Results 21 to 30 of about 793,543 (339)

G Protein-Coupled Receptors: Undervalued Targets for Cancer Therapy

Iraqi Journal of Pharmaceutical Sciences, 2022
Despite the G protein-coupled receptors (GPCRs) being the largest family of signalling proteins at the surface of cells, their potential to be targeted in cancer therapy is still under-utilised.
Ismail Ibrahim Al-Janabi
doaj   +1 more source

G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35 [PDF]

, 2017
It is widely appreciated that G protein-coupled receptors have been the most successfully exploited class of targets for the development of small molecule medicines. Despite this, to date, less than 15% of the non-olfactory G protein-coupled receptors in
Milligan, Graeme
core   +1 more source

Evolution of vertebrate GnRH receptors from the perspective of a basal vertebrate

Frontiers in Endocrinology, 2012
This minireview provides the current status on gonadotropin-releasing hormone receptors (GnRH-R) in vertebrates, from the perspective of a basal vertebrate, the sea lamprey, and provides an evolutionary scheme based on the recent advance of whole genome ...
Stacia A Sower, Wayne A Decatur, Nerine T Joseph, Mihael eFreamat   +3 more
doaj   +1 more source

G Protein–Coupled Receptor Heteromers [PDF]

Annual Review of Pharmacology and Toxicology, 2016
G protein–coupled receptors (GPCRs) compose one of the largest families of membrane proteins involved in intracellular signaling. They are involved in numerous physiological and pathological processes and are prime candidates for drug development. Over the past decade, an increasing number of studies have reported heteromerization between GPCRs.
Gomes, Ivone, Ayoub, Mohammed Akli, Fujita, Wakako, Jaeger, Werner C., Pfleger, Kevin D.G., Devi, Lakshmi A.   +5 more
openaire   +3 more sources

Metabolite G-Protein Coupled Receptors in Cardio-Metabolic Diseases

Cells, 2021
G protein-coupled receptors (GPCRs) have originally been described as a family of receptors activated by hormones, neurotransmitters, and other mediators.
Derek Strassheim, Timothy Sullivan, David C. Irwin, Evgenia Gerasimovskaya, Tim Lahm, Dwight J. Klemm, Edward C. Dempsey, Kurt R. Stenmark, Vijaya Karoor   +8 more
doaj   +1 more source

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

FEBS Letters, 2020
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
Nadia Arang, J. Gutkind
semanticscholar   +1 more source

The G protein-coupled oestrogen receptor GPER in health and disease: an update

Nature Reviews Endocrinology, 2023
The 7-transmembrane G protein-coupled receptor GPR30 has been recognized as a G protein-coupled oestrogen receptor (GPER) since 2008. This Review discusses progress in GPER research in physiology and disease and its potential implications for clinical ...
E. Prossnitz, M. Barton
semanticscholar   +1 more source

On the hierarchical classification of G Protein-Coupled Receptors [PDF]

, 2007
Motivation: G protein-coupled receptors (GPCRs) play an important role in many physiological systems by transducing an extracellular signal into an intracellular response. Over 50% of all marketed drugs are targeted towards a GPCR.
A. A. Freitas, A. Secker, Attwood, Bhasin, Bhasin, Bissantz, Cardoso, Christopoulos, D. R. Flower, Das, Davies, Flower, Flower, Foord, Gether, Gloriam, Guo, Horn, H  bert, J. Timmis, Karchin, Keerthi, Klabunde, Kolakowski, Lapinsh, M. Mendao, M. N. Davies, Milligan, Papasaikas, Prabhu, Sandberg, Schi  th   +31 more
core   +2 more sources

Neuropeptide G Protein-Coupled Receptors as Oncotargets

Frontiers in Endocrinology, 2018
Neuropeptide G protein-coupled receptors (GPCRs) are overexpressed on numerous cancer cells. In a number of tumors, such as small cell lung cancer (SCLC), bombesin (BB) like peptides and neurotensin (NTS) function as autocrine growth factors whereby they
Terry W. Moody, Irene Ramos-Alvarez, Robert T. Jensen   +2 more
doaj   +1 more source

Inhibition of Subsets of G Protein-coupled Receptors by Empty Mutants of G Protein α Subunits in Go, G11, and G16 [PDF]

, 2000
We previously reported that the xanthine nucleotide binding Goα mutant, GoαX, inhibited the activation of Gi-coupled receptors. We constructed similar mutations in G11α and G16α and characterized their nucleotide binding and receptor interaction.
Gu, Lingjie, Simon, Melvin I., Yu, Bo
core   +1 more source