Understanding the Allosteric Modulation of PTH1R by a Negative Allosteric Modulator [PDF]
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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Capsaicin Is a Negative Allosteric Modulator of the 5-HT3 Receptor [PDF]
Frontiers in Pharmacology, 2020 In this study, effects of capsaicin, an active ingredient of the capsicum plant, were investigated on human 5-hydroxytryptamine type 3 (5-HT3) receptors.
Eslam El Nebrisi +9 more
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Mechanism and function of GPR3 regulated by a negative allosteric modulator [PDF]
Nature CommunicationsAllosteric modulators have gained substantial interest in current GPCR drug discovery. Here, we present a mechanism of allosteric modulation involving the dimerization of GPR3, a promising drug target for metabolic diseases and central nervous system ...
Geng Chen +9 more
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Identification of a Novel Delta Opioid Receptor Agonist Chemotype with Potential Negative Allosteric Modulator Capabilities [PDF]
Molecules, 2021 The δ-opioid receptor (δOR) holds great potential as a therapeutic target. Yet, clinical drug development, which has focused on δOR agonists that mimic the potent and selective tool compound SNC80 have largely failed.
Yazan J. Meqbil +7 more
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Evidence for Two Modes of Binding of the Negative Allosteric Modulator SB269,652 to the Dopamine D2 Receptor [PDF]
Biomedicines, 2021 SB269,652 has been described as the first negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R), however, the binding mode and allosteric mechanism of action of this ligand remain incompletely understood.
Richard Ågren, Kristoffer Sahlholm
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Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells [PDF]
Nature CommunicationsA promising drug target, SETDB1, is a dual methyl-lysine (Kme) reader and methyltransferase implicated in cancer and neurodegenerative disease progression.
Mélanie Uguen +25 more
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Partial mGlu5 Negative Allosteric Modulator M-5MPEP Demonstrates Antidepressant-Like Effects on Sleep Without Affecting Cognition or Quantitative EEG [PDF]
Frontiers in Neuroscience, 2021 Selective negative allosteric modulators (NAMs) targeting the metabotropic glutamate receptor subtype 5 (mGlu5) demonstrate anxiolytic-like and antidepressant-like effects yet concern regarding adverse effect liability remains.
Kimberly M. Holter +11 more
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Radiprodil, a NR2B negative allosteric modulator, from bench to bedside in infantile spasm syndrome [PDF]
Annals of Clinical and Translational Neurology, 2020 Objective Infantile spasm syndrome (ISS) is an epileptic encephalopathy without established treatment after the failure to standard of care based on steroids and vigabatrin.
Stéphane Auvin +8 more
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Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator [PDF]
eLife, 2017 Light-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex diseases (i.e. chronic pain). JF-NP-26 is an inactive photocaged derivative of the metabotropic glutamate type
Joan Font +17 more
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Negative effect of treatment with mGluR5 negative allosteric modulator AFQ056 on blood biomarkers in young individuals with Fragile X syndrome [PDF]
SAGE Open MedicineBackground: Fragile X syndrome, with an approximate incidence rate of 1 in 4000 males to 1 in 8000 females, is the most prevalent genetic cause of heritable intellectual disability and the most common monogenic cause of autism spectrum disorder. The full
Dragana Protic +22 more
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