A serotonin receptor antagonist induces oocyte maturation in both frogs and mice: Evidence that the same G protein-coupled receptor is responsible for maintaining meiosis arrest in both species

2004 ◽  
Vol 202 (3) ◽  
pp. 777-786 ◽  
Author(s):  
Yinglun Sheng ◽  
Ling Wang ◽  
X. Shawn Liu ◽  
V�ronique Montplaisir ◽  
Mario Tiberi ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
G Protein ◽  
Oocyte Maturation ◽  
Serotonin Receptor ◽  
G Protein Coupled Receptor ◽  
Serotonin Receptor Antagonist ◽  
G Protein Coupled

scholarly journals Dihydromunduletone Is a Small-Molecule Selective Adhesion G Protein–Coupled Receptor Antagonist

2016 ◽  
Vol 90 (3) ◽  
pp. 214-224 ◽  
Author(s):  
Hannah M. Stoveken ◽  
Laura L. Bahr ◽  
M. W. Anders ◽  
Andrew P. Wojtovich ◽  
Alan V. Smrcka ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
G Protein ◽  
Small Molecule ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

scholarly journals A G protein–coupled receptor mediates neuropeptide-induced oocyte maturation in the jellyfish Clytia

PLoS Biology ◽  
2020 ◽  
Vol 18 (3) ◽  
pp. e3000614 ◽  
Author(s):  
Gonzalo Quiroga Artigas ◽  
Pascal Lapébie ◽  
Lucas Leclère ◽  
Philipp Bauknecht ◽  
Julie Uveira ◽  
...  
Keyword(s):  
G Protein ◽  
Oocyte Maturation ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

scholarly journals The Xenopus laevis Isoform of G Protein-Coupled Receptor 3 (GPR3) Is a Constitutively Active Cell Surface Receptor that Participates in Maintaining Meiotic Arrest in X. laevis Oocytes

2008 ◽  
Vol 22 (8) ◽  
pp. 1853-1865 ◽  
Author(s):  
James Deng ◽  
Stephanie Lang ◽  
Christopher Wylie ◽  
Stephen R. Hammes
Keyword(s):  
Cell Surface ◽  
Xenopus Laevis ◽  
G Protein ◽  
Oocyte Maturation ◽  
Cell Surface Receptor ◽  
Xenopus Laevis Oocytes ◽  
Intracellular Camp ◽  
G Protein Coupled Receptor ◽  
Meiotic Arrest ◽  
G Protein Coupled

Abstract Oocytes are held in meiotic arrest in prophase I until ovulation, when gonadotropins trigger a subpopulation of oocytes to resume meiosis in a process termed “maturation.” Meiotic arrest is maintained through a mechanism whereby constitutive cAMP production exceeds phosphodiesterase-mediated degradation, leading to elevated intracellular cAMP. Studies have implicated a constitutively activated Gαs-coupled receptor, G protein-coupled receptor 3 (GPR3), as one of the molecules responsible for maintaining meiotic arrest in mouse oocytes. Here we characterized the signaling and functional properties of GPR3 using the more amenable model system of Xenopus laevis oocytes. We cloned the X. laevis isoform of GPR3 (XGPR3) from oocytes and showed that overexpressed XGPR3 elevated intraoocyte cAMP, in large part via Gβγ signaling. Overexpressed XGPR3 suppressed steroid-triggered kinase activation and maturation of isolated oocytes, as well as gonadotropin-induced maturation of follicle-enclosed oocytes. In contrast, depletion of XGPR3 using antisense oligodeoxynucleotides reduced intracellular cAMP levels and enhanced steroid- and gonadotropin-mediated oocyte maturation. Interestingly, collagenase treatment of Xenopus oocytes cleaved and inactivated cell surface XGPR3, which enhanced steroid-triggered oocyte maturation and activation of MAPK. In addition, human chorionic gonadotropin-treatment of follicle-enclosed oocytes triggered metalloproteinase-mediated cleavage of XGPR3 at the oocyte cell surface. Together, these results suggest that GPR3 moderates the oocyte response to maturation-promoting signals, and that gonadotropin-mediated activation of metalloproteinases may play a partial role in sensitizing oocytes for maturation by inactivating constitutive GPR3 signaling.

Design and Synthesis of a G-Protein-Coupled Receptor Antagonist Library of Aryloxyalkanolamines Using a Polymer-Supported Acyclic Acetal Linker

2009 ◽  
Vol 11 (1) ◽  
pp. 72-82 ◽  
Author(s):  
Jacques Y. Roberge ◽  
Lalgudi S. Harikrishnan ◽  
Muthoni G. Kamau ◽  
Zheming Ruan ◽  
Katy Van Kirk ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
G Protein ◽  
G Protein Coupled Receptor ◽  
Design And Synthesis ◽  
Polymer Supported ◽  
G Protein Coupled

scholarly journals Broad-Spectrum G Protein–Coupled Receptor Antagonist, [D-Arg1,D-Trp5,7,9,Leu11]SP: A Dual Inhibitor of Growth and Angiogenesis in Pancreatic Cancer

2005 ◽  
Vol 65 (7) ◽  
pp. 2738-2745 ◽  
Author(s):  
Sushovan Guha ◽  
Guido Eibl ◽  
Krisztina Kisfalvi ◽  
Robert S. Fan ◽  
Marie Burdick ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Receptor Antagonist ◽  
G Protein ◽  
Broad Spectrum ◽  
G Protein Coupled Receptor ◽  
Dual Inhibitor ◽  
G Protein Coupled

scholarly journals Class A G Protein-Coupled Receptor Antagonist Famotidine as a Therapeutic Alternative against SARS-CoV2: An In Silico Analysis

Biomolecules ◽  
2020 ◽  
Vol 10 (6) ◽  
pp. 954 ◽  
Author(s):  
Joseph T. Ortega ◽  
Maria Luisa Serrano ◽  
Beata Jastrzebska
Keyword(s):  
Receptor Antagonist ◽  
G Protein ◽  
In Silico ◽  
Antiviral Agent ◽  
The United States ◽  
Clinical Report ◽  
G Protein Coupled Receptor ◽  
Class A ◽  
Short Period ◽  
G Protein Coupled

The pandemic associated with Severe Acute Respiratory Syndrome Coronavirus type 2 (SARS-CoV2) and its disease named COVID-19 challenged the scientific community to discover effective therapeutic solutions in a short period. Repurposing existing drugs is one viable approach that emphasizes speed during these urgent times. Famotidine, a class A G protein-coupled receptor antagonist used for the treatment of gastroesophageal reflux was recently identified in an in silico screening. Additionally, a recent retrospective clinical report showed that the treatment with famotidine provided a good outcome in patients infected with SARS-CoV2. A clinical trial testing effectiveness of famotidine in combination with hydroxychloroquine is currently ongoing in the United States (US). In the 1990s, famotidine was described as an antiviral agent against human immunodeficiency virus (HIV). Interestingly, some HIV protease inhibitors are presently being used against SARS-CoV2. However, it is not clear if famotidine could be effective against SARS-CoV2. Thus, by using a computational analysis, we aimed to examine if the antiviral effect of famotidine could be related to the inhibition of proteases involved in the virus replication. Our results showed that famotidine could interact within the catalytic site of the three proteases associated with SARS-CoV2 replication. However, weak binding affinity of famotidine to these proteases suggests that a successful famotidine therapy could likely be achieved only in combination with other antiviral drugs. Finally, analysis of famotidine’s pharmacokinetic parameters indicated that its effect against SARS-CoV2 infection could be reached only upon intravenous administration. This work will contribute to the pharmacological knowledge of famotidine as an antiviral agent against SARS-CoV2.

Small-Molecule Vasopressin-2 Receptor Antagonist Identified by a G-Protein Coupled Receptor “Pathway” Screen

2007 ◽  
Vol 72 (1) ◽  
pp. 86-94 ◽  
Author(s):  
Buranee Yangthara ◽  
Aaron Mills ◽  
Varanuj Chatsudthipong ◽  
Lukmanee Tradtrantip ◽  
A. S. Verkman
Keyword(s):  
Receptor Antagonist ◽  
G Protein ◽  
Small Molecule ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled
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