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Updated: Feb 3, 2026

Surface-enhanced Resonance Raman Scattering Nanoprobe Ratiometry for Detecting Microscopic Ovarian Cancer via Folate Receptor Targeting
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Targeting adenosine A2A receptor antagonism for treatment of cancer

Miles Congreve1, Giles A Brown1, Alexandra Borodovsky2

  • 1a Heptares Therapeutics Limited, Steinmetz Building , Cambridge , Granta Park , UK.

Expert Opinion on Drug Discovery
|October 20, 2018
PubMed
Abstract

Insights

Adenosine A2A Receptor (A2AAR) antagonists show promise in cancer treatment by counteracting immune evasion within the tumor microenvironment. Ongoing research and structure-based drug design are advancing their clinical validation in immuno-oncology.

Area of Science:

  • Oncology
  • Immunology
  • Pharmacology

Background:

  • Extracellular adenosine accumulation in tumors promotes immune evasion.
  • Adenosine A2A Receptor (A2AAR) antagonists offer a therapeutic strategy against this mechanism.
  • The field of A2AAR antagonists has evolved from CNS indications to immuno-oncology.

Purpose of the Study:

  • To provide a perspective on the current status of A2AAR antagonists in oncology.
  • To highlight the biological rationale for using A2AAR antagonists in cancer therapy.
  • To discuss the impact of A2AAR structure determination on drug design.

Main Methods:

  • Review of existing literature on A2AAR antagonists in CNS and oncology.
  • Analysis of the biological mechanisms of adenosine in the tumor microenvironment.
  • Discussion of structure-based drug design approaches for A2AAR antagonists.

Main Results:

  • A2AAR antagonists are emerging as a significant therapeutic class in oncology.
  • Structure-based drug design, informed by A2AAR structural data, is accelerating development.
  • Clinical validation by major companies indicates strong therapeutic potential.

Conclusions:

  • A2AAR antagonists represent a promising approach for cancer immunotherapy.
  • Advances in structural biology are crucial for the rational design of these agents.
  • The field is poised for rapid development and clinical translation in the near future.
Keywords:
A2ARG protein-coupled receptorGPCRSBDDadenosine receptorsimmune-oncologystructure-based drug design

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