Results 21 to 30 of about 22,949 (304)

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
doaj   +1 more source

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

, 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

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

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
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
doaj   +1 more source

Allosteric modulation of the activity of thrombin [PDF]

Biochemical Journal, 1997
Substrates containing a P3 aspartic residue are in general cleaved poorly by thrombin. This may be partly due to an unfavourable interaction between the P3 aspartate and Glu192 in the active site of thrombin. In Protein C activation and perhaps also thrombin receptor cleavage, binding of ligands at the anion-binding exosite of thrombin seems to improve
DUFFY, Edward J., ANGLIKER, Herbert, BONNIEC, Bernard F. Le, STONE, Stuart R.   +3 more
openaire   +3 more sources

Modulation of Allosteric Control and Evolution of Hemoglobin

Biomolecules, 2023
Allostery arises when a ligand-induced change in shape of a binding site of a protein is coupled to a tertiary/quaternary conformational change with a consequent modulation of functional properties. The two-state allosteric model of Monod, Wyman and Changeux [J. Mol. Biol.
Maurizio Brunori, Adriana Erica Miele
openaire   +4 more sources

Indomethacin Enhances Type 1 Cannabinoid Receptor Signaling

Frontiers in Molecular Neuroscience, 2019
In addition to its known actions as a non-selective cyclooxygenase (COX) 1 and 2 inhibitor, we hypothesized that indomethacin can act as an allosteric modulator of the type 1 cannabinoid receptor (CB1R) because of its shared structural features with the ...
Robert B. Laprairie, Robert B. Laprairie, Kawthar A. Mohamed, Ayat Zagzoog, Melanie E. M. Kelly, Melanie E. M. Kelly, Lesley A. Stevenson, Roger Pertwee, Eileen M. Denovan-Wright, Ganesh A. Thakur   +9 more
doaj   +1 more source

Conformational transitions and allosteric modulation in a heteromeric glycine receptor

Nature Communications, 2023
Glycine receptors (GlyR) are a critical postsynaptic component of spinal neurons. Here, the auhtors present cryo-EM structures of a heteromeric GlyR in the presence of an antagonist, agonist and agonist with a positive allosteric modulator.
Eric Gibbs, Emily Klemm, David Seiferth, Arvind Kumar, Serban L. Ilca, Philip C. Biggin, Sudha Chakrapani   +6 more
doaj   +1 more source

An NMDAR positive and negative allosteric modulator series share a binding site and are interconverted by methyl groups

eLife, 2018
N-methyl-d-aspartate receptors (NMDARs) are an important receptor in the brain and have been implicated in multiple neurological disorders. Many non-selective NMDAR-targeting drugs are poorly tolerated, leading to efforts to target NMDAR subtypes to ...
Riley Perszyk, Brooke M Katzman, Hirofumi Kusumoto, Steven A Kell, Matthew P Epplin, Yesim A Tahirovic, Rhonda L Moore, David Menaldino, Pieter Burger, Dennis C Liotta, Stephen F Traynelis   +10 more
doaj   +1 more source