G Protein-coupled receptor 87: A promising opportunity for cancer drug discovery

Yanhong Zhang, Ariane Scoumanne, Xinbin Chen

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

G protein-coupled receptors (GPRs) constitute one of the largest families of membrane proteins encoded by the human genome. Upon binding to various ligands, these seven-transmembrane receptors play an essential role in many physiological processes, including neurotransmission, immunity, inflammation, regulation of mood and behavior. In view of their important functions, aberrant expression and activity of GPRs have been implicated in a wide spectrum of diseases, including tumorigenesis. GPR87, a cell surface GPR related to the LPA receptor family, is overexpressed in diverse carcinomas and plays an essential role in tumor cell survival. In our recent work, we uncovered that GPR87 expression is regulated by the tumor suppressor p53 and by DNA damage in a p53-dependent manner. Moreover, we found that a lack of GPR87 triggers an increase in p53, concomitant with a decrease in Akt, which results in the sensitization of tumor cells to DNA damage-induced apoptosis and growth suppression. Altogether, we uncovered an essential function for GPR87 in p53-dependent cell survival in response to stress signals. Due to their unique structure, localization and ligand binding ability, GPRs have been extensively used for drug development and are the most common targets of commercial drugs. Although studies are required to determine GPR87 natural ligand(s) and signaling pathways, GPR87 is undoubtedly a very promising novel target for cancer prevention and treatment.

Original languageEnglish (US)
Pages (from-to)111-116
Number of pages6
JournalMolecular and Cellular Pharmacology
Volume2
Issue number3
DOIs
StatePublished - 2010

Fingerprint

Drug Discovery
G-Protein-Coupled Receptors
Ligands
DNA Damage
Neoplasms
Cell Survival
Membrane Proteins
Lysophosphatidic Acid Receptors
Physiological Phenomena
Aptitude
Human Genome
Synaptic Transmission
Pharmaceutical Preparations
Immunity
Carcinogenesis
Apoptosis
Inflammation
Carcinoma
Growth

Keywords

  • Apoptosis
  • Cancer therapy
  • DNA damage
  • G protein-coupled receptor 87 (GPR87)
  • p53

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Molecular Biology

Cite this

G Protein-coupled receptor 87 : A promising opportunity for cancer drug discovery. / Zhang, Yanhong; Scoumanne, Ariane; Chen, Xinbin.

In: Molecular and Cellular Pharmacology, Vol. 2, No. 3, 2010, p. 111-116.

Research output: Contribution to journalArticle

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