Allosteric modulator ORG27569 induces CB1 cannabinoid receptor high affinity agonist binding state, receptor internalization, and Gi protein-independent ERK1/2 kinase activation
about
Modulation of cellular redox homeostasis by the endocannabinoid systemMinireview: From the bench, toward the clinic: therapeutic opportunities for cannabinoid receptor modulationRegulation of G protein-coupled receptors by allosteric ligandsThe dynamic nature of type 1 cannabinoid receptor (CB(1) ) gene transcriptionEndogenous vs Exogenous Allosteric Modulators in GPCRs: A dispute for shuttling CB1 among different membrane microenvironments.Ligand-specific endocytic dwell times control functional selectivity of the cannabinoid receptor 1Computational analysis of the CB1 carboxyl-terminus in the receptor-G protein complexComputationally-predicted CB1 cannabinoid receptor mutants show distinct patterns of salt-bridges that correlate with their level of constitutive activity reflected in G protein coupling levels, thermal stability, and ligand binding.Mapping Cannabinoid 1 Receptor Allosteric Site(s): Critical Molecular Determinant and Signaling Profile of GAT100, a Novel, Potent, and Irreversibly Binding Probe.In-vivo pharmacological evaluation of the CB1-receptor allosteric modulator Org-27569CB1 allosteric modulator Org27569 is an antagonist/inverse agonist of ERK1/2 signaling.Effects of the cannabinoid CB₁ receptor allosteric modulator ORG 27569 on reinstatement of cocaine- and methamphetamine-seeking behavior in ratsDiarylureas 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).Behavioral effects of the cannabinoid CB1 receptor allosteric modulator ORG27569 in ratsOptimization of chemical functionalities of indole-2-carboxamides to improve allosteric parameters for the cannabinoid receptor 1 (CB1).Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders.HPLC-MS-MS Determination of ZCZ-011, A Novel Pharmacological Tool for Investigation of the Cannabinoid Receptor in Mouse Brain Using Clean Screen FASt™ Column Extraction.Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).Allosteric Modulation: An Alternate Approach Targeting the Cannabinoid CB1 Receptor.Disruption of the Na+ ion binding site as a mechanism for positive allosteric modulation of the mu-opioid receptor.(4-(Bis(4-fluorophenyl)methyl)piperazin-1-yl)(cyclohexyl)methanone hydrochloride (LDK1229): a new cannabinoid CB1 receptor inverse agonist from the class of benzhydryl piperazine analogs.Structural dynamics and energetics underlying allosteric inactivation of the cannabinoid receptor CB1.Computational 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.Aiming for allosterism: Evaluation of allosteric modulators of CB1 in a neuronal model.Peptide-guided targeting of GPR55 for anti-cancer therapy.Drug discovery strategies that focus on the endocannabinoid signaling system in psychiatric disease.Anti-inflammatory lipoxin A4 is an endogenous allosteric enhancer of CB1 cannabinoid receptorCB(1) receptor allosteric modulators display both agonist and signaling pathway specificity.Juxtaglomerular cell CaSR stimulation decreases renin release via activation of the PLC/IP(3) pathway and the ryanodine receptor.Profiling two indole-2-carboxamides for allosteric modulation of the CB1 receptor.Distinct roles of β-arrestin 1 and β-arrestin 2 in ORG27569-induced biased signaling and internalization of the cannabinoid receptor 1 (CB1).Computational Prediction and Biochemical Analyses of New Inverse Agonists for the CB1 ReceptorPractical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate ReceptorsReal-time characterization of cannabinoid receptor 1 (CB1 ) allosteric modulators reveals novel mechanism of action.Molecular basis of cannabinoid CB1 receptor coupling to the G protein heterotrimer Gαiβγ: identification of key CB1 contacts with the C-terminal helix α5 of Gαi.Rendomab B4, a monoclonal antibody that discriminates the human endothelin B receptor of melanoma cells and inhibits their migration.Structure-activity relationship study of indole-2-carboxamides identifies a potent allosteric modulator for the cannabinoid receptor 1 (CB1).Allosteric modulation of a cannabinoid G protein-coupled receptor: binding site elucidation and relationship to G protein signaling.Cannabinoids in pain management: CB1, CB2 and non-classic receptor ligands.
P2860
Q26744211-815CC933-06EB-435A-877F-990644A92566Q26829111-C8614449-6090-4F31-8EDE-6DEAA6761451Q26864384-93DAF3DE-F294-495C-BD3E-E1C639865D34Q27026491-9B58B69F-ABB6-4AC4-845C-2E2C1F1DDA98Q27308091-3E22B1E4-1F4B-4E4B-8568-170C71F309AEQ28245037-148E64D3-BC35-4E33-8E1F-90976E53017FQ30385837-FCAC6225-293D-4A4D-8AA7-DB33F9EB7E79Q30427185-6844BD41-BA82-415D-861C-092A938ED876Q30842363-2C91ADE2-CDCF-473C-B58B-FB0E6C78C2BDQ33703103-C2FE3C90-DE38-4F64-8A85-857D17793853Q33833528-9A2FA6DA-E660-4279-84A3-AC5D496A4F46Q34167669-F5BA88CB-ABC6-41CA-9C58-4E9F2B607437Q34243225-C0D62129-8186-4C43-B38A-2821533009FEQ34292608-055FE38F-39CD-4043-99D6-CA498C9B509FQ34372488-109C95B6-E15B-4409-BB93-57F066EB9F70Q34399823-FFFF889F-1A1A-4E81-AFD1-A00358C6729BQ34465562-5C113335-F6C7-4184-AEB8-5E5C45B5788DQ34500324-FCDA7BC9-A932-4BCB-8740-83B4A42C5136Q34545629-2FDBF45D-9B79-4641-9043-C68FCBC52D91Q34793269-984D115C-86E4-489B-A1D2-90B8AD2F3F6AQ34946743-D239114B-D391-4CF2-A8C6-57704252A7A7Q35845768-80B62CAF-C032-4B59-94B2-A01D4A31FC47Q35967903-A04C8833-E079-414C-ABBA-F376EB467330Q35990953-2F7AA8D3-1576-47D7-8815-231D83D1DBDEQ36071373-5AF8263B-C87B-4284-BC46-D659426FC27EQ36234465-29A38C0D-B5DA-4A75-BBCD-EAFBBA2042E4Q36417706-19895470-1031-437A-85AC-972615FF6B1FQ36485064-6F9BA8D4-E636-4EDA-9FD2-0D6EB493A942Q36573169-275731C2-8877-4AB0-A1D2-EE77EAF8CC35Q36593142-729172AF-6E20-4FA1-AD09-585A6C7F0688Q36625465-2064D3D0-275C-4C1A-9565-F3C4F25EB017Q36742217-3E8C6943-2C70-4616-9001-FF36BDACBF7AQ36890833-A2B98BBF-77A7-4EB1-9DF4-F1EE3096E89AQ37183072-F8A33C97-CE20-448B-90CD-685D11D112E3Q37237174-6817F244-EC3F-44DB-8DD0-0058A3E0F1CFQ37289241-198FE657-8B55-456B-8159-2593954822D2Q37327310-3FAFBA56-1F22-4CDF-B232-D2D9871793E7Q37432662-19515DE1-3118-4878-A988-48001553B4ABQ37608491-E1DB0FD6-EEBD-440D-876F-853F25E70B80Q38212376-E1B0529A-58B3-4774-B7E2-12DD7E6DB36D
P2860
Allosteric modulator ORG27569 induces CB1 cannabinoid receptor high affinity agonist binding state, receptor internalization, and Gi protein-independent ERK1/2 kinase activation
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 modulator ORG27569 ...... ndent ERK1/2 kinase activation
@ast
Allosteric modulator ORG27569 ...... ndent ERK1/2 kinase activation
@en
type
label
Allosteric modulator ORG27569 ...... ndent ERK1/2 kinase activation
@ast
Allosteric modulator ORG27569 ...... ndent ERK1/2 kinase activation
@en
prefLabel
Allosteric modulator ORG27569 ...... ndent ERK1/2 kinase activation
@ast
Allosteric modulator ORG27569 ...... ndent ERK1/2 kinase activation
@en
P2860
P921
P356
P1476
Allosteric modulator ORG27569 ...... ndent ERK1/2 kinase activation
@en
P2093
Debra A Kendall
Kwang H Ahn
P2860
P304
12070-12082
P356
10.1074/JBC.M111.316463
P407
P577
2012-02-16T00:00:00Z