Understanding the Allosteric Modulation of PTH1R by a Negative Allosteric Modulator
Cells, 2022 The parathyroid hormone type 1 receptor (PTH1R) acts as a canonical class B G protein-coupled receptor, regulating crucial functions including calcium homeostasis and bone formation.
Mengrong Li +5 more
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Allosteric modulation of chemoattractant receptors [PDF]
Frontiers in Immunology, 2016 Chemoattractants control selective leukocyte homing via interactions with a dedicated family of related GPCR. Emerging evidence indicates that the signalling activity of these receptors, as for other GPCR, is influenced by allosteric modulators, which ...
Maria Candida Cesta +3 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 +5 more
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Mechanism of Allosteric Modulation of the Cys-loop Receptors [PDF]
Pharmaceuticals, 2010 The cys-loop receptor family is a major family of neurotransmitter-operated ion channels. They play important roles in fast synaptic transmission, controlling neuronal excitability, and brain function.
Paul Whiteaker +2 more
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Coarse-grained models of biomolecule dynamics and allostery [PDF]
, 2010 Recently, it has become increasingly accepted that thermal fluctuations take active part in functional tasks of biological molecules. We employ a set of coarse-grained models to investigate the mechanism of transmission of allosteric signal via spatial ...
Toncrova, Hedvika
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Allo-network drugs: Extension of the allosteric drug concept to protein-protein interaction and signaling networks [PDF]
, 2013 Allosteric drugs are usually more specific and have fewer side effects than orthosteric drugs targeting the same protein. Here, we overview the current knowledge on allosteric signal transmission from the network point of view, and show that most ...
Csermely, Péter +3 more
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Disorder driven allosteric control of protein activity
Current Research in Structural Biology, 2020 Studies of protein allostery increasingly reveal an involvement of the back and forth order-disorder transitions in this mechanism of protein activity regulation.
Wei-Ven Tee +2 more
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In silico Insights on the Allosteric Modulation of the µ-Opioid Receptor and G protein Complex in the Presence of Agonist Ligand BU72 and Potential Positive Allosteric Modulator BMS-986121 [PDF]
, 2020 The G protein-coupled receptor (GPCR) µ-opioid receptor (µOR) is one of several drug targets of commercially available therapeutics for pain. Various opioid drugs like morphines have been associated to numerous substance abuse-related deaths around the ...
Ricky, Nellas, Mac Kevin, Braza
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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
core +1 more source
Pharmaceutics, 2022 The acquisition of penicillin-binding protein (PBP) 2a in resistant strains of Staphylococcus aureus allows for the continuous production of cell walls even after the inactivation of intrinsic PBPs. Thus, the discovery of novel therapeutics with enhanced
Jamiu Olaseni Aribisala, Saheed Sabiu
doaj +1 more source