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Quantifying Agonist Activity at G Protein-coupled Receptors
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Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Agonists as Potential Small Molecule Therapeutics for

Ruomeng Qiu1, Yonghui Wang1

  • 1Department of Medicinal Chemistry, School of Pharmacy , Fudan University , 826 Zhangheng Road , 201203 Shanghai , China.

Journal of Medicinal Chemistry
|February 8, 2018
PubMed

Insights

Small molecule RORγt agonists show promise for cancer immunotherapy by activating immune cells. This review explores RORγt agonists as a novel therapeutic strategy to enhance antitumor efficacy.

Area of Science:

  • Immunology
  • Oncology
  • Pharmacology

Background:

  • Immune system activation, exemplified by PD-1/PD-L1 antibodies, is effective against advanced cancers.
  • This success fuels interest in small molecule immunomodulators for cancer immunotherapy.
  • Retinoid-related Orphan Receptor gamma t (RORγt) is crucial for Th17 cell differentiation and IL-17 production, which can activate CD8+ T cells for antitumor effects.

Purpose of the Study:

  • To review sterol and synthetic RORγt agonists.
  • To analyze the shared mechanisms of action for RORγt agonists.
  • To discuss the potential of RORγt agonists as small molecule therapeutics in cancer immunotherapy.

Main Methods:

  • Literature review of RORγt agonists.
  • Analysis of RORγt signaling pathways.
  • Evaluation of RORγt agonists' role in immune activation and antitumor efficacy.

Main Results:

  • RORγt agonists increase RORγt basal activity.
  • RORγt agonists promote Th17 cell differentiation.
  • RORγt agonists have potential to activate CD8+ T cells and elicit antitumor responses.

Conclusions:

  • RORγt agonists represent a promising avenue for cancer immunotherapy.
  • Small molecule RORγt agonists offer a unique therapeutic approach.
  • Further development of RORγt agonists could lead to novel cancer treatments.

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