“Phenotypic” pharmacology: The influence of cellular environment on G protein-coupled receptor antagonist and inverse agonist pharmacology

2007 ◽  
Vol 73 (6) ◽  
pp. 737-751 ◽  
Author(s):  
Carl P. Nelson ◽  
R.A. John Challiss
Keyword(s):  
Receptor Antagonist ◽  
G Protein ◽  
Inverse Agonist ◽  
G Protein Coupled Receptor ◽  
Cellular Environment ◽  
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 The extracellular N-terminal domain of G-protein coupled receptor 83 regulates signaling properties and is an intramolecular inverse agonist

2014 ◽  
Vol 7 (1) ◽  
pp. 913 ◽  
Author(s):  
Anne Müller ◽  
Brinja Leinweber ◽  
Jana Fischer ◽  
Timo D Müller ◽  
Annette Grüters ◽  
...  
Keyword(s):  
G Protein ◽  
Inverse Agonist ◽  
G Protein Coupled Receptor ◽  
Terminal Domain ◽  
G Protein Coupled

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 Identification of the First Nonpeptidergic Inverse Agonist for a Constitutively Active Viral-encoded G Protein-coupled Receptor

2002 ◽  
Vol 278 (7) ◽  
pp. 5172-5178 ◽  
Author(s):  
Paola Casarosa ◽  
Wiro M. Menge ◽  
Rosalba Minisini ◽  
Claas Otto ◽  
Jane van Heteren ◽  
...  
Keyword(s):  
G Protein ◽  
Inverse Agonist ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled ◽  
Constitutively Active

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.

scholarly journals G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody

Nature ◽  
2012 ◽  
Vol 482 (7384) ◽  
pp. 237-240 ◽  
Author(s):  
Tomoya Hino ◽  
Takatoshi Arakawa ◽  
Hiroko Iwanari ◽  
Takami Yurugi-Kobayashi ◽  
Chiyo Ikeda-Suno ◽  
...  
Keyword(s):  
G Protein ◽  
Inverse Agonist ◽  
G Protein Coupled Receptor ◽  
Receptor Inactivation ◽  
Agonist Antibody ◽  
G Protein Coupled

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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