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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

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

Peng He1, Wenbo Zhou1, Mingyao Liu1

  • 1Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, 200241, China.

Current Topics in Medicinal Chemistry
|July 3, 2019
PubMed

Insights

New small molecule drugs targeting G Protein-Coupled Receptors (GPCRs) show promise for enhancing cancer immunotherapy. These GPCRs regulate the tumor microenvironment, potentially improving patient responses to treatments like CAR-T cell therapy and immune checkpoint inhibitors.

Area of Science:

  • Oncology
  • Immunology
  • Pharmacology

Background:

  • Chimeric antigen receptor T cell (CAR-T) and PD-1/PDL-1 inhibitor therapies have advanced cancer immunotherapy.
  • However, many patients do not benefit due to immunosuppressive tumor microenvironments.

Purpose of the Study:

  • To review advances in small molecular regulators targeting G Protein-Coupled Receptors (GPCRs) for cancer immunotherapy.
  • To explore how these GPCRs modulate tumor immunity and stromal cell biology.

Main Methods:

  • Review of recent literature on small molecular regulators targeting GPCRs in oncology.
  • Analysis of GPCRs including chemokine, purinergic, prostaglandin E receptor EP4, and opioid receptors.
  • Examination of clinical data for GPCR-targeted therapies combined with immune checkpoint blockers.

Main Results:

  • GPCRs significantly influence immune cell recruitment and tumor stromal biology.
  • Small molecular regulators targeting specific GPCRs demonstrate potential in modulating the tumor microenvironment.
  • Combination therapies involving GPCR modulators and immune checkpoint inhibitors are emerging.

Conclusions:

  • Targeting GPCRs represents a promising strategy to overcome resistance in cancer immunotherapy.
  • Further research and clinical trials are warranted to optimize combination therapies for improved patient outcomes.
Keywords:
Combination immunotherapyFDAG protein-coupled receptors (GPCRs)ImmunotherapySmall molecular regulatorTAMs.

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