Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery
about
Discovery 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)Drug Repurposing Is a New Opportunity for Developing Drugs against Neuropsychiatric DisordersThe role of serotonin 5-HT2A receptors in memory and cognitionThe concept of allosteric interaction and its consequences for the chemistry of the brainDrugs for allosteric sites on receptorsPositive allosteric modulators of the μ-opioid receptor: a novel approach for future pain medicationsEndogenous vs Exogenous Allosteric Modulators in GPCRs: A dispute for shuttling CB1 among different membrane microenvironments.Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probeDevelopment of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)Discovery of ML326: The first sub-micromolar, selective M5 PAMDiscovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375)Potentiation of insulin-mediated glucose lowering without elevated hypoglycemia risk by a small molecule insulin receptor modulatorAllosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's diseaseVirtual screening on an α-helix to β-strand switchable region of the FGFR2 extracellular domain revealed positive and negative modulators.Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence.Exploration 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)picolinSubstituted 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.N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169.G protein-coupled receptors in cardiac biology: old and new receptorsSerotonin at the nexus of impulsivity and cue reactivity in cocaine addiction.2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1).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.Allosteric transition: a comparison of two modelsStructure-based ligand discovery targeting orthosteric and allosteric pockets of dopamine receptors.Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.Copper-promoted synthesis of 1,4-benzodiazepinones via alkene diamination.Interplay between Structure and Charge as a Key to Allosteric Modulation of Human 20S Proteasome by the Basic Fragment of HIV-1 Tat ProteinComputational Advances for the Development of Allosteric Modulators and Bitopic Ligands in G Protein-Coupled ReceptorsStructure-activity relationships of substituted 1H-indole-2-carboxamides as CB1 receptor allosteric modulators.Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypesTotal synthesis and biological evaluation of phidianidines A and B uncovers unique pharmacological profiles at CNS targets.Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.Integrated In Silico Fragment-Based Drug Design: Case Study with Allosteric Modulators on Metabotropic Glutamate Receptor 5.Novel selective allosteric and bitopic ligands for the S1P(3) receptor.Modulation of pyramidal cell output in the medial prefrontal cortex by mGluR5 interacting with CB1.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.Allosteric Modulation of G Protein-Coupled Receptors: An Emerging Approach of Drug Discovery.
P2860
Q24625985-02AD8B15-7AB0-4FC6-919D-6856D20F6F24Q26748728-EE2B329C-D05C-467D-8846-06B60CDDA8E1Q26779278-0D6C5C37-A405-44FE-8BC7-EA7C9989E1E7Q26827321-C9154679-6BFE-4AF1-AA21-3E655B0E2A24Q27006721-0CE5D14B-D565-4413-942D-82BCBEFE2313Q27027736-DA74B63F-04D1-4571-8D6D-1A1A230E4620Q27308091-867CD7BB-393F-4C02-B341-7520F38527BFQ28237300-B617A646-1E23-4C09-BCE4-4869FE52A59CQ28246512-83EE38A4-1EF0-4E52-B042-3ACB1D220F9DQ28288485-598EAD64-7869-4458-9795-E7CF1A90ADD7Q28300950-56186E34-E534-4B7B-AB4C-0188397626C4Q28544827-215E990C-F5A8-4D5C-B2AC-C6A2AE5E841CQ28660933-549938E1-E2CC-43E1-B0FC-75FCC2FA8C10Q30365357-8C36A803-B6D1-47EF-AFE6-5E49B5B68281Q30414307-4437AEEB-E69E-4287-92F8-1768411215D0Q30427775-5BF042E6-94C2-4FD4-B789-6F42208F0CB9Q30432649-EFF4EFB3-CD27-47EB-A7CF-202B7DBBFC98Q30435534-8FB88ABC-CEB2-42F4-90B8-6F0620516055Q30446914-DA69D614-40C7-4C97-BAFF-FE2483D16D49Q33639685-EE127481-EC68-4BD6-8FF4-248B25C065B8Q33874819-FFE75766-8C46-4B95-89AF-AD232B8A2A7FQ34243209-D8B3A718-5410-40D0-9188-C32F01837399Q34243225-6228237C-456A-4126-8354-1A61FC1B9E71Q34373958-3168FDBB-BEF5-49C0-BED4-CDD37AFF1F19Q34399823-A2882D59-CF33-4183-90AF-8709E2087E74Q34539431-CEE2914D-D045-415E-81C1-E0F7B038F76AQ34983219-878EF30D-6EDE-4D92-845F-5E0F5925E24FQ35534556-99028B49-E538-4625-AE4F-83FC5DC1EC2DQ35664392-FA93F0F4-E484-4ACA-A61F-8D9B2247FE51Q35843506-9CDBE589-CFA5-4312-AF1C-6A3EE3F1DBBEQ35967903-DD9AF7CF-730D-4AB9-9446-70D7371B0C5BQ35990953-B8ED4E46-DE7C-4F40-A8E8-639E12E8FF31Q36098318-0311D44F-6201-4FEB-B0DB-B8A0C37F0676Q36248536-BC3E9AD8-A88C-4A6B-AADC-95ECD1C24136Q36335613-63D2DF9A-6056-423D-B285-D69DC30898FDQ36385771-117462AB-05C1-45EF-94B7-D08A8FB6775CQ36484486-A14DC6C6-5360-48AC-967D-67752A27D870Q36598822-C44C1A3B-52DB-4B89-A7F0-4063981A71F7Q36776760-0052AA10-757D-4F03-A681-C2F8C9257A9EQ36856715-102FD6F5-D349-4ECA-802C-AA560B9CC368
P2860
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery
description
2012 nî lūn-bûn
@nan
2012年の論文
@ja
2012年論文
@yue
2012年論文
@zh-hant
2012年論文
@zh-hk
2012年論文
@zh-mo
2012年論文
@zh-tw
2012年论文
@wuu
2012年论文
@zh
2012年论文
@zh-cn
name
Allosteric modulation of seven ...... nervous system drug discovery
@ast
Allosteric modulation of seven ...... nervous system drug discovery
@en
type
label
Allosteric modulation of seven ...... nervous system drug discovery
@ast
Allosteric modulation of seven ...... nervous system drug discovery
@en
prefLabel
Allosteric modulation of seven ...... nervous system drug discovery
@ast
Allosteric modulation of seven ...... nervous system drug discovery
@en
P2093
P2860
P50
P356
P1476
Allosteric modulation of seven ...... nervous system drug discovery
@en
P2093
Arthur Christopoulos
Bruce J Melancon
Corey R Hopkins
Kyle A Emmitte
Michael R Wood
P2860
P304
P356
10.1021/JM201139R
P407
P577
2012-01-06T00:00:00Z