Allosteric Modulation of Chemoattractant Receptors [PDF]
Frontiers in Immunology, 2016 Chemoattractants control selective leukocyte homing via interactions with a dedicated family of related G protein-coupled receptor (GPCR). Emerging evidence indicates that the signaling activity of these receptors, as for other GPCR, is influenced by allosteric modulators, which interact with the receptor in a binding site distinct from the binding ...
Maria Candida Cesta +3 more
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Prospects for the use of allosteric drugs in real-world clinical practice
Реальная клиническая практика: данные и доказательства, 2023 While the clinical validity of the use of allosteric regulation is known, scientists are working on the discovery of new methods for the development of allosteric drugs that can modulate the functions of enzymes, depending on the desired therapeutic ...
I. R. Svechkareva, A. S. Kolbin
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Recent Advances in the Discovery of Nicotinic Acetylcholine Receptor Allosteric Modulators
Molecules, 2023 Positive allosteric modulators (PAMs), negative allosteric modulators (NAMs), silent agonists, allosteric activating PAMs and neutral or silent allosteric modulators are compounds capable of modulating the nicotinic receptor by interacting at allosteric ...
Dina Manetti +6 more
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An allosteric modulator binds to a conformational hub in the β2 adrenergic receptor [PDF]
, 2020 Most drugs acting on G-protein-coupled receptors target the orthosteric binding pocket where the native hormone or neurotransmitter binds. There is much interest in finding allosteric ligands for these targets because they modulate physiologic signaling ...
Hirata, Kunio +31 more
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Surface dynamics in allosteric regulation of protein-protein interactions: modulation of calmodulin functions by Ca2+. [PDF]
PLoS Computational Biology, 2013 Knowledge of the structural basis of protein-protein interactions (PPI) is of fundamental importance for understanding the organization and functioning of biological networks and advancing the design of therapeutics which target PPI.
Yosef Y Kuttner +2 more
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COR758, a negative allosteric modulator of GABAB receptors [PDF]
, 2021 Allosteric modulators of G protein coupled receptors (GPCRs), including GABABRs (GABABRs), are promising therapeutic candidates. While several positive allosteric modulators (PAM) of GABABRs have been characterized, only recently the first negative ...
Ferraro, Luca +12 more
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Biochemical pharmacology of the positive allosteric modulation of the GABAb receptor "in Vitro" and "in Vivo" [PDF]
, 2007 Allosteric modulators of G-protein coupled receptors (GPCRs) interact with binding sites on the receptor molecule that are topographically distinct from the classic orthosteric site.
Gjoni, Tina
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Development of allosteric modulators of GPCRs for treatment of CNS disorders
Neurobiology of Disease, 2014 The discovery of allosteric modulators of G protein-coupled receptors (GPCRs) provides a promising new strategy with potential for developing novel treatments for a variety of central nervous system (CNS) disorders.
Hilary Highfield Nickols +1 more
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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 +15 more
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Allosteric modulation of adenosine receptors [PDF]
Purinergic Signalling, 2008 Allosteric ligands for G protein-coupled receptors (GPCRs) may alter receptor conformations induced by an orthosteric ligand. These modulators can thus fine-tune classical pharmacological responses. In this review we will describe efforts to synthesize and characterize allosteric modulators for one particular GPCR subfamily, the adenosine receptors ...
Göblyös, Anikó, IJzerman, Ad P.
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