Tumor Immunotherapy Using A_2A Adenosine Receptor Antagonists

• Main Authors: Jinfeng Zhang, Wenzhong Yan, Wenwen Duan, Kurt Wüthrich, Jianjun Cheng
• Format: Article
• Language: English
• Published: MDPI AG 2020-09-01
• Series: Pharmaceuticals
• Subjects: GPCR; immuno-oncology; Parkinson’s disease; drug binding modes; cancer therapy
• Online Access: https://www.mdpi.com/1424-8247/13/9/237
• ISSN: 1424-8247

The A_2A adenosine receptor (A_2AAR) plays critical roles in human physiology and pathophysiology, which makes it an important drug target. Previous drug-discovery efforts targeting the A_2AAR have been focused on the use of A_2AAR antagonists for the treatment of Parkinson’s disease. More recently, the A_2AAR has attracted additional attention for its roles in immuno-oncology, and a number of A_2AAR antagonists are currently used as lead compounds for antitumor drugs in both preclinical models and clinical trials. This review surveys recent advances in the development of A_2AAR antagonists for cancer immunotherapy. The therapeutic potential of representative A_2AAR antagonists is discussed based on both animal efficacy studies and clinical data.