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Updated: Jan 3, 2026

A Real-time Potency Assay for Chimeric Antigen Receptor T Cells Targeting Solid and Hematological Cancer Cells
Published on: November 12, 2019
Targeting CXCR1/2: The medicinal potential as cancer immunotherapy agents, antagonists research highlights and
Jinxin Che1, Rui Song2, Binhui Chen1
1ZJU-ENS Joint Laboratory of Medicinal Chemistry, Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, Hangzhou Institute of Innovative Medicine, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.
Abstract:
Immune suppression in the tumor microenvironment (TME) is an intractable issue in anti-cancer immunotherapy. The chemokine receptors CXCR1 and CXCR2 recruit immune suppressive cells such as the myeloid derived suppressor cells (MDSCs) to the TME. Therefore, CXCR1/2 antagonists have aroused pharmaceutical interest in recent years. In this review, the medicinal chemistry of CXCR1/2 antagonists and their relevance in cancer immunotherapy have been summarized. The development of the drug candidates, along with their design rationale, clinical status and current challenges have also been discussed.
Insights
Targeting CXCR1/2 receptors can overcome immune suppression in the tumor microenvironment (TME). This review details CXCR1/2 antagonists for cancer immunotherapy, discussing drug development, clinical progress, and challenges.
Area of Science:
- Oncology
- Immunology
- Medicinal Chemistry
Background:
- Tumor microenvironment (TME) immune suppression hinders anti-cancer immunotherapy effectiveness.
- Chemokine receptors CXCR1 and CXCR2 mediate the recruitment of immunosuppressive myeloid-derived suppressor cells (MDSCs) to the TME.
Purpose of the Study:
- To review the medicinal chemistry of CXCR1/2 antagonists.
- To summarize their relevance and development in cancer immunotherapy.
- To discuss clinical status and challenges.
Main Methods:
- Literature review of CXCR1/2 antagonists.
- Analysis of medicinal chemistry strategies.
- Evaluation of clinical trial data.
Main Results:
- CXCR1/2 antagonists represent a promising therapeutic strategy.
- Several drug candidates have advanced in development.
- Understanding design rationale is key to overcoming challenges.
Conclusions:
- CXCR1/2 antagonists offer a viable approach to reversing TME-mediated immune suppression.
- Further development is warranted to address clinical challenges and optimize efficacy.
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