Results 211 to 220 of about 37,458 (256)

Meaty Aroma Compounds Enhance MSG Umami Perception Through Allosteric Modulation of T1R1/T1R3 Receptor: Evidence from Nasal Clip Sensory Evaluation and Molecular Dynamics Simulation. [PDF]

Foods
Zhao Y, Zhang J, Zhao M, Zhao X, Su G.
europepmc   +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.
Jan Jakubik, Esam E El-Fakahany, Jakubik Jan   +2 more
exaly   +3 more sources

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Olfaction: Allosteric modulation

Current Biology, 2023
New research indicates that the odor-evoked responses of human olfactory receptors can be enhanced via the non-competitive binding of an allosteric modulator. This modulatory mechanism adds an additional layer of complexity to the peripheral encoding of odors.
Samuel, Caton, Adam, Dewan
openaire   +2 more sources

Current Advances in Allosteric Modulation of Muscarinic Receptors

Biomolecules, 2020
Allosteric modulators are ligands that bind to a site on the receptor that is spatially separated from the orthosteric binding site for the endogenous neurotransmitter.
Jan Jakubik, Esam E El-Fakahany, Jakubik Jan   +2 more
exaly   +3 more sources

Allosteric modulation of caspases

Pharmacology & Therapeutics, 2011
Caspases are proteolytic enzymes mainly involved in the induction and execution phases of apoptosis. This type of programmed cell death is an essential regulatory process required to maintain the integrity and homeostasis of multicellular organisms. Inappropriate apoptosis is attributed a key role in many human diseases, including neurodegenerative ...
Hans-Georg, Häcker, Mihiret Tekeste, Sisay, Michael, Gütschow   +2 more
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Allosteric modulation of monomeric proteins*

Biochemistry and Molecular Biology Education, 2005
AbstractMultimeric proteins (e.g. hemoglobin) are considered to be the prototypes of allosteric enzymes, whereas monomeric proteins (e.g. myoglobin) usually are assumed to be nonallosteric. However, the modulation of the functional properties of monomeric proteins by heterotropic allosteric effectors casts doubts on this assumption.
ASCENZI P, BOCEDI A, BOLLI A, FASANO, MAURO, NOTARI S, POLTICELLI F.   +5 more
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Neurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator

Biochemistry, 2023
The NTSR1 neurotensin receptor (NTSR1) is a G protein-coupled receptor (GPCR) found in the brain and peripheral tissues with neurotensin (NTS) being its endogenous peptide ligand. In the brain, NTS modulates dopamine neuronal activity, induces opioid-independent analgesia, and regulates food intake.
Brian E. Krumm, Jeffrey F. DiBerto, Reid H. J. Olsen, Hye Jin Kang, Samuel T. Slocum, Shicheng Zhang, Ryan T. Strachan, Xi-Ping Huang, Lauren M. Slosky, Anthony B. Pinkerton, Lawrence S. Barak, Marc G. Caron, Terry Kenakin, Jonathan F. Fay, Bryan L. Roth   +14 more
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Allosteric Agonist Modulators

Journal of Receptors and Signal Transduction, 2007
This article discusses a model to describe the effects of molecules that bind to a site on the receptor separate from that of the endogenous agonist to actively produce receptor signals (direct agonism). In addition, these molecules also modify the biological responses of the endogenous agonist (either potentiation or antagonism).
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Tuning Down the Pain – An Overview of Allosteric Modulation of Opioid Receptors: Mechanisms of Modulation, Allosteric Sites, Modulator Syntheses

Current Topics in Medicinal Chemistry, 2020
Opioid signaling plays a central role in pain perception. As such, it remains the main target in the development of antinociceptive agents, despite serious side effects involved. In recent years, hopes for improved opioid painkillers are rising, together with our understanding of allosterism and biased signaling mechanisms.
Damian Bartuzi, Tomasz M. Wróbel, Agnieszka A. Kaczor, Dariusz Matosiuk   +3 more
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GPCR Allosteric Modulator Discovery

2019
G protein-coupled receptors (GPCRs) influence virtually every aspect of human physiology; about one-third of all marketed drugs target members of this family. GPCR allosteric ligands hold the promise of improved subtype selectivity, spatiotemporal sensitivity, and possible biased property over typical orthosteric ligands.
Yiran, Wu, Jiahui, Tong, Kang, Ding, Qingtong, Zhou, Suwen, Zhao   +4 more
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