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There are four subtypes of adenosine receptors (ARs), named A₁, A_2A, A_2B and A₃, all of which are G protein-coupled receptors (GPCRs). Locally produced adenosine is a suppressant in anti-tumor immune surveillance. The A_2BAR, coupled to both Gαs and Gαi G proteins, is one of the several GPCRs that are expressed in a significantly higher level in certain cancer tissues, in comparison to adjacent normal tissues. There is growing evidence that the A_2BAR plays an important role in tumor cell proliferation, angiogenesis, metastasis, and immune suppression. Thus, A_2BAR antagonists are novel, potentially attractive anticancer agents. Several antagonists targeting A_2BAR are currently in clinical trials for various types of cancers. In this review, we first describe the signaling, agonists, and antagonists of the A_2BAR. We further discuss the role of the A_2BAR in the progression of various cancers, and the rationale of using A_2BAR antagonists in cancer therapy.