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

Journal Title: The AAPS Journal - Year 2016, Vol 18, Issue 2

Abstract

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.

Authors and Affiliations

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

Keywords

Related Articles

Role of Physiological Intestinal Water in Oral Absorption

Water volume has impact when the compound has low aqueous solubility. For example, the absorption of compounds with a Biopharmaceutics Classification System class 2 or 4 is likely to be solubility-limited. Provided the f...

Advanced pharmacokinetic models based on organ clearance, circulatory, and fractal concepts

Three advanced models of pharmacokinetics are described. In the first class are physiologically based pharmacokinetic models based on in vitro data on transport and metabolism. The information is translated as transporte...

Light-scattering investigations on dilute nonionic oil-in-water microemulsions

Dilute 3-component nonionic oil-in-water microemulsions formulated with either a polyoxyethylene surfactant (C18∶1E10 or C12E10) or the alkylamine-N-oxide surfactant, DDAO (C12AO), and containing either a triglyc...

Effect of Type 2 Diabetes Mellitus and Diabetic Nephropathy on IgG Pharmacokinetics and Subcutaneous Bioavailability in the Rat

The objective of this research was to assess the effects of type 2 diabetes mellitus (T2DM) and diabetic nephropathy (DN) on the pharmacokinetics of human IgG (hIgG), an antibody isotype, in Zucker diabetic fatty (ZDF) r...

In Vitro Considerations to Support Bioequivalence of Locally Acting Drugs in Dry Powder Inhalers for Lung Diseases

Dry powder inhalers (DPIs) are used to deliver locally acting drugs (e.g., bronchodilators and corticosteroids) for treatment of lung diseases such as asthma and chronic obstructive pulmonary disease (COPD). Demonstratin...

Download PDF file
  • EP ID EP680841
  • DOI  10.1208/s12248-016-9881-6
  • Views 61
  • Downloads 0

How To Cite

Rosamaria Lappano, Damiano Rigiracciolo, Paola De Marco, Silvia Avino, Anna Rita Cappello, Camillo Rosano, Marcello Maggiolini, Ernestina Marianna De Francesco (2016). Recent Advances on the Role of G Protein-Coupled Receptors in Hypoxia-Mediated Signaling. The AAPS Journal, 18(2), -. https://europub.co.uk/articles/-A-680841