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 +3 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
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 +8 more
doaj +1 more source
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 +2 more
doaj +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 +31 more
core +2 more sources
Role of G-protein coupled receptors in cardiovascular diseases
Frontiers in Cardiovascular Medicine, 2023 Cardiovascular diseases (CVDs) are the leading cause of death globally, with CVDs accounting for nearly 30% of deaths worldwide each year. G-protein-coupled receptors (GPCRs) are the most prominent family of receptors on the cell surface, and play an ...
Yuanqiang Li +4 more
doaj +1 more source
Journal of Biological Chemistry, 2003 GPR41 and GPR43 are related members of a homologous family of orphan G protein-coupled receptors that are tandemly encoded at a single chromosomal locus in both humans and mice.
Andrew J. Brown +21 more
semanticscholar +1 more source
Thrombin Protease-activated Receptor-1 Signals through Gq- and G13-initiated MAPK Cascades Regulating c-Jun Expression to Induce Cell Transformation [PDF]
, 2003 Although the ability of G protein-coupled receptors to stimulate normal and aberrant cell growth has been intensely investigated, the precise nature of the molecular mechanisms underlying their transforming potential are still not fully understood.
Gutkind, J. Silvio +4 more
core +1 more source