Proton-sensing G Protein-coupled Receptors: Detectors of Tumor Acidosis and Candidate Drug Targets

Overview

Journal Future Med Chem

Specialties Chemistry
Pharmacy

Date 2020 Mar 3

PMID 32116003

Citations 15

Authors

Paul A Insel

Krishna Sriram

Cristina Salmeron

Shu Z Wiley

Affiliations

Soon will be listed here.

Abstract

Cells in tumor microenvironments (TMEs) use several mechanisms to sense their low pH (<7.0), including via proton-sensing G protein-coupled receptors (psGPCRs): GPR4, GPR65/TDAG8, GPR68/OGR1 and GPR132/G2A. Numerous cancers have increased expression of psGPCRs. The psGPCRs may contribute to features of the malignant phenotype via actions on specific cell-types in the TME and thereby promote tumor survival and growth. Here, we review data regarding psGPCR expression in tumors and cancer cells, impact of psGPCRs on survival in solid tumors and a bioinformatics approach to infer psGPCR expression in cell types in the TME. New tools are needed to help define contributions of psGPCRs in tumor biology and to identify potentially novel therapeutic agents for a variety of cancers.

Citing Articles

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Proton Sensing GPCR's: The missing link to Warburg's Oncogenic Legacy?.

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The Molecular Effects of Dietary Acid Load on Metabolic Disease (The Cellular PasaDoble: The Fast-Paced Dance of pH Regulation).

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