Partial Agonist and Biased Signaling Properties of the Synthetic Enantiomers J113863/UCB35625 at Chemokine Receptors CCR2 and CCR5.

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Partial Agonist and Biased Signaling Properties of the Synthetic Enantiomers J113863/UCB35625 at Chemokine Receptors CCR2 and CCR5. is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1074/JBC.M116.757559
P932PMC publication ID5241733
P698PubMed publication ID27895119

P50authorCéline GalèsQ73251493
Marc ParmentierQ96095332
Jean-Yves SpringaelQ123124182
P2093author name stringAlexandre Huszagh
Jenny Corbisier
P2860cites workBiased and g protein-independent signaling of chemokine receptorsQ26823970
A small molecule antagonist of chemokine receptors CCR1 and CCR3. Potent inhibition of eosinophil function and CCR3-mediated HIV-1 entry.Q31395542
Small molecule receptor agonists and antagonists of CCR3 provide insight into mechanisms of chemokine receptor activation.Q33291059
Stereospecific pharmacokinetics and pharmacodynamics of beta-adrenergic blockers in humansQ34084671
Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance.Q34134694
A G Protein-Biased Ligand at the μ-Opioid Receptor Is Potently Analgesic with Reduced Gastrointestinal and Respiratory Dysfunction Compared with MorphineQ34321618
The importance of stereoselective determination of drugs in the clinical laboratoryQ35051388
Biased signaling at chemokine receptorsQ35351711
Fulfilling the Promise of "Biased" G Protein-Coupled Receptor Agonism.Q35999789
Therapeutic potential of β-arrestin- and G protein-biased agonists.Q36773331
Beta-blockers alprenolol and carvedilol stimulate beta-arrestin-mediated EGFR transactivation.Q36936400
Biased agonism as a mechanism for differential signaling by chemokine receptors.Q37368610
Chemokines and chemokine receptors: an overview.Q37409994
Distinct conformations of the chemokine receptor CCR4 with implications for its targeting in allergyQ37662609
Internalization of the chemokine receptor CCR4 can be evoked by orthosteric and allosteric receptor antagonistsQ37706598
CXCL11-dependent induction of FOXP3-negative regulatory T cells suppresses autoimmune encephalomyelitis.Q37726647
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Agonist-induced internalization of CC chemokine receptor 5 as a mechanism to inhibit HIV replicationQ39002273
Activation of CCR5 by chemokines involves an aromatic cluster between transmembrane helices 2 and 3.Q39030338
Quantification of ligand bias for clinically relevant β2-adrenergic receptor ligands: implications for drug taxonomy.Q39040325
CCL17/thymus and activation-regulated chemokine induces calcitonin gene–related peptide in human airway epithelial cells through CCR4Q39144493
Aminooxypentane-RANTES induces CCR5 internalization but inhibits recycling: a novel inhibitory mechanism of HIV infectivityQ39200573
Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist.Q39464587
Structural basis for the interaction of CCR5 with a small molecule, functionally selective CCR5 agonistQ40241635
Biased and constitutive signaling in the CC-chemokine receptor CCR5 by manipulating the interface between transmembrane helices 6 and 7.Q40323977
Site-directed mutagenesis of CC chemokine receptor 1 reveals the mechanism of action of UCB 35625, a small molecule chemokine receptor antagonist.Q40467514
Pharmacological blockade of CCR1 ameliorates murine arthritis and alters cytokine networks in vivoQ41603563
Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteersQ42705103
First Clinical Experience with TRV027: Pharmacokinetics and Pharmacodynamics in Healthy VolunteersQ44339339
Highly potent HIV inhibition: engineering a key anti-HIV structure from PSC-RANTES into MIP-1 beta/CCL4.Q47989447
Functional Selectivity and Biased Receptor SignalingQ48656806
The interaction of the enantiomers of carvedilol with alpha 1- and beta 1-adrenoceptorsQ51760841
Evidence for negative binding cooperativity within CCR5-CCR2b heterodimersQ51822453
Operational models of pharmacological agonismQ52699226
Metabolic and pharmacodynamic interactions of enantiomers of propoxyphene and methorphanQ53729191
Pharmacological characteristics of the stereoisomers of carvedilolQ68093321
P433issue2
P407language of work or nameEnglishQ1860
P921main subjectenantiomerQ494483
biasQ742736
P304page(s)575-584
P577publication date2016-11-28
P1433published inJournal of Biological ChemistryQ867727
P1476titlePartial Agonist and Biased Signaling Properties of the Synthetic Enantiomers J113863/UCB35625 at Chemokine Receptors CCR2 and CCR5.
P478volume292

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cites work (P2860)
Q47231111Biased signalling: from simple switches to allosteric microprocessors
Q60046351CCR5 structural plasticity shapes HIV-1 phenotypic properties
Q59791974Cannabinoid Receptor 2 Signalling Bias Elicited by 2,4,6-Trisubstituted 1,3,5-Triazines
Q50130085Correspondence: Reply to 'Compound 17b and formyl peptide receptor biased agonism in relation to cardioprotective effects in ischaemia-reperfusion injury'.
Q57181974Novel peptide nanoparticle-biased antagonist of CCR3 blocks eosinophil recruitment and airway hyperresponsiveness
Q45930874Protein engineering of the chemokine CCL20 prevents psoriasiform dermatitis in an IL-23-dependent murine model.
Q131901489Targeting the CCL2–CCR2 axis for atheroprotection

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