Results 21 to 30 of about 3,750,504 (279)
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
doaj +1 more source
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
core +7 more sources
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
doaj +1 more source
Negative Allosteric Modulators of mGlu7 Receptor as Putative Antipsychotic Drugs [PDF]
Frontiers in Molecular Neuroscience, 2018 The data concerning antipsychotic-like activity of negative allosteric modulators (NAMs)/antagonists of mGlu7 receptors are limited. The only available ligands for this receptor are MMPIP and ADX71743. In the present studies, we used stable cell line expressing mGlu7 receptor and it was shown that both compounds dose-dependently potentiated forskolin ...
Cieslik, Paulina +12 more
openaire +4 more sources
Discovery of a Negative Allosteric Modulator of GABAB Receptors [PDF]
ACS Medicinal Chemistry Letters, 2014 Initialized from the scaffold of CGP7930, an allosteric agonist of GABAB receptors, a series of noncompetitive antagonists were discovered. Among these compounds, compounds 3, 6, and 14 decreased agonist GABA-induced maximal effect of IP3 production in HEK293 cells overexpressing GABAB receptors and Gqi9 proteins without changing the EC50. Compounds 3,
Lin-Hai, Chen +6 more
openaire +2 more sources
Frontiers in Pharmacology, 2021 The development of GPCR (G-coupled protein receptor) allosteric modulators has attracted increasing interest in the last decades. The use of allosteric modulators in therapy offers several advantages with respect to orthosteric ones, as they can fine ...
Elisabetta Barresi +6 more
doaj +1 more source
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
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
doaj +1 more source
BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder [PDF]
ACS Medicinal Chemistry Letters, 2018 Hyunsoo Park, Jianqing Li, James Kempson
exaly +2 more sources
GABAA receptor: Positive and negative allosteric modulators [PDF]
Neuropharmacology, 2018 gamma-Aminobutyric acid (GABA)-mediated inhibitory neurotransmission and the gene products involved were discovered during the mid-twentieth century. Historically, myriad existing nervous system drugs act as positive and negative allosteric modulators of these proteins, making GABA a major component of modern neuropharmacology, and suggesting that many
openaire +2 more sources