GPCRs: Emerging anti-cancer drug targets.

Abstract:

:G protein-coupled receptors (GPCRs) constitute the largest and most diverse protein family in the human genome with over 800 members identified to date. They play critical roles in numerous cellular and physiological processes, including cell proliferation, differentiation, neurotransmission, development and apoptosis. Consequently, aberrant receptor activity has been demonstrated in numerous disorders/diseases, and as a result GPCRs have become the most successful drug target class in pharmaceuticals treating a wide variety of indications such as pain, inflammation, neurobiological and metabolic disorders. Many independent studies have also demonstrated a key role for GPCRs in tumourigenesis, establishing their involvement in cancer initiation, progression, and metastasis. Given the growing appreciation of the role(s) that GPCRs play in cancer pathogenesis, it is surprising to note that very few GPCRs have been effectively exploited in pursuit of anti-cancer therapies. The present review provides a broad overview of the roles that various GPCRs play in cancer growth and development, highlighting the potential of pharmacologically modulating these receptors for the development of novel anti-cancer therapeutics.

journal_name

Cell Signal

journal_title

Cellular signalling

authors

Nieto Gutierrez A,McDonald PH

doi

10.1016/j.cellsig.2017.09.005

subject

Has Abstract

pub_date

2018-01-01 00:00:00

pages

65-74

eissn

0898-6568

issn

1873-3913

pii

S0898-6568(17)30239-5

journal_volume

41

pub_type

杂志文章,评审