Results 31 to 40 of about 702,558 (291)
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.
openaire +3 more sources
MembranesBioluminescence and fluorescence resonance energy transfer (BRET and FRET) together with the proximity ligation method revealed the existence of G-protein-coupled receptors, Ionotropic and Receptor tyrosine kinase heterocomplexes, e.g., A2AR–D2R, GABAA ...
Marina Mirchandani-Duque +9 more
doaj +1 more source
Modulation of Allosteric Control and Evolution of Hemoglobin
Biomolecules, 2023 Allostery arises when a ligand-induced change in shape of a binding site of a protein is coupled to a tertiary/quaternary conformational change with a consequent modulation of functional properties. The two-state allosteric model of Monod, Wyman and Changeux [J. Mol. Biol.
Maurizio Brunori, Adriana Erica Miele
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Ligand recognition and allosteric modulation of the human MRGPRX1 receptor [PDF]
, 2023 The human MAS-related G protein–coupled receptor X1 (MRGPRX1) is preferentially expressed in the small-diameter primary sensory neurons and involved in the mediation of nociception and pruritus.
Liu, Y +10 more
core +1 more source
Allosteric modulation of glycine receptors [PDF]
British Journal 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 ...
Yévenes, G E, Zeilhofer, Hanns Ulrich
openaire +4 more sources
Review on allosteric modulators of dopamine receptors so far
Health Science ReportsBackground Contemporary research is predominantly directed towards allosteric modulators, a class of compounds designed to interact with specific sites distinct from the orthosteric site on G protein‐coupled receptors.
Fentaw Girmaw
doaj +1 more source
AI-Driven Design of Miniproteins as Potential Allosteric Modulators
PharmaceuticalsAllosteric modulation has emerged as a powerful strategy for achieving superior selectivity and safety in drug discovery and protein function regulation.
Xin Liu +4 more
doaj +1 more source
Correction for Inhibition Leads to an Allosteric Co-Agonist Model for Pentobarbital Modulation and Activation of α1β3γ2L GABAA Receptors. [PDF]
PLoS ONE, 2016 BACKGROUND:Pentobarbital, like propofol and etomidate, produces important general anesthetic effects through GABAA receptors. Photolabeling also indicates that pentobarbital binds to some of the same sites where propofol and etomidate act.
Alexis M Ziemba, Stuart A Forman
doaj +1 more source
Engineering peptides into antibodies—opportunities and strategies for therapeutic innovation
FEBS Letters, EarlyView.Peptides and antibodies occupy complementary therapeutic niches. Peptides recognize difficult targets in a compact format, while antibodies add specificity, long half‐life, and effector functions. This review examines strategies that merge both modalities—peptide grafting into loops, terminal and Fc fusions, and bioconjugation—highlighting how ...
Jinling Wang +2 more
wiley +1 more source
Structurally similar allosteric modulators of α7 nicotinic acetylcholine receptors exhibit five distinct pharmacological effects. [PDF]
, 2015 Activation of nicotinic acetylcholine receptors (nAChRs) is associated with the binding of agonists such as acetylcholine to an extracellular site that is located at the interface between two adjacent receptor subunits.
Dhankher, P +4 more
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