Results 1 to 10 of about 35,992 (141)
Allosteric modulation of gonadotropin receptors [PDF]
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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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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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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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 Muscarinic Acetylcholine Receptors [PDF]
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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Allosteric modulation by the fatty acid site in the glycosylated SARS-CoV-2 spike [PDF]
eLifeThe spike protein is essential to the SARS-CoV-2 virus life cycle, facilitating virus entry and mediating viral-host membrane fusion. The spike contains a fatty acid (FA) binding site between every two neighbouring receptor-binding domains.
A Sofia F Oliveira +9 more
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Allosteric Modulation of αβδ GABAA Receptors [PDF]
Pharmaceuticals, 2010 GABAA receptors mediate the majority of the fast inhibition in the mature brain and play an important role in the pathogenesis of many neurological and psychiatric disorders.
Hua-Jun Feng
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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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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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