Results 121 to 130 of about 36,012 (161)

Allosteric modulation of nicotinic acetylcholine receptors

Biochemical Pharmacology, 2007
Allosteric modulation refers to the concept that proteins could exist in multiple conformational states and that binding of allosteric ligands alters the energy barriers or "isomerization coefficients" between various states. In the context of ligand gated ion channels such as nicotinic acetylcholine receptors (nAChRs), it implies that endogenous ...
Daniel, Bertrand, Murali, Gopalakrishnan
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Allosteric modulation of nicotinic acetylcholine receptors

Biochemical Pharmacology, 2015
Nicotinic acetylcholine receptors (nAChRs) are receptors for the neurotransmitter acetylcholine and are members of the 'Cys-loop' family of pentameric ligand-gated ion channels (LGICs). Acetylcholine binds in the receptor extracellular domain at the interface between two subunits and research has identified a large number of nAChR-selective ligands ...
Anna, Chatzidaki, Neil S, Millar
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Allosteric Adenosine Modulation to Reduce Allodynia

Anesthesiology, 2001
Background Adenosine and adenosine agonists reduce hypersensitivity following inflammation and peripheral nerve injury models of chronic pain. Because inhibitors of adenosine reuptake or metabolism are also effective at reducing hypersensitivity, it is likely that there is a tonic release of spinal adenosine in these models ...
H L, Pan, Z, Xu, E, Leung, J C, Eisenach
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Allosteric Modulation of Intrinsically Disordered Proteins

2019
The allosteric property of globular proteins is applauded as their intrinsic ability to regulate distant sites, and this property further plays a critical role in a wide variety of cellular regulatory mechanisms. Recent advancements and studies have revealed the manifestation of allostery in intrinsically disordered proteins or regions as allosteric ...
Ashfaq Ur, Rehman, Mueed Ur, Rahman, Taaha, Arshad, Hai-Feng, Chen   +3 more
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Fused heterocyclic M1 positive allosteric modulators

Bioorganic & Medicinal Chemistry Letters, 2011
Fused aromatics such as naphthalene were identified as highly potent and CNS penetrant M(1) positive allosteric modulators during an SAR study to replace the phenyl B-ring linkage.
Scott D, Kuduk, Christina N, Di Marco, Victoria, Cofre, William J, Ray, Lei, Ma, Marion, Wittmann, Matthew A, Seager, Kenneth A, Koeplinger, Charles D, Thompson, George D, Hartman, Mark T, Bilodeau   +10 more
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Muscarinic Receptors Allosteric Modulation

2016
This chapter describes recent activity in the advancement of ligands and therapeutic lead compounds for the allosteric modulation of the muscarinic receptors and their potential utility as therapies for central nervous system (CNS) disorders. The chapter reviews the activity over the past five years of allosteric modulation of the muscarinic receptor ...
Bruce J. Melancon, Corey R. Hopkins
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Profiling Allosteric Modulators of CB₁R with an Allosteric Fluoroprobe

Angewandte Chemie
AbstractAllosteric modulation of cannabinoid receptor type 1 (CB1R) offers a promising alternative to conventional therapeutic approaches using orthosteric ligands (OLs). Currently, CB1R allosteric modulators (AMs) are characterized based on their ability to modulate binding or functional response of OLs, preventing isolation of individual ...
Miroslav Kosar, Themiya Perera, Rudolf L. Z. Ganzoni, Roman C. Sarott, Leire Borrega‐Roman, Rosa Maria Vitale, Alessia Ligresti, Arne C. Rufer, Wolfgang Guba, Uwe Grether, Erick M. Carreira, Dmitry B. Veprintsev, David A. Sykes   +12 more
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Allosteric modulators of human A2B adenosine receptor

Biochimica et Biophysica Acta (BBA) - General Subjects, 2014
Among adenosine receptors (ARs) the A2B subtype exhibits low affinity for the endogenous agonist compared with the A1, A2A, and A3 subtypes and is therefore activated when concentrations of adenosine increase to a large extent following tissue damages (e.g. ischemia, inflammation).
TRINCAVELLI, MARIA LETIZIA, GIACOMELLI, CHIARA, DANIELE, SIMONA, TALIANI, SABRINA, Cosimelli B, Laneri S, Severi E, BARRESI, ELISABETTA, Pugliesi I, Greco G, Novellino E, DA SETTIMO PASSETTI, FEDERICO, MARTINI, CLAUDIA   +12 more
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Allosteric Modulation of G Protein-Coupled Receptors

Current Pharmaceutical Design, 2004
The past decade has witnessed a significant growth in the identification of allosteric modulators of G protein–coupled receptors (GPCRs), i.e., ligands that interact with binding sites that are topographically distinct from the orthosteric site recognized by the receptor's endogenous agonist.
L T, May, V A, Avlani, P M, Sexton, A, Christopoulos   +3 more
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Allosteric Modulation of G-Protein–Coupled Receptors

Expert Opinion on Therapeutic Patents, 2001
Allosteric modulation of G protein-coupled receptors has recently been recognized as an alternative approach for selectivity in drug action. Allosteric modulators that enhance or diminish the effects of (endogenous) agonists or antagonists on a variety of G protein-coupled receptors are described in this review, with emphasis on the latest developments
Willem, Soudijn, Ineke, van Wijngaarden, Ad P, IJzerman   +2 more
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