAR) of small-molecule drug candidates.
Main Methods:
- Literature review of tumor immunotherapy mechanisms.
- Analysis of research on small-molecule immunomodulators.
- Examination of structure-activity relationships (SAR) for drug design.
Main Results:
- Small-molecule drugs offer unique advantages in tumor immunotherapy.
- Overexpressed immunosuppressive signals (e.g., PD-L1, IDO1, TGF-β) create a tumor immunosuppressive microenvironment.
- Multi-pathway combined immunotherapy shows verified efficacy.
Conclusions:
- Small-molecule modulators are crucial for advancing tumor immunotherapy.
- Understanding SAR is key to designing novel small-molecule immune modulators.
- Further research into small molecules offers new avenues for cancer treatment.
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