Pharmacological modulation of chemokine receptor function

Effect of CC Chemokine Receptor 2 CCR2 Blockade on Serum C-Reactive Protein in Individuals at Atherosclerotic Risk and With a Single Nucleotide Polymorphism of the Monocyte Chemoattractant Protein-1 Promoter Region

(2011) Jim Gilbert et al.   AMERICAN JOURNAL OF CARDIOLOGY

Guide to Receptors and Channels (GRAC), 5th edition

(2011) SPH Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

Ligand supported homology modeling and docking evaluation of CCR2: docked pose selection by consensus scoring

(2011) Jong-Hoon Kim et al.   JOURNAL OF MOLECULAR MODELING

Status of GPCR Modeling and Docking as Reflected by Community-wide GPCR Dock 2010 Assessment

(2011) Irina Kufareva et al.   STRUCTURE

Phase 2a Study of the CCR5 Monoclonal Antibody PRO 140 Administered Intravenously to HIV-Infected Adults

(2010) J. M. Jacobson et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

A common intracellular allosteric binding site for antagonists of the CXCR2 receptor

(2010) K Salchow et al.   BRITISH JOURNAL OF PHARMACOLOGY

Defucosylated Humanized Anti-CCR4 Monoclonal Antibody KW-0761 as a Novel Immunotherapeutic Agent for Adult T-cell Leukemia/Lymphoma

(2010) T. Ishii et al.   CLINICAL CANCER RESEARCH

Anti-chemokine small molecule drugs: a promising future?

(2010) Amanda EI Proudfoot et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Conserved Water-mediated Hydrogen Bond Network between TM-I, -II, -VI, and -VII in 7TM Receptor Activation

(2010) Rie Nygaard et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Epstein-Barr Virus-encoded G Protein-coupled Receptor BILF1 Hetero-oligomerizes with Human CXCR4, Scavenges GαiProteins, and Constitutively Impairs CXCR4 Functioning

(2010) Saskia Nijmeijer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The cytomegalovirus-encoded chemokine receptor US28 promotes intestinal neoplasia in transgenic mice

(2010) Gerold Bongers et al.   JOURNAL OF CLINICAL INVESTIGATION

Anti–HIV‐1 Activity of Weekly or Biweekly Treatment with Subcutaneous PRO 140, a CCR5 Monoclonal Antibody

(2010) Jeffrey M. Jacobson et al.   JOURNAL OF INFECTIOUS DISEASES

Synthesis and Biological Evaluation of Bivalent Ligands for the Cannabinoid 1 Receptor

(2010) Yanan Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

An Imidazopiperidine Series of CCR5 Antagonists for the Treatment of HIV: The Discovery ofN-{(1S)-1-(3-Fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-232798)

(2010) Paul A. Stupple et al.   JOURNAL OF MEDICINAL CHEMISTRY

Monomeric Rhodopsin Is the Minimal Functional Unit Required for Arrestin Binding

(2010) Hisao Tsukamoto et al.   JOURNAL OF MOLECULAR BIOLOGY

Functional Selectivity and Biased Receptor Signaling

(2010) T. Kenakin   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

G protein coupled receptors as allosteric proteins and the role of allosteric modulators

(2010) Terry Kenakin   JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION

Bivalent Ligands of CXCR4 with Rigid Linkers for Elucidation of the Dimerization State in Cells

(2010) Tomohiro Tanaka et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Therapeutic antibodies directed at G protein-coupled receptors

(2010) Catherine J. Hutchings et al.   mAbs

Different Effects of the Different Natural CC Chemokine Receptor 2b Ligands on  -Arrestin Recruitment, G i Signaling, and Receptor Internalization

(2010) Y. A. Berchiche et al.   MOLECULAR PHARMACOLOGY

Biopharmaceutical benchmarks 2010

(2010) Gary Walsh   NATURE BIOTECHNOLOGY

Development trends for human monoclonal antibody therapeutics

(2010) Aaron L. Nelson et al.   NATURE REVIEWS DRUG DISCOVERY

Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

(2010) T. Kenakin et al.   PHARMACOLOGICAL REVIEWS

Recent advances on the use of the CXCR4 antagonist plerixafor (AMD3100, Mozobil™) and potential of other CXCR4 antagonists as stem cell mobilizers

(2010) Erik De Clercq   PHARMACOLOGY & THERAPEUTICS

Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cells

(2010) B. Tchernychev et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

CXCR4 nanobodies (VHH-based single variable domains) potently inhibit chemotaxis and HIV-1 replication and mobilize stem cells

(2010) S. Jahnichen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Formation and dissociation of M1 muscarinic receptor dimers seen by total internal reflection fluorescence imaging of single molecules

(2010) J. A. Hern et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2010) B. Wu et al.   SCIENCE

Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist

(2010) E. Y. T. Chien et al.   SCIENCE

HCMV-Encoded Chemokine Receptor US28 Mediates Proliferative Signaling Through the IL-6-STAT3 Axis

(2010) E. Slinger et al.   Science Signaling

Multiple interests in structural models of DARC transmembrane protein

(2010) D. Smolarek et al.   TRANSFUSION CLINIQUE ET BIOLOGIQUE

Duffy antigen inhibitors: useful therapeutics for malaria?

(2010) Tracy M. Handel et al.   TRENDS IN PARASITOLOGY

The minor binding pocket: a major player in 7TM receptor activation

(2010) Mette M. Rosenkilde et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

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

(2009) A. Levoye et al.   BLOOD

G protein-coupled receptor hetero-dimerization: contribution to pharmacology and function

(2009) Graeme Milligan   BRITISH JOURNAL OF PHARMACOLOGY

SB265610 is an allosteric, inverse agonist at the human CXCR2 receptor

(2009) ME Bradley et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Human Cytomegalovirus-Encoded Chemokine Receptor US28 Promotes Angiogenesis and Tumor Formation via Cyclooxygenase-2

(2009) D. Maussang et al.   CANCER RESEARCH

The role of dimerisation in the cellular trafficking of G-protein-coupled receptors

(2009) Graeme Milligan   CURRENT OPINION IN PHARMACOLOGY

Dimerization in GPCR mobility and signaling

(2009) Martin J Lohse   CURRENT OPINION IN PHARMACOLOGY

Customizing G Protein-Coupled Receptor Models for Structure-Based Virtual Screening

(2009) Chris de Graaf et al.   CURRENT PHARMACEUTICAL DESIGN

Leukotriene BLT2 Receptor Monomers Activate the Gi2GTP-binding Protein More Efficiently than Dimers

(2009) Laure Arcemisbéhère et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Hetero-oligomerization of CCR2, CCR5, and CXCR4 and the Protean Effects of “Selective” Antagonists

(2009) Denis Sohy et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Purification and Functional Reconstitution of Monomeric μ-Opioid Receptors

(2009) Adam J. Kuszak et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural Basis of the Interaction between Chemokine Stromal Cell-derived Factor-1/CXCL12 and Its G-protein-coupled Receptor CXCR4

(2009) Yutaka Kofuku et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of Novel HIV Entry Inhibitors for the CXCR4 Receptor by Prospective Virtual Screening

(2009) Violeta I. Pérez-Nueno et al.   Journal of Chemical Information and Modeling

Significance of N-Terminal Proteolysis of CCL14a to Activity on the Chemokine Receptors CCR1 and CCR5 and the Human Cytomegalovirus-Encoded Chemokine Receptor US28

(2009) R. Richter et al.   JOURNAL OF IMMUNOLOGY

Increasing Selectivity of CC Chemokine Receptor 8 Antagonists by Engineering Nondesolvation Related Interactions with the Intended and Off-Target Binding Sites

(2009) Igor Shamovsky et al.   JOURNAL OF MEDICINAL CHEMISTRY

Nicotinamide Glycolates Antagonize CXCR2 Activity through an Intracellular Mechanism

(2009) D. Y. Maeda et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Nonpeptidergic Allosteric Antagonists Differentially Bind to the CXCR2 Chemokine Receptor

(2009) P. de Kruijf et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Elucidation of Binding Sites of Dual Antagonists in the Human Chemokine Receptors CCR2 and CCR5

(2009) S. E. Hall et al.   MOLECULAR PHARMACOLOGY

Instability of a Class A G Protein-Coupled Receptor Oligomer Interface

(2009) J. M. Fonseca et al.   MOLECULAR PHARMACOLOGY

AMD3100 Is a CXCR7 Ligand with Allosteric Agonist Properties

(2009) I. Kalatskaya et al.   MOLECULAR PHARMACOLOGY

Analysis of receptor oligomerization by FRAP microscopy

(2009) Sandra Dorsch et al.   NATURE METHODS

Toward the Discovery of Vaccine Adjuvants: Coupling In Silico Screening and In Vitro Analysis of Antagonist Binding to Human and Mouse CCR4 Receptors

(2009) Matthew N. Davies et al.   PLoS One

 -arrestin- but not G protein-mediated signaling by the "decoy" receptor CXCR7

(2009) S. Rajagopal et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective engagement of G protein coupled receptor kinases (GRKs) encodes distinct functions of biased ligands

(2009) D. A. Zidar et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

CCR5 monoclonal antibodies for HIV-1 therapy

(2009) William C Olson et al.   Current Opinion in HIV and AIDS

Is CCR2 the right chemokine receptor to target in rheumatoid arthritis?

(2008) Amanda E. I. Proudfoot   ARTHRITIS AND RHEUMATISM

Modulation of CCR2 in rheumatoid arthritis: A double‐blind, randomized, placebo‐controlled clinical trial

(2008) Clarissa E. Vergunst et al.   ARTHRITIS AND RHEUMATISM

CXCR2 chemokine receptor antagonism enhances DOP opioid receptor function via allosteric regulation of the CXCR2–DOP receptor heterodimer

(2008) Geraldine Parenty et al.   BIOCHEMICAL JOURNAL

Chemokines and cancer: migration, intracellular signalling and intercellular communication in the microenvironment

(2008) Morgan O'Hayre et al.   BIOCHEMICAL JOURNAL

Synthesis and evaluation of cis-3,4-disubstituted piperidines as potent CC chemokine receptor 2 (CCR2) antagonists

(2008) Robert J. Cherney et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Ligand stabilization of CXCR4/δ-opioid receptor heterodimers reveals a mechanism for immune response regulation

(2008) Oscar M. Pello et al.   EUROPEAN JOURNAL OF IMMUNOLOGY

Imaging chemokine receptor dimerization with firefly luciferase complementation

(2008) Kathryn E. Luker et al.   FASEB JOURNAL

PositiveVersusNegative Modulation of Different Endogenous Chemokines for CC-chemokine Receptor 1 by Small Molecule Agonists through AllostericVersusOrthosteric Binding

(2008) Pia C. Jensen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Antiviral Activity of Single‐Dose PRO 140, a CCR5 Monoclonal Antibody, in HIV‐Infected Adults

(2008) Jeffrey M. Jacobson et al.   JOURNAL OF INFECTIOUS DISEASES

Safety, Pharmacokinetics, and Antiviral Activity of HGS004, a Novel Fully Human IgG4 Monoclonal Antibody against CCR5, in HIV‐1–Infected Patients

(2008) Jacob Lalezari et al.   JOURNAL OF INFECTIOUS DISEASES

Orally Bioavailable Isothioureas Block Function of the Chemokine Receptor CXCR4 In Vitro and In Vivo

(2008) Gebhard Thoma et al.   JOURNAL OF MEDICINAL CHEMISTRY

Involvement of the Second Extracellular Loop and Transmembrane Residues of CCR5 in Inhibitor Binding and HIV-1 Fusion: Insights into the Mechanism of Allosteric Inhibition

(2008) Kenji Maeda et al.   JOURNAL OF MOLECULAR BIOLOGY

Noncompetitive Antagonism and Inverse Agonism as Mechanism of Action of Nonpeptidergic Antagonists at Primate and Rodent CXCR3 Chemokine Receptors

(2008) D. Verzijl et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Pharmacological Profile of JNJ-27141491 [(S)-3-[3,4-Difluorophenyl)-propyl]-5-isoxazol-5-yl-2-thioxo-2,3-dihydro-1H-imidazole-4-carboxyl Acid Methyl Ester], as a Noncompetitive and Orally Active Antagonist of the Human Chemokine Receptor CCR2

(2008) M. Buntinx et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Identification of a Putative Intracellular Allosteric Antagonist Binding-Site in the CXC Chemokine Receptors 1 and 2

(2008) D. J. Nicholls et al.   MOLECULAR PHARMACOLOGY

Comparison of the Potential Multiple Binding Modes of Bicyclam, Monocylam, and Noncyclam Small-Molecule CXC Chemokine Receptor 4 Inhibitors

(2008) R. S. Y. Wong et al.   MOLECULAR PHARMACOLOGY

The Relative Activity of "Function Sparing" HIV-1 Entry Inhibitors on Viral Entry and CCR5 Internalization: Is Allosteric Functional Selectivity a Valuable Therapeutic Property?

(2008) V. M. Muniz-Medina et al.   MOLECULAR PHARMACOLOGY

The Duffy Antigen/Receptor for Chemokines Exists in an Oligomeric Form in Living Cells and Functionally Antagonizes CCR5 Signaling through Hetero-Oligomerization

(2008) A. Chakera et al.   MOLECULAR PHARMACOLOGY

Discovery of a Novel CCR5 Antagonist Lead Compound Through Fragment Assembly

(2008) Yanqing Liu et al.   MOLECULES

Structure of a β1-adrenergic G-protein-coupled receptor

(2008) Tony Warne et al.   NATURE

Fluorescence Resonance Energy Transfer Imaging Reveals that Chemokine-Binding Modulates Heterodimers of CXCR4 and CCR5 Receptors

(2008) Nilgun Isik et al.   PLoS One

CXCR4-CCR5: A couple modulating T cell functions

(2008) R. L. Contento et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

In silico identified CCR4 antagonists target regulatory T cells and exert adjuvant activity in vaccination

(2008) J. Bayry et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

(2008) V.-P. Jaakola et al.   SCIENCE

Structural Basis of CXCR4 Sulfotyrosine Recognition by the Chemokine SDF-1/CXCL12

(2008) C. T. Veldkamp et al.   Science Signaling

Chemokines and Their Receptors: Drug Targets in Immunity and Inflammation

(2007) Antonella Viola et al.   Annual Review of Pharmacology and Toxicology

Molecular modeling of the second extracellular loop of G-protein coupled receptors and its implication on structure-based virtual screening

(2007) Chris de Graaf et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS