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Curr Top Med Chem. 2019 Jun 28. doi: 10.2174/1568026619666190628115644. [Epub ahead of print]

Recent Advances of Small Molecular Regulators Targeting G Protein-Coupled Receptors Family for Oncology Immunotherapy.

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Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, 200241. China.


The great clinical successes of chimeric antigen receptor T cell (CAR-T) and PD-1/PDL-1 inhibitor therapies suggest the draw of a cancer immunotherapy age. However, a considerable proportion of cancer patients currently receive little benefit from these treatment modalities, indicating that multiple immunosuppressive mechanisms that exist in the tumor microenvironment. In this review, we mainly discuss recent advances in small molecular regulators targeting G protein-coupled receptors (GPCRs) that are associated with oncology immunomodulation, including chemokine receptors, purinergic receptors, histamine receptors, prostaglandin E receptor EP4 and opioid receptors. Moreover, we outline how they affect tumor immunity and neoplasia by regulating immune cell recruitment and modulating tumor stromal cell biology. We also summarize the data from recent clinical advances in small molecular regulators targeting these GPCRs, in combination with immune checkpoints blockers, such as PD-1/PDL-1 and CTLA4 inhibitors, for cancer treatments.


G protein-coupled receptors (GPCRs); combination immunotherapy; immunotherapy; small molecular regulato

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