Results 111 to 120 of about 36,012 (161)

Negative allosteric modulation of CB1 cannabinoid receptor signalling decreases intravenous morphine self-administration and relapse in mice. [PDF]

Addict Biol
Oliva I, Kazi F, Cantwell LN, Thakur GA, Crystal JD, Hohmann AG.   +5 more
europepmc   +1 more source

Allosteric modulation of the CXCR4:CXCL12 axis by targeting receptor nanoclustering via the TMV-TMVI domain. [PDF]

Elife
García-Cuesta EM, Martínez P, Selvaraju K, Ulltjärn G, Gómez Pozo AM, D'Agostino G, Gardeta S, Quijada-Freire A, Blanco Gabella P, Roca C, Hoyo DD, Jiménez-Saiz R, García-Rubia A, Soler Palacios B, Lucas P, Ayala-Bueno R, Santander Acerete N, Carrasco Y, Oscar Sorzano C, Martinez A, Campillo NE, Jensen LD, Rodriguez Frade JM, Santiago C, Mellado M.   +24 more
europepmc   +1 more source

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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

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
openaire   +5 more sources

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).
openaire   +2 more sources

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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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 Modulation of Dopamine Receptors

Mini-Reviews in Medicinal Chemistry, 2005
Allosteric modulators allow for the fine-tuning of receptor responses to endogenous neurotransmitters and exogenous therapeutic agents. Different types of allosteric modulation of dopamine receptors are discussed as well as the significance of such modulation in the control of normal biological processes and in the treatment of disease.
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Allosteric modulation of muscarinic acetylcholine receptors

Trends in Pharmacological Sciences, 1995
Five subtypes of muscarinic acetylcholine receptors have been identified in mammalian tissues, but the selectivity of ligands that are active at these receptors is low. It is possible, however, that selective compounds may be developed by targeting their allosteric site(s).
S, Tucek, J, Proska
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