Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines.
about
Drugs for allosteric sites on receptorsExploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinStructure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders.Molecular Insights into Metabotropic Glutamate Receptor Allosteric ModulationPositive allosteric modulators of type 5 metabotropic glutamate receptors (mGluR5) and their therapeutic potential for the treatment of CNS disorders.Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5.Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.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).A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signalingProbing 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 receptors as therapeutic targets for schizophrenia.Metabotropic glutamate receptor 4 (mGlu4)-positive allosteric modulators for the treatment of Parkinson's disease: historical perspective and review of the patent literature.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 indicationsDiscovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists.A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 and Glucagon Receptors.Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild TypeSynthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold.Acyl-2-aminobenzimidazoles: a novel class of neuroprotective agents targeting mGluR5Synthesis and SAR of substituted pyrazolo[1,5-a]quinazolines as dual mGlu(2)/mGlu(3) NAMs.Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold.Cyclopropyl-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5.Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator.Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity.Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.mGluR4 positive allosteric modulators with potential for the treatment of Parkinson's disease: WO09010455.In vitro binding of a radio-labeled positive allosteric modulator for metabotropic glutamate receptor subtype 5.Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype.Triple-addition assay protocols for detecting and characterizing modulators of seven-transmembrane receptors.In silico studies targeting G-protein coupled receptors for drug research against Parkinson's disease.
P2860
Q27006721-D3F277C3-D4B1-4BB5-9AFC-B8DED38218BBQ30427775-CC60548C-25A7-4A2A-9DEF-1478C1A75CA9Q33856038-A783731B-19E7-472C-98A3-FCA2F78D65BEQ33894613-3275E238-BF1A-423B-8FB0-C3992FF79AF5Q34243209-765AFA7A-EDCB-4560-96A3-FF32FB51E9A1Q34399823-7DC0EB49-D0FC-482E-9E89-97104087A958Q34468639-291D5C3F-374E-46DB-BDF1-C560E8C69CD8Q34761363-504C1BD2-D487-4651-998A-286CFB8CE651Q34850993-F64405B4-BB0A-4592-ADD8-F1707047CC5FQ35688485-47773E43-864C-4183-BD69-15B1EBB3746FQ35952381-89083408-83A6-494B-B168-774FCB2C4D6AQ36015452-4778A1AC-AA08-406B-9A3E-1DD26E19A5D7Q36717066-84F97EBA-B1F4-478A-AC3E-0B2BF8293730Q36776760-CFDB8200-F9D4-4E3D-A699-6D37486E3A07Q37183072-95D0377E-3EDB-482D-94EC-106C60421E60Q37422727-9702ED12-015B-4CBA-9D06-6434B942D50DQ37709393-17EC57E0-62EC-469C-B7AE-C18D80AEE2A5Q37845809-1C551B01-418E-48C2-9F95-AF38919B6957Q37881198-B45F0C59-64CB-4E42-B3EF-EE427CD3879EQ38002888-F3DF78BB-338C-4CA2-9A8A-D30CAC6BCCBEQ38162957-4723C7D1-DCE6-498E-A78F-851A6EC0FE95Q38209092-D38BAC0C-8D8D-4238-BB73-FA4945DC8379Q38551529-A2E05E92-A22A-4FF8-918C-812278B63432Q39024066-9772D6B2-4501-4659-ACF1-4A27CBE9FAECQ39346114-0A5F3838-DD96-4440-9DB6-47EC1E595891Q40435465-E53A41B8-5A8E-4835-8417-2545359FA4D5Q41136066-09095ADF-969C-401A-8CD9-94CAD910609AQ41438539-0FFBA564-9CFD-4F04-9019-B9BB0D481109Q41469232-599858E9-76BF-49ED-B3F7-081A795B55B4Q41820126-7182F5F5-0406-4764-97C9-D4F38F030BD9Q41855122-6E19F6BA-87F9-4557-A1A4-C00D839F6094Q42557866-A573278A-17D1-46AB-8880-4A0942998103Q42572290-D10F153F-CD48-4DD6-8A0F-FB8763F97B16Q42573965-9D27FEF1-21D0-434E-A082-981ED4B29599Q43151764-49DA034E-AE28-4276-B870-36C2C0B1C345Q45397715-297B2590-64C7-46AA-A188-303C4E006D00Q46379917-C40C5481-8756-4B69-BE08-1ACFD93C3F8CQ50877969-A9FB6D01-FDB8-45BE-B2E0-508702E31D6AQ52665081-055F9E2B-D558-4534-9AEC-3463FA471635
P2860
Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines.
description
2009 nî lūn-bûn
@nan
2009年の論文
@ja
2009年学术文章
@wuu
2009年学术文章
@zh-cn
2009年学术文章
@zh-hans
2009年学术文章
@zh-my
2009年学术文章
@zh-sg
2009年學術文章
@yue
2009年學術文章
@zh
2009年學術文章
@zh-hant
name
Discovery of molecular switche ...... 5-(phenylethynyl)pyrimidines.
@en
type
label
Discovery of molecular switche ...... 5-(phenylethynyl)pyrimidines.
@en
prefLabel
Discovery of molecular switche ...... 5-(phenylethynyl)pyrimidines.
@en
P2093
P2860
P356
P1476
Discovery of molecular switche ...... 5-(phenylethynyl)pyrimidines.
@en
P2093
Alice L Rodriguez
Carrie K Jones
Jeffrey Kedrowski
Jerri M Rook
Randy L Smith
Sameer Sharma
P2860
P304
P356
10.1021/JM900654C
P407
P577
2009-07-01T00:00:00Z