Title:GPR18 and GPR55-related Ligands Serving as Antagonists or Agonists:
Current Situation, Challenges and Perspectives
Volume: 19
Issue: 9
Author(s): Linjie Zhang, Yiwen Fang, Sijing Hang, Wenhui Wu, Ruilong Sheng and Ruihua Guo*
Affiliation:
- College of Food Science and Technology, Shanghai Ocean University, Shanghai, 201306, China
- Laboratory of Quality and Safety Risk
Assessment for Aquatic Product on Storage and Preservation (Shanghai), Ministry of Agriculture, Shanghai, 201306,
China
- Shanghai Engineering Research Center of Aquatic-Product Processing & Preservation, Shanghai, 201306,
China
Keywords:
GPR18, GPR55, antagonist, agonist, cannabinoid receptor, orphan receptors.
Abstract: GPCR superfamily, the largest known family of membrane receptors, consists of six
classes from A to F. GPR18 and GPR55, δ-branch of A class, had been reported to have no confirmed
endogenous ligand and were named as “orphan receptors”. Previous studies suggest that both
GPR18 and GPR55 are possibly related to the migration and proliferation of cancer cells, macrophages
and other inflammation-associated immune cells. Thus, they may be potential targets for inflammation,
cancer and analgesia therapy. In this paper, we aimed to summarize the chemical structures
and bioactivities of the agonists and antagonists of GPR18 and GPR55; moreover, we have
briefly discussed the challenges and future perspectives in this field. This review will be beneficial
for further design and synthesis of efficient agonists and antagonists towards GPR18 and GPR55-
related disease treatment.
