Adenosine-mediated activation of A(2A)R drives immunosuppressive signaling in high-adenosine tumor microenvironments (TMEs), impeding anticancer immunity. Targeting A(2A)R with negative allosteric modulators (NAMs) is a promising approach for cancer immunotherapy: unlike the orthosteric antagonists currently in use, which face competitive and off-target limitations, NAMs leverage a noncompetitive, saturable mechanism that enhances receptor selectivity. The development of a novel series of A(2A)R NAMs demonstrates potent activity within high-adenosine TMEs, underscoring a significant translational potential in oncology.
Negative Allosteric Modulators of A2AR: A New Weapon for Cancer Immunotherapy? / Zambon, A.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 68:4(2025), pp. 4053-4055. [10.1021/acs.jmedchem.5c00137]
Negative Allosteric Modulators of A2AR: A New Weapon for Cancer Immunotherapy?
Zambon A.
2025
Abstract
Adenosine-mediated activation of A(2A)R drives immunosuppressive signaling in high-adenosine tumor microenvironments (TMEs), impeding anticancer immunity. Targeting A(2A)R with negative allosteric modulators (NAMs) is a promising approach for cancer immunotherapy: unlike the orthosteric antagonists currently in use, which face competitive and off-target limitations, NAMs leverage a noncompetitive, saturable mechanism that enhances receptor selectivity. The development of a novel series of A(2A)R NAMs demonstrates potent activity within high-adenosine TMEs, underscoring a significant translational potential in oncology.File | Dimensione | Formato | |
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