G Protein‐Coupled receptors and heterotrimeric G proteins as cancer drivers

• Published in: FEBS letters Vol. 594; no. 24; pp. 4201 - 4232
• Main Authors: Arang, Nadia, Gutkind, J. Silvio
• Format: Journal Article
• Language: English
• Published: England 01.12.2020
• Subjects: angiogenesis; cancer; cancer metabolism; Carcinogenesis; Disease Progression; drug resistance; G protein‐coupled receptors; GTPases; Heterotrimeric GTP-Binding Proteins - metabolism; Humans; immune evasion; immune therapy; inflammation; landscapes; metastasis; morbidity; mortality; neoplasms; Neoplasms - metabolism; Neoplasms - pathology; precision medicine; Receptors, G-Protein-Coupled - metabolism; Signal Transduction; therapeutics; cancer metabolism; immune therapy; G protein-coupled receptors; GTPases; inflammation; metastasis; signal transduction; angiogenesis; precision medicine; cancer
• ISSN: 0014-5793; 1873-3468; 1873-3468
• DOI: 10.1002/1873-3468.14017

G protein‐coupled receptors (GPCRs) and heterotrimeric G proteins play central roles in a diverse array of cellular processes. As such, dysregulation of GPCRs and their coupled heterotrimeric G proteins can dramatically alter the signalling landscape and functional state of a cell. Consistent with their fundamental physiological functions, GPCRs and their effector heterotrimeric G proteins are implicated in some of the most prevalent human diseases, including a complex disease such as cancer that causes significant morbidity and mortality worldwide. GPCR/G protein‐mediated signalling impacts oncogenesis at multiple levels by regulating tumour angiogenesis, immune evasion, metastasis, and drug resistance. Here, we summarize the growing body of research on GPCRs and their effector heterotrimeric G proteins as drivers of cancer initiation and progression, and as emerging antitumoural therapeutic targets.