Small molecular CD73 inhibitors: Recent progress and future perspectives

• Published in: European journal of medicinal chemistry Vol. 264; p. 116028
• Main Authors: Ge, Gong-Hui, Wang, Qiu-Yin, Zhang, Zhen-Hao, Zhang, Xu, Guo, Shuai, Zhang, Ting-Jian, Meng, Fan-Hao
• Format: Journal Article
• Language: English
• Published: France 15.01.2024
• Subjects: 5'-Nucleotidase; Adenosine - metabolism; Adenosine - pharmacology; Antineoplastic Agents - pharmacology; Humans; Immunosuppressive Agents; Neoplasms - metabolism; Receptors, Purinergic P1; Tumor Microenvironment; Adenosine; CD73; Structure-activity relationship
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2023.116028

The occurrence and development of the tumor are very complex biological processes. In recent years, a large number of research data shows that CD73 is closely related to tumor growth and metastasis. It has been confirmed that the cascade hydrolysis of extracellular ATP to adenosine is one of the most important immunosuppressive regulatory pathways in the tumor microenvironment. The metabolite adenosine can mediate immunosuppression by activating adenosine receptor (such as A ) on effector Immune cells and enable tumor cells to achieve immune escape. Therefore, attenuating or completely removing adenosine-mediated immunosuppression in the tumor microenvironment by inhibiting CD73 is a promising approach in the treatment of solid tumors. This paper focuses on the research progress of CD73 enzyme and CD73 small molecule inhibitors, and is expected to provide some insights into the development of small-molecule antitumor drugs targeting CD73.