Results 11 to 20 of about 19,325 (262)

Allosteric Modulation of Muscarinic Acetylcholine Receptors [PDF]

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   +3 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, Marcello eAllegretti, Massimo eLocati, Massimo eLocati   +3 more
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Allosteric modulation of gonadotropin receptors

Frontiers in Endocrinology, 2023
Gonadotropins regulate reproductive functions by binding to G protein-coupled receptors (FSHR and LHCGR) expressed in the gonads. They activate multiple, cell-specific signalling pathways, consisting of ligand-dependent intracellular events. Signalling cascades may be modulated by synthetic compounds which bind allosteric sites of FSHR and LHCGR or by ...
Clara Lazzaretti, Manuela Simoni, Manuela Simoni, Manuela Simoni, Livio Casarini, Livio Casarini, Elia Paradiso   +6 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, Tal Nagar, Stanislav Engel   +2 more
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Allosteric Modulators for mGlu Receptors [PDF]

Current Neuropharmacology, 2007
The metabotropic glutamate receptor family comprises eight subtypes (mGlu1-8) of G-protein coupled receptors. mGlu receptors have a large extracellular domain which acts as recognition domain for the natural agonist glutamate. In contrast to the ionotropic glutamate receptors which mediate the fast excitatory neurotransmission, mGlu receptors have been
Gasparini, F, Spooren, W
openaire   +2 more sources

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, P. Jeffrey Conn   +1 more
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The unconventional activation of the muscarinic acetylcholine receptor M4R by diverse ligands

Nature Communications, 2022
The authors report the structural characterization of M4R selective allosteric agonist, compound-110, as well as agonist iperoxo and positive allosteric modulator LY2119620.
Jingjing Wang, Meng Wu, Zhangcheng Chen, Lijie Wu, Tian Wang, Dongmei Cao, Huan Wang, Shenhui Liu, Yueming Xu, Fei Li, Junlin Liu, Na Chen, Suwen Zhao, Jianjun Cheng, Sheng Wang, Tian Hua   +15 more
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Allosteric control of an asymmetric transduction in a G protein-coupled receptor heterodimer

eLife, 2017
GPCRs play critical roles in cell communication. Although GPCRs can form heteromers, their role in signaling remains elusive. Here we used rat metabotropic glutamate (mGlu) receptors as prototypical dimers to study the functional interaction between each
Junke Liu, Zongyong Zhang, David Moreno-Delgado, James AR Dalton, Xavier Rovira, Ana Trapero, Cyril Goudet, Amadeu Llebaria, Jesús Giraldo, Qilin Yuan, Philippe Rondard, Siluo Huang, Jianfeng Liu, Jean-Philippe Pin   +13 more
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Allosteric modulation of adenosine receptors [PDF]

Purinergic Signalling, 2008
Allosteric ligands for G protein-coupled receptors (GPCRs) may alter receptor conformations induced by an orthosteric ligand. These modulators can thus fine-tune classical pharmacological responses. In this review we will describe efforts to synthesize and characterize allosteric modulators for one particular GPCR subfamily, the adenosine receptors ...
Göblyös, Anikó, IJzerman, Ad P.
openaire   +3 more sources

Contrasting properties of α7-selective orthosteric and allosteric agonists examined on native nicotinic acetylcholine receptors. [PDF]

PLoS ONE, 2013
Subtype-selective ligands are important tools for the pharmacological characterisation of neurotransmitter receptors. This is particularly the case for nicotinic acetylcholine receptors (nAChRs), given the heterogeneity of their subunit composition.
JasKiran K Gill, Anna Chatzidaki, Daniel Ursu, Emanuele Sher, Neil S Millar   +4 more
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