"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.
about
Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenicsDiscovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM)Itraconazole and arsenic trioxide inhibit Hedgehog pathway activation and tumor growth associated with acquired resistance to smoothened antagonistsPositive allosteric modulators of metabotropic glutamate 2 receptors in schizophrenia treatmentDrugs for allosteric sites on receptorsG-protein-coupled receptors targeting: the allosteric approachNovel Allosteric Modulators of G Protein-coupled ReceptorsEmerging Computational Methods for the Rational Discovery of Allosteric Drugs.Virtual screening on an α-helix to β-strand switchable region of the FGFR2 extracellular domain revealed positive and negative modulators.The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptorsTetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound.2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.Action of molecular switches in GPCRs--theoretical and experimental studies.Development of allosteric modulators of GPCRs for treatment of CNS disordersOpportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders.Molecular Insights into Metabotropic Glutamate Receptor Allosteric ModulationProfound methyl effects in drug discovery and a call for new C-H methylation reactions.Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discoveryProgress toward positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signalingThe role of allostery in the ubiquitin-proteasome systemSensing conformational changes in metabotropic glutamate receptors.Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology.The Emerging Role of Metabotropic Glutamate Receptors in the Pathophysiology of Chronic Stress-Related DisordersPractical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate ReceptorsAllosteric modulators for the treatment of schizophrenia: targeting glutamatergic networksBiotransformation of a novel positive allosteric modulator of metabotropic glutamate receptor subtype 5 contributes to seizure-like adverse events in rats involving a receptor agonism-dependent mechanism.Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site.Metabotropic glutamate receptor 4 (mGlu4)-positive allosteric modulators for the treatment of Parkinson's disease: historical perspective and review of the patent literature.Molecular alliance-from orthosteric and allosteric ligands to dualsteric/bitopic agonists at G protein coupled receptors.Allosteric modulation of Class C GPCRs: a novel approach for the treatment of CNS disorders.Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004-2012).Allostery and compartmentalization: old but not forgotten.Progress toward advanced understanding of metabotropic glutamate receptors: structure, signaling and therapeutic indicationsDiscovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition.Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine coreLead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core.Metabotropic glutamate receptor subtype 5: molecular pharmacology, allosteric modulation and stimulus bias
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"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.
description
article científic
@ca
article scientifique
@fr
articolo scientifico
@it
artigo científico
@pt
bilimsel makale
@tr
scientific article published on 04 March 2011
@en
vedecký článok
@sk
vetenskaplig artikel
@sv
videnskabelig artikel
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vědecký článek
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name
"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.
@en
"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.
@nl
type
label
"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.
@en
"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.
@nl
prefLabel
"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.
@en
"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.
@nl
P2860
P50
P356
P1433
P1476
"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.
@en
P2093
John T Brogan
Michael R Wood
P2860
P304
P356
10.1021/BI200129S
P407
P577
2011-03-04T00:00:00Z