Results 21 to 30 of about 139,314 (301)

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
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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
doaj   +1 more source

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
doaj   +1 more source

Allosteric inhibition enhances the efficacy of ABL kinase inhibitors to target unmutated BCR-ABL and BCR-ABL-T315I [PDF]

, 2012
Background: Chronic myelogenous leukemia (CML) and Philadelphia chromosome-positive (Ph+) acute lymphatic leukemia (Ph + ALL) are caused by the t(9;22), which fuses BCR to ABL resulting in deregulated ABL-tyrosine kinase activity.
Ruimi, Nili, Martin Ruthardt, Mahajna, Jamal, Khateb, Mamduh, Jamal Mahajna, Ruthardt, Martin, Ottmann, Oliver G., Oliver Gerhard Ottmann, Mian, Afsar Ali, Nili Ruimi, Yousef Najajreh, Afsar Ali Mian, Ottmann, Oliver Gerhard, Susanne Badura, Metodieva, Anna, Najajreh, Yousef, Anna Metodieva, Mamduh Khateb, Badura, Susanne   +18 more
core   +2 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

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
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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
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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

Functional Consequences of GPCR Heterodimerization: GPCRs as Allosteric Modulators

Pharmaceuticals, 2011
G Protein Coupled Receptors (GPCRs) represent the largest family of membrane proteins in the human genome, are the targets of approximately 25% of all marketed pharmaceuticals, and the focus of intensive research worldwide given that this superfamily of ...
Karla K.V. Haack, Nael A. McCarty
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
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