scholarly journals Adhesion GPCRs in Glioblastoma

2021 ◽  
Author(s):  
Gabriele Stephan ◽  
Niklas Ravn-Boess ◽  
Dimitris G Placantonakis
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptors ◽  
The Past ◽  
Novel Treatment ◽  
The Family ◽  
Health And Disease ◽  
Basic Biology ◽  
G Protein Coupled ◽  
Potential Use ◽  
Receptor Family

Abstract Members of the adhesion family of G protein-coupled receptors (GPCRs) have received attention for their roles in health and disease, including cancer. Over the past decade, several members of the family have been implicated in the pathogenesis of glioblastoma. Here, we discuss the basic biology of adhesion GPCRs and review in detail specific members of the receptor family with known functions in glioblastoma. Finally, we discuss the potential use of adhesion GPCRs as novel treatment targets in neuro-oncology.

scholarly journals Metabolite Sensing GPCRs: Promising Therapeutic Targets for Cancer Treatment?

Cells ◽  
2020 ◽  
Vol 9 (11) ◽  
pp. 2345
Author(s):  
Jesús Cosín-Roger ◽  
Dolores Ortiz-Masia ◽  
Maria Dolores Barrachina ◽  
Sara Calatayud
Keyword(s):  
Cancer Treatment ◽  
G Protein ◽  
G Protein Coupled Receptors ◽  
Cancer Development ◽  
Metabolic Alterations ◽  
Pharmacological Targets ◽  
G Protein Coupled ◽  
Potential Use ◽  
Shed Light ◽  
Receptor Family

G-protein-coupled receptors constitute the most diverse and largest receptor family in the human genome, with approximately 800 different members identified. Given the well-known metabolic alterations in cancer development, we will focus specifically in the 19 G-protein-coupled receptors (GPCRs), which can be selectively activated by metabolites. These metabolite sensing GPCRs control crucial processes, such as cell proliferation, differentiation, migration, and survival after their activation. In the present review, we will describe the main functions of these metabolite sensing GPCRs and shed light on the benefits of their potential use as possible pharmacological targets for cancer treatment.

scholarly journals Applications of molecular replacement to G protein-coupled receptors

2013 ◽  
Vol 69 (11) ◽  
pp. 2287-2292 ◽  
Author(s):  
Andrew C. Kruse ◽  
Aashish Manglik ◽  
Brian K. Kobilka ◽  
William I. Weis
Keyword(s):  
G Protein ◽  
Structural Biology ◽  
Structural Information ◽  
G Protein Coupled Receptors ◽  
Integral Membrane Proteins ◽  
Molecular Replacement ◽  
Gpcr Activation ◽  
Health And Disease ◽  
Almost All ◽  
G Protein Coupled

G protein-coupled receptors (GPCRs) are a large class of integral membrane proteins involved in regulating virtually every aspect of human physiology. Despite their profound importance in human health and disease, structural information regarding GPCRs has been extremely limited until recently. With the advent of a variety of new biochemical and crystallographic techniques, the structural biology of GPCRs has advanced rapidly, offering key molecular insights into GPCR activation and signal transduction. To date, almost all GPCR structures have been solved using molecular-replacement techniques. Here, the unique aspects of molecular replacement as applied to individual GPCRs and to signaling complexes of these important proteins are discussed.

scholarly journals The secretin G-protein-coupled receptor family: teleost receptors

2005 ◽  
Vol 34 (3) ◽  
pp. 753-765 ◽  
Author(s):  
J C R Cardoso ◽  
M S Clark ◽  
F A Viera ◽  
P D Bridge ◽  
A Gilles ◽  
...  
Keyword(s):  
Vasoactive Intestinal Peptide ◽  
G Protein ◽  
Strong Support ◽  
Duplicated Genes ◽  
Related Peptide ◽  
Fugu Genome ◽  
The Family ◽  
Genome Consortium ◽  
G Protein Coupled ◽  
Receptor Family

Twenty-one members of the secretin family (family 2) of G-protein-coupled receptors (GPCRs) were identified via directed cloning and data-mining of the Fugu Genome Consortium database, representing the most comprehensive description of secretin GPCRs in a teleost fish to date. Duplicated genes were identified for many of the family members, namely the receptors for pituitary adenylate cyclase-activating polypeptide (PACAP)/vasoactive intestinal peptide (VIP), calcitonin, calcitonin gene-related peptide (CGRP), growth hormone releasing hormone (GHRH), glucagon receptor/glucagon-like peptide (GLP) and parathyroid hormone-related peptide (PTHrP)/PTH. Mining of other teleost genomes (zebrafish and Tetraodon) revealed that the duplicated genes identified in the Takifugu genome were also present in these fish. Additional database searching of the Escherichia coli, yeast, Drosophila, Caenorhabditis elegans and Ciona genomes revealed that the family 2 of GPCRs were only present in the multicellular organisms. Orthologues of all the human secretin receptors were identified with the exception of secretin itself. Additional database searches in the Fugu Genome Consortium database also failed to reveal a secretin ligand and so it is hypothesised that both the receptor and the ligand evolved after the divergence of teleost/tetrapod lineages. Phylogenetic analysis at both the protein and the DNA level provided strong support for each of the individual receptor family groupings, but weak support between groups, making evolutionary inferences difficult. A more critical analysis of the PACAP/VIP receptor family confirmed previous hypotheses that the vasoactive intestinal peptide receptor (VPAC1R) gene is the ancestral form of the receptor.

Neural Receptors Associated with Depression: A Systematic Review of the Past 10 Years

2020 ◽  
Vol 19 (6) ◽  
pp. 417-436
Author(s):  
Alice Barros Câmara ◽  
Igor Augusto Brandão
Keyword(s):  
Cerebral Cortex ◽  
Basal Ganglia ◽  
Cell Survival ◽  
G Protein ◽  
G Protein Coupled Receptors ◽  
Protective Effects ◽  
Inflammation Response ◽  
The Past ◽  
Open Access Journals ◽  
G Protein Coupled

Over the past few years, experimental research has been carried out to analyze the role of specific receptors in depression to better understand the mechanisms and pathophysiological aspects of the disease. In this paper, we aim to investigate the receptors family most involved in depression, as well as the tissues in which most depression related-receptors are expressed. The article also aims to identify the functions of the main receptors predominantly associated with the pathology. This review used a systematic methodology (Prospero; ID 168584) and followed the PRISMA guidelines. Studies were searched in PubMed/MEDLINE, Scientific Electronic Library Online, Web of Science, and Directory of Open Access Journals databases. Quantitative studies with conclusive results regarding receptors involved in depression were selected. The charts and network were made using R programming language and statistical analyses were carried out using SPSS v25 software. It can be seen that G protein-coupled receptors family is the most studied (p < 0.05). These receptors are expressed in the cerebral cortex, basal ganglia, and can interact with each other. A great number of studies have evaluated receptors related to beneficial effects in the disease (p < 0.05). The inflammation response and cell survival/proliferation are the main functions related to these receptors (p < 0.01) and behavioral tests in mice are the main methodologies applied in these studies (p < 0.05). Finally, the most influential protein on the network of receptors involved in depression is the Bradykinin receptor B1. G protein- coupled receptors located in cell membranes involving especially protective effects in depression and that expressed mainly in the cerebral cortex and basal ganglia have shown significant importance in this review. In addition, inflammation response or cell survival/proliferation are the main functions performed by the receptors related to depression as observed in this work.

Corticotropin-releasing hormone receptors

2002 ◽  
Vol 30 (4) ◽  
pp. 428-432 ◽  
Author(s):  
E. W. Hillhouse ◽  
H. Randeva ◽  
G. Ladds ◽  
D. Grammatopoulos
Keyword(s):  
G Protein ◽  
Hormone Receptors ◽  
G Protein Coupled Receptors ◽  
Corticotropin Releasing Hormone ◽  
Functional Characteristics ◽  
Releasing Hormone ◽  
The Family ◽  
G Protein Coupled

Corticotropin-releasing hormone (CRH) and related peptides (urocortins, sauvagine, urotensin) play a central role in the co-ordination of autonomic, behavioural, cardiovascular, immune and endocrine responses to stressful stimuli. Their actions are mediated through activation of two types of G-protein-coupled receptors encoded by separate genes. In this review we focus on the diverse structural and functional characteristics of the family of CRH-like peptides and their receptors.

scholarly journals A Long Road to the Spatial Structure and Mechanisms of Action

Acta Naturae ◽  
2012 ◽  
Vol 4 (4) ◽  
pp. 6-7
Author(s):  
V. I. Tsetlin
Keyword(s):  
Spatial Structure ◽  
G Protein ◽  
Nobel Prize ◽  
Medical Center ◽  
Mechanisms Of Action ◽  
G Protein Coupled Receptors ◽  
The Past ◽  
School Of Medicine ◽  
Duke University ◽  
G Protein Coupled

The 2012 Nobel Prize in chemistry has been awarded to Robert Lefkowitz, professor at Duke University Medical Center, and Brian Kobilka, professor at Stanford University School of Medicine, for research into G protein-coupled receptors. The wording research, rather than discovery, elucidation, or identification of something, speaks to the fact that such studies have been under way for nearly 40 years, from almost the zero level to the peaks conquered over the past few years.

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