EAR-20 peptide, a novel NMDA receptor positive allosteric modulator [PDF]
Frontiers in PharmacologyAllosteric modulation of ligand-gated ion channels provides a powerful mechanism to fine-tune their activity without competing with endogenous ligands.
Roberto García-Díaz +16 more
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Identification and Characterization of a Phenyl(trifluoro-methyl)-pyrimidine Positive Allosteric Modulator of the Secretin Receptor [PDF]
MembranesG protein-coupled receptors (GPCRs) are among the most common drug targets, with numerous agonists and antagonists approved for clinical use. More recently, it has been appreciated that drugs can also modulate the action of natural agonists of these ...
Kaleeckal G. Harikumar +5 more
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The binding and mechanism of a positive allosteric modulator of Kv3 channels [PDF]
Nature CommunicationsSmall-molecule modulators of diverse voltage-gated K+ (Kv) channels may help treat a wide range of neurological disorders. However, developing effective modulators requires understanding of their mechanism of action.
Qiansheng Liang +11 more
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Gestodene, a novel positive allosteric modulator of PAR1, enhances PAR1-mediated human platelet aggregation [PDF]
Frontiers in PharmacologyBackground: Protease-activated receptor 1 (PAR1) is expressed in human platelets and can be activated by low concentrations of thrombin. Vorapaxar, a selective antagonist of PAR1, inhibits thrombin-induced calcium mobilization in human platelet, which is
So-Hyeon Park +9 more
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Recent Advances in the Discovery of Nicotinic Acetylcholine Receptor Allosteric Modulators
Molecules, 2023 Positive allosteric modulators (PAMs), negative allosteric modulators (NAMs), silent agonists, allosteric activating PAMs and neutral or silent allosteric modulators are compounds capable of modulating the nicotinic receptor by interacting at allosteric ...
Dina Manetti +6 more
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The allosterically modulated FFAR2 is transactivated by signals generated by other neutrophil GPCRs.
PLoS ONE, 2023 Positive allosteric modulators for free fatty acid receptor 2 (FFAR2/GPR43), that affect receptor function through binding to two distinct allosteric binding sites, were used to determine the correlation between the responses induced in neutrophils by ...
Simon Lind +3 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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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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Toxins, 2021 α-conotoxins are 13–19 amino acid toxin peptides that bind various nicotinic acetylcholine receptor (nAChR) subtypes. α-conotoxin Mr1.7c (MrIC) is a 17 amino acid peptide that targets α7 nAChR.
Alican Gulsevin +6 more
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Pharmaceuticals, 2020 Schizophrenia was first described by Emil Krapelin in the 19th century as one of the major mental illnesses causing disability worldwide. Since the introduction of chlorpromazine in 1952, strategies aimed at modifying the activity of dopamine receptors ...
Irene Fasciani +7 more
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