The Chemokine Receptor CCR1 Is Constitutively Active, Which Leads to G Protein-independent, β-Arrestin-mediated Internalization

 -Arrestin-Dependent Activation of the Cofilin Pathway Is Required for the Scavenging Activity of the Atypical Chemokine Receptor D6

(2013) E. M. Borroni et al.   Science Signaling

Development of operational models of receptor activation including constitutive receptor activity and their use to determine the efficacy of the chemokine CCL17 at the CC chemokine receptor CCR4

(2012) RJ Slack et al.   BRITISH JOURNAL OF PHARMACOLOGY

Chemokine receptor oligomerization: A further step toward chemokine function

(2012) Laura Martínez Muñoz et al.   IMMUNOLOGY LETTERS

Review: Structure–function and biological properties of the atypical chemokine receptor D6

(2012) Cinzia Cancellieri et al.   MOLECULAR IMMUNOLOGY

CCR2 Acts as Scavenger for CCL2 during Monocyte Chemotaxis

(2012) Silvia Volpe et al.   PLoS One

Constitutive formation of an RXFP1-signalosome: a novel paradigm in GPCR function and regulation

(2011) Michelle L Halls   BRITISH JOURNAL OF PHARMACOLOGY

Pharmacological modulation of chemokine receptor function

(2011) DJ Scholten et al.   BRITISH JOURNAL OF PHARMACOLOGY

A rapid and efficient way to obtain modified chemokines for functional and biophysical studies

(2011) Samantha J. Allen et al.   CYTOKINE

Mechanisms regulating chemokine receptor activity

(2011) Laura D. Bennett et al.   IMMUNOLOGY

CXCR7/CXCR4 Heterodimer Constitutively Recruits β-Arrestin to Enhance Cell Migration

(2011) Fabien M. Décaillot et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Few Residues within an Extensive Binding Interface Drive Receptor Interaction and Determine the Specificity of Arrestin Proteins

(2011) Sergey A. Vishnivetskiy et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

High Constitutive Activity Is an Intrinsic Feature of Ghrelin Receptor Protein

(2011) Marjorie Damian et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Crystal structure of the β2 adrenergic receptor–Gs protein complex

(2011) Søren G. F. Rasmussen et al.   NATURE

Why CCR2 and CCR5 Blockade Failed and Why CCR1 Blockade Might Still Be Effective in the Treatment of Rheumatoid Arthritis

(2011) Maria C. Lebre et al.   PLoS One

Distinct expression and ligand-binding profiles of two constitutively active GPR17 splice variants

(2010) T Benned-Jensen et al.   BRITISH JOURNAL OF PHARMACOLOGY

KLHL12-mediated ubiquitination of the dopamine D4 receptor does not target the receptor for degradation

(2010) Pieter Rondou et al.   CELLULAR SIGNALLING

CCR1 Antagonists: What Have We Learned From Clinical Trials

(2010) Ronald P. Gladue et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Sub-picomolar relaxin signalling by a pre-assembled RXFP1, AKAP79, AC2, β-arrestin 2, PDE4D3 complex

(2010) Michelle L Halls et al.   EMBO JOURNAL

Deficiency of Chemokine Receptor CCR1 Causes Osteopenia Due to Impaired Functions of Osteoclasts and Osteoblasts

(2010) Akiyoshi Hoshino et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Constitutive and chemokine-dependent internalization and recycling of CXCR7 in breast cancer cells to degrade chemokine ligands

(2010) K E Luker et al.   ONCOGENE

Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists

(2010) B. Wu et al.   SCIENCE

MLN3897 plus methotrexate in patients with rheumatoid arthritis: Safety, efficacy, pharmacokinetics, and pharmacodynamics of an oral CCR1 antagonist in a phase IIa, double-blind, placebo-controlled, randomized, proof-of-concept study

(2009) Clarissa E. Vergunst et al.   ARTHRITIS AND RHEUMATISM

High Constitutive Activity and a G-Protein-Independent High-Affinity State of the Human Histamine H4-Receptor†

(2009) Erich H. Schneider et al.   BIOCHEMISTRY

CXCR7 heterodimerizes with CXCR4 and regulates CXCL12-mediated G protein signaling

(2009) A. Levoye et al.   BLOOD

Resistance of the dopamine D4 receptor to agonist-induced internalization and degradation

(2009) Anneleen Spooren et al.   CELLULAR SIGNALLING

Agonist-Independent Interactions between β-Arrestins and Mutant Vasopressin Type II Receptors Associated with Nephrogenic Syndrome of Inappropriate Antidiuresis

(2009) Martina Kocan et al.   MOLECULAR ENDOCRINOLOGY

The Constitutively Active V2 Receptor Mutants Conferring NSIAD Are Weakly Sensitive to Agonist and Antagonist Regulation

(2009) Julie Tenenbaum et al.   PLoS One

Expression, purification and in vitro functional reconstitution of the chemokine receptor CCR1

(2009) Samantha J. Allen et al.   PROTEIN EXPRESSION AND PURIFICATION

The BRET technology and its application to screening assays

(2008) Johan Bacart et al.   Biotechnology Journal

Scavenging roles of chemokine receptors: chemokine receptor deficiency is associated with increased levels of ligand in circulation and tissues

(2008) A. E. Cardona et al.   BLOOD

Structural Motifs of Importance for the Constitutive Activity of the Orphan 7TM Receptor EBI2: Analysis of Receptor Activation in the Absence of an Agonist

(2008) T. Benned-Jensen et al.   MOLECULAR PHARMACOLOGY

How chemokines invite leukocytes to dance

(2008) Marcus Thelen et al.   NATURE IMMUNOLOGY

Functional reconstitution of the human chemokine receptor CXCR4 with Gi/Go-proteins in Sf9 insect cells

(2008) Patrick Kleemann et al.   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

Constitutive activation of G protein-coupled receptors and diseases: Insights into mechanisms of activation and therapeutics

(2008) Y TAO   PHARMACOLOGY & THERAPEUTICS

Distinct conformational changes in  -arrestin report biased agonism at seven-transmembrane receptors

(2008) A. K. Shukla et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

GPCR monomers and oligomers: it takes all kinds

(2008) Vsevolod V. Gurevich et al.   TRENDS IN NEUROSCIENCES

How and why do GPCRs dimerize?

(2008) Vsevolod V. Gurevich et al.   TRENDS IN PHARMACOLOGICAL SCIENCES