Exploring the Effect of Halogenation in a Series of Potent and Selective A2B Adenosine Receptor Antagonists
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c01768
Abstract: The modulation of the A2B adenosine receptor is a promising strategy in cancer (immuno) therapy, with A2BAR antagonists emerging as immune checkpoint inhibitors. Herein, we report a systematic assessment of the impact of (di- and… read more here.
Keywords: affinity; halogenation; a2bar; a2b adenosine ... See more keywords
Improving combination therapies: Targeting A2B adenosine receptor to modulate metabolic tumor microenvironment and immunosuppression.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of the National Cancer Institute"
DOI: 10.1093/jnci/djad091
Abstract: BACKGROUND We investigated the role of A2B-adenosine receptor (A2BAR) in regulating immunosuppressive metabolic stress in the tumor microenvironment (TME). Novel A2BAR antagonist PBF-1129 was tested for anti-tumor activity in animals and evaluated for safety and… read more here.
Keywords: adenosine; pbf 1129; efficacy; a2bar ... See more keywords
A2B adenosine receptor antagonists rescue lymphocyte activity in adenosine-producing patient-derived cancer models
Sign Up to like & getrecommendations! Published in 2022 at "Journal for Immunotherapy of Cancer"
DOI: 10.1136/jitc-2022-004592
Abstract: Background Adenosine is a metabolite that suppresses antitumor immune response of T and NK cells via extracellular binding to the two subtypes of adenosine-2 receptors, A2ARs. While blockade of the A2AARs subtype effectively rescues lymphocyte… read more here.
Keywords: a2aar a2bar; a2bar; patient derived; lymphocyte activity ... See more keywords
Irreversible Antagonists for the Adenosine A2B Receptor
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DOI: 10.3390/molecules27123792
Abstract: Blockade of the adenosine A2B receptor (A2BAR) represents a potential novel strategy for the immunotherapy of cancer. In the present study, we designed, synthesized, and characterized irreversible A2BAR antagonists based on an 8-p-sulfophenylxanthine scaffold. Irreversible… read more here.
Keywords: irreversible a2bar; a2b receptor; a2bar; a2bar antagonists ... See more keywords