Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists.
about
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 receptorsNovel Allosteric Modulators of G Protein-coupled ReceptorsSubstituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction.Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).Molecular Insights into Metabotropic Glutamate Receptor Allosteric ModulationAllosteric 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).A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signalingDiscovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.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.Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate ReceptorsBiotransformation 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."Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004-2012).Progress toward advanced understanding of metabotropic glutamate receptors: structure, signaling and therapeutic indicationsSynthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold.Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold.Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxietySynthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator.Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
P2860
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P2860
Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists.
description
2010 nî lūn-bûn
@nan
2010年の論文
@ja
2010年論文
@yue
2010年論文
@zh-hant
2010年論文
@zh-hk
2010年論文
@zh-mo
2010年論文
@zh-tw
2010年论文
@wuu
2010年论文
@zh
2010年论文
@zh-cn
name
Discovery of molecular switche ...... PAMs and partial antagonists.
@en
type
label
Discovery of molecular switche ...... PAMs and partial antagonists.
@en
prefLabel
Discovery of molecular switche ...... PAMs and partial antagonists.
@en
P2093
P2860
P50
P1476
Discovery of molecular switche ...... PAMs and partial antagonists.
@en
P2093
Alice L Rodriguez
Darren W Engers
Daryl F Venable
Jeffrey P Lamb
P2860
P304
P356
10.1016/J.BMCL.2010.11.119
P407
P577
2010-12-03T00:00:00Z