Recent Advances on the Role of G Protein-Coupled Receptors in Hypoxia-Mediated Signaling

Rosamaria Lappano, Damiano Rigiracciolo, Paola De Marco, Silvia Avino, Anna Rita Cappello, Camillo Rosano, Marcello Maggiolini, Ernestina Marianna De Francesco

Research output: Contribution to journalArticlepeer-review


G protein-coupled receptors (GPCRs) are cell surface proteins mainly involved in signal transmission; however, they play a role also in several pathophysiological conditions. Chemically heterogeneous molecules like peptides, hormones, lipids, and neurotransmitters activate second messengers and induce several biological responses by binding to these seven transmembrane receptors, which are coupled to heterotrimeric G proteins. Recently, additional molecular mechanisms have been involved in GPCR-mediated signaling, leading to an intricate network of transduction pathways. In this regard, it should be mentioned that diverse GPCR family members contribute to the adaptive cell responses to low oxygen tension, which is a distinguishing feature of several illnesses like neoplastic and cardiovascular diseases. For instance, the G protein estrogen receptor, namely G protein estrogen receptor (GPER)/GPR30, has been shown to contribute to relevant biological effects induced by hypoxia via the hypoxia-inducible factor (HIF)-1α in diverse cell contexts, including cancer. Likewise, GPER has been found to modulate the biological outcome of hypoxic/ischemic stress in both cardiovascular and central nervous systems. Here, we describe the role exerted by GPCR-mediated signaling in low oxygen conditions, discussing, in particular, the involvement of GPER by a hypoxic microenvironment.

Original languageEnglish
Pages (from-to)305-310
Number of pages6
JournalAAPS Journal
Issue number2
Publication statusPublished - Mar 1 2016


  • angiogenesis
  • GPCRs
  • GPER
  • hypoxia
  • signal transduction

ASJC Scopus subject areas

  • Pharmaceutical Science


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