Results 31 to 40 of about 22,949 (304)
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
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Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor [PDF]
Proceedings of the National Academy of Sciences, 2013 μ-Opioid receptors are among the most studied G protein-coupled receptors because of the therapeutic value of agonists, such as morphine, that are used to treat chronic pain. However, these drugs have significant side effects, such as respiratory suppression, constipation, allodynia, tolerance, and dependence, as well as abuse potential.
Neil T, Burford +7 more
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Pharmaceuticals, 2013 The effect of an allosteric modulator of the adenosine A1 receptors was investigated using an ischaemia-reperfusion protocol in murine isolated hearts. Isolated hearts were perfused with Kreb-Henseleit solution gassed with carbogen gas (95% O2 and 5% CO2)
Roselyn B. Rose'Meyer +4 more
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The Structural Basis of ATP as an Allosteric Modulator [PDF]
PLoS Computational Biology, 2014 Adenosine-5'-triphosphate (ATP) is generally regarded as a substrate for energy currency and protein modification. Recent findings uncovered the allosteric function of ATP in cellular signal transduction but little is understood about this critical behavior of ATP.
Shaoyong Lu +6 more
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iScience, 2020 Summary: Insulin regulates glucose metabolism through thousands of regulatory mechanisms; however, which regulatory mechanisms are keys to control glucose metabolism remains unknown.
Satoshi Ohno +10 more
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Allosteric Modulation of Beta1 Integrin Function Induces Lung Tissue Repair [PDF]
, 2012 The cellular cytoskeleton, adhesion receptors, extracellular matrix composition, and their spatial distribution are together fundamental in a cell's balanced mechanical sensing of its environment.
Susan McIntyre +13 more
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Aiming for allosterism: Evaluation of allosteric modulators of CB1 in a neuronal model [PDF]
Pharmacological Research, 2015 Cannabinoid pharmacology has proven nettlesome with issues of promiscuity a common theme among both agonists and antagonists. One recourse is to develop allosteric ligands to modulate cannabinoid receptor signaling. Cannabinoids have come late to the allosteric table.
Alex, Straiker +4 more
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Allosteric modulation of glycine receptors.
British Jounral of Pharmacology, 2011 Inhibitory (or strychnine sensitive) glycine receptors (GlyRs) are anion-selective transmitter-gated ion channels of the cys-loop superfamily, which includes among others also the inhibitory γ-aminobutyric acid receptors (GABA(A) receptors). While GABA mediates fast inhibitory neurotransmission throughout the CNS, the action of glycine as a fast ...
Yevenes GE, Zeilhofer HU
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PLoS ONE, 2015 The interleukin-1 receptor (IL-1R) is the founding member of the interleukin 1 receptor family which activates innate immune response by its binding to cytokines.
Chao-Yie Yang
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Nature Communications, 2021 Here, the authors use smFRET to assess the structural dynamics of metabotropic glutamate receptor mGlu2 and show that a positive allosteric modulator or the Gi protein stabilize mGlu2 in the glutamate-induced active state, leading to the full activation ...
Anne-Marinette Cao +5 more
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