Results 1 to 10 of about 40,045 (117)
Structural pharmacology of SV2A reveals an allosteric modulation mechanism in the major facilitator superfamily [PDF]
Nature CommunicationsThe synaptic vesicle glycoprotein 2A (SV2A), a member of the major facilitator superfamily (MFS), is a key target for antiseizure medications and a biomarker for synaptic density imaging.
Shabareesh Pidathala +7 more
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Allosteric Modulation of Muscarinic Acetylcholine Receptors
Pharmaceuticals, 2010 An allosteric modulator is a ligand that binds to an allosteric site on the receptor and changes receptor conformation to produce increase (positive cooperativity) or decrease (negative cooperativity) in the binding or action of an orthosteric agonist (e.
Esam E. El-Fakahany, Jan Jakubík
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Current Advances in Allosteric Modulation of Muscarinic Receptors
Biomolecules, 2020 Allosteric modulators are ligands that bind to a site on the receptor that is spatially separated from the orthosteric binding site for the endogenous neurotransmitter.
Jan Jakubik, Esam E. El-Fakahany
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Conformational fingerprinting of allosteric modulators in metabotropic glutamate receptor 2
eLife, 2022 Activation of G protein-coupled receptors (GPCRs) is an allosteric process. It involves conformational coupling between the orthosteric ligand binding site and the G protein binding site. Factors that bind at non-cognate ligand binding sites to alter the
Brandon Wey-Hung Liauw +5 more
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Glycine Transporter 2: Mechanism and Allosteric Modulation
Frontiers in Molecular Biosciences, 2021 Neurotransmitter sodium symporters (NSS) are a subfamily of SLC6 transporters responsible for regulating neurotransmitter signalling. They are a major target for psychoactive substances including antidepressants and drugs of abuse, prompting substantial ...
Zachary J. Frangos +2 more
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Allosteric modulation of gonadotropin receptors
Frontiers in Endocrinology, 2023 Gonadotropins regulate reproductive functions by binding to G protein-coupled receptors (FSHR and LHCGR) expressed in the gonads. They activate multiple, cell-specific signalling pathways, consisting of ligand-dependent intracellular events.
Clara Lazzaretti +6 more
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eLife, 2023 Allosteric modulation of G protein-coupled receptors (GPCRs) is a major paradigm in drug discovery. Despite decades of research, a molecular-level understanding of the general principles that govern the myriad pharmacological effects exerted by GPCR ...
Ziva Vuckovic +23 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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A Structure-Based Allosteric Modulator Design Paradigm
Health Data Science, 2023 Importance: Allosteric drugs bound to topologically distal allosteric sites hold a substantial promise in modulating therapeutic targets deemed undruggable at their orthosteric sites. Traditionally, allosteric modulator discovery has predominantly relied
Mingyu Li +3 more
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Chronic cough relief by allosteric modulation of P2X3 without taste disturbance
Nature Communications, 2023 P2X receptors are cation channels that sense extracellular ATP. Many therapeutic candidates targeting P2X receptors have begun clinical trials or acquired approval for the treatment of refractory chronic cough (RCC) and other disorders.
Chang-Run Guo +17 more
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