Understanding the Allosteric Modulation of PTH1R by a Negative Allosteric Modulator
Cells, 2022 The parathyroid hormone type 1 receptor (PTH1R) acts as a canonical class B G protein-coupled receptor, regulating crucial functions including calcium homeostasis and bone formation.
Mengrong Li +5 more
doaj +4 more sources
Kinetic Benefit(s) of Allosteric Receptor Blockade by Positive Allosteric Modulator Antagonists. [PDF]
ACS Pharmacol Transl SciThis paper discusses how targeted pharmacologic experiments can elucidate the mechanism of allosteric receptor inhibitors (NAMs) to identify NAMs that may have exceptionally useful properties and target residence times in vivo.
Vauquellin G, Kenakin T.
europepmc +2 more sources
Allosteric Modulation of Chemoattractant Receptors [PDF]
Frontiers in Immunology, 2016 Chemoattractants control selective leukocyte homing via interactions with a dedicated family of related G protein-coupled receptor (GPCR). Emerging evidence indicates that the signaling activity of these receptors, as for other GPCR, is influenced by allosteric modulators, which interact with the receptor in a binding site distinct from the binding ...
Maria Candida Cesta +3 more
openaire +3 more sources
In silico Insights on the Allosteric Modulation of the µ-Opioid Receptor and G protein Complex in the Presence of Agonist Ligand BU72 and Potential Positive Allosteric Modulator BMS-986121 [PDF]
, 2020 The G protein-coupled receptor (GPCR) µ-opioid receptor (µOR) is one of several drug targets of commercially available therapeutics for pain. Various opioid drugs like morphines have been associated to numerous substance abuse-related deaths around the ...
Ricky, Nellas, Mac Kevin, Braza
core +1 more source
Allo-network drugs: Extension of the allosteric drug concept to protein-protein interaction and signaling networks [PDF]
, 2013 Allosteric drugs are usually more specific and have fewer side effects than orthosteric drugs targeting the same protein. Here, we overview the current knowledge on allosteric signal transmission from the network point of view, and show that most ...
Csermely, Péter +3 more
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Surface dynamics in allosteric regulation of protein-protein interactions: modulation of calmodulin functions by Ca2+. [PDF]
PLoS Computational Biology, 2013 Knowledge of the structural basis of protein-protein interactions (PPI) is of fundamental importance for understanding the organization and functioning of biological networks and advancing the design of therapeutics which target PPI.
Yosef Y Kuttner +2 more
doaj +1 more source
Biochemical pharmacology of the positive allosteric modulation of the GABAb receptor "in Vitro" and "in Vivo" [PDF]
, 2007 Allosteric modulators of G-protein coupled receptors (GPCRs) interact with binding sites on the receptor molecule that are topographically distinct from the classic orthosteric site.
Gjoni, Tina
core +1 more source
Allosteric Modulation of Muscarinic Acetylcholine Receptors
Pharmaceuticals, 2010 An allosteric modulator is a ligand that binds to an allosteric site on the receptor and changes receptor conformation to produce increase (positive cooperativity) or decrease (negative cooperativity) in the binding or action of an orthosteric agonist (e.
Esam E. El-Fakahany, Jan Jakubík
doaj +1 more source
An allosteric modulator binds to a conformational hub in the β2 adrenergic receptor [PDF]
, 2020 Most drugs acting on G-protein-coupled receptors target the orthosteric binding pocket where the native hormone or neurotransmitter binds. There is much interest in finding allosteric ligands for these targets because they modulate physiologic signaling ...
Hirata, Kunio +31 more
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Development of allosteric modulators of GPCRs for treatment of CNS disorders
Neurobiology of Disease, 2014 The discovery of allosteric modulators of G protein-coupled receptors (GPCRs) provides a promising new strategy with potential for developing novel treatments for a variety of central nervous system (CNS) disorders.
Hilary Highfield Nickols +1 more
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