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A2B Adenosine Receptor and Cancer

Zhan-Guo Gao1, Kenneth A Jacobson2

  • 1Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA. zg21o@nih.gov.

International Journal of Molecular Sciences
|October 20, 2019
PubMed

Insights

Adenosine receptors (ARs) are GPCRs. Targeting the A2BAR, which is upregulated in cancers, with antagonists may offer a novel anticancer therapy approach by inhibiting tumor progression and immune suppression.

Area of Science:

  • Pharmacology
  • Immunology
  • Oncology

Background:

  • Adenosine receptors (ARs) are G protein-coupled receptors (GPCRs) with four subtypes: A1, A2A, A2B, and A3.
  • Locally produced adenosine suppresses anti-tumor immune surveillance.
  • The A2BAR subtype is significantly overexpressed in various cancer tissues compared to normal tissues.

Purpose of the Study:

  • To review the signaling, agonists, and antagonists of the A2BAR.
  • To discuss the role of A2BAR in cancer progression, including proliferation, angiogenesis, metastasis, and immune suppression.
  • To explore the rationale for using A2BAR antagonists as a potential anticancer therapeutic strategy.

Main Methods:

  • Literature review of A2BAR signaling pathways.
  • Analysis of studies on A2BAR expression in different cancer types.
  • Review of preclinical and clinical data on A2BAR antagonists in cancer therapy.

Main Results:

  • A2BAR plays a critical role in promoting tumor cell proliferation, angiogenesis, metastasis, and immune evasion.
  • A2BAR antagonists have demonstrated potential as anticancer agents in preclinical studies.
  • Several A2BAR antagonists are currently undergoing clinical trials for various cancers.

Conclusions:

  • A2BAR is a promising therapeutic target for cancer treatment.
  • Targeting A2BAR may overcome tumor-induced immune suppression and inhibit cancer progression.
  • A2BAR antagonists represent a novel class of anticancer agents with potential clinical applications.
Keywords:
adenosine receptorcancer therapycell proliferationimmune systemmetastasistumor microenvironment

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