CCR5 receptor antagonists in preclinical to phase II clinical development for treatment of HIV

CCR5 blockade for neuroinflammatory diseases — beyond control of HIV

(2016) Guillaume Martin-Blondel et al.   Nature Reviews Neurology

Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists

(2015) Suwen Hu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Pyrazolo-Piperidines Exhibit Dual Inhibition of CCR5/CXCR4 HIV Entry and Reverse Transcriptase

(2015) Bryan D. Cox et al.   ACS Medicinal Chemistry Letters

Chemokines and Chemokine Receptors: Positioning Cells for Host Defense and Immunity

(2014) Jason W. Griffith et al.   Annual Review of Immunology

Shift of HIV Tropism in Stem-Cell Transplantation with CCR5 Delta32 Mutation

(2014) Lambros Kordelas et al.   NEW ENGLAND JOURNAL OF MEDICINE

Intensification of a raltegravir-based regimen with maraviroc in early HIV-1 infection

(2013) Maria C. Puertas et al.   AIDS

Virological and Immunological Response to Antiretroviral Regimens Containing Maraviroc in HIV Type 1-Infected Patients in Clinical Practice: Role of Different Tropism Testing Results and of Concomitant Treatments

(2013) Barbara Rossetti et al.   AIDS RESEARCH AND HUMAN RETROVIRUSES

Does Total Body Irradiation Conditioning Improve Outcomes of Myeloablative Human Leukocyte Antigen–Identical Sibling Transplantations for Chronic Lymphocytic Leukemia?

(2013) Mitchell Sabloff et al.   BIOLOGY OF BLOOD AND MARROW TRANSPLANTATION

Design, synthesis, and biological evaluation of novel piperidine-4-carboxamide derivatives as potent CCR5 inhibitors

(2013) Suwen Hu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Lack of Prophylactic Efficacy of Oral Maraviroc in Macaques despite High Drug Concentrations in Rectal Tissues

(2013) I. Massud et al.   JOURNAL OF VIROLOGY

Design, Synthesis and Biological Evaluation of Novel Piperazine Derivatives as CCR5 Antagonists

(2013) Tao Liu et al.   PLoS One

Primary CD8+ T cells from elite suppressors effectively eliminate non-productively HIV-1 infected resting and activated CD4+ T cells

(2013) Robert W Buckheit et al.   Retrovirology

A common mechanism of clinical HIV-1 resistance to the CCR5 antagonist maraviroc despite divergent resistance levels and lack of common gp120 resistance mutations

(2013) Michael Roche et al.   Retrovirology

Preparation and Activities of Macromolecule Conjugates of the CCR5 Antagonist Maraviroc

(2013) Shigehiro Asano et al.   ACS Medicinal Chemistry Letters

HIV-1 entry inhibitors: recent development and clinical use

(2013) Timothy J Henrich et al.   Current Opinion in Virology

Design, synthesis, and biological activity of novel 1,4-disubstituted piperidine/piperazine derivatives as CCR5 antagonist-based HIV-1 entry inhibitors

(2012) Ming-xin Dong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The MOTIVATE trials: maraviroc therapy in antiretroviral treatment-experienced HIV-1-infected patients

(2012) Steven FL van Lelyveld et al.   Expert Review of Anti-Infective Therapy

In vitro effects of the CCR5 inhibitor maraviroc on human T cell function

(2012) H. Arberas et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

CCR5 Antagonist TD-0680 Uses a Novel Mechanism for Enhanced Potency against HIV-1 Entry, Cell-mediated Infection, and a Resistant Variant

(2012) Yuanxi Kang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Chemokine Receptor Antagonists

(2012) James Pease et al.   JOURNAL OF MEDICINAL CHEMISTRY

HIV-1 Resistance to Maraviroc Conferred by a CD4 Binding Site Mutation in the Envelope Glycoprotein gp120

(2012) A. N. Ratcliff et al.   JOURNAL OF VIROLOGY

Blockade of Lymphocyte Chemotaxis in Visceral Graft-versus-Host Disease

(2012) Ran Reshef et al.   NEW ENGLAND JOURNAL OF MEDICINE

The Chemokine Receptor CCR5, a Therapeutic Target for HIV/AIDS Antagonists, Is Critical for Recovery in a Mouse Model of Japanese Encephalitis

(2012) Maximilian Larena et al.   PLoS One

Effects of sequence changes in the HIV-1 gp41 fusion peptide on CCR5 inhibitor resistance

(2012) Cleo G. Anastassopoulou et al.   VIROLOGY

Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication

(2011) Renato Skerlj et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist

(2011) Changsheng Zheng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and evaluation of 2-phenyl-1,4-butanediamine-based CCR5 antagonists for the treatment of HIV-1

(2011) Matthew D. Tallant et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and synthesis of pyridin-2-yloxymethylpiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication

(2011) Renato Skerlj et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of a novel series of cyclic urea as potent CCR5 antagonists

(2011) Maosheng Duan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of novel pyridyl carboxamides as potent CCR5 antagonists and optimization of their pharmacokinetic profile in rats

(2011) Maosheng Duan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

In vitro effect of anti-human immunodeficiency virus CCR5 antagonist maraviroc on chemotactic activity of monocytes, macrophages and dendritic cells

(2011) R. Rossi et al.   CLINICAL AND EXPERIMENTAL IMMUNOLOGY

Clinical Utility of Maraviroc

(2011) Jorge Parra et al.   CLINICAL DRUG INVESTIGATION

Highlights from the 50th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC)

(2011) P. Cole et al.   DRUGS OF THE FUTURE

CXCR4 and CCR5 ligands cooperate in monocyte and lymphocyte migration and in inhibition of dual-tropic (R5/X4) HIV-1 infection

(2011) Mieke Gouwy et al.   EUROPEAN JOURNAL OF IMMUNOLOGY

Chemokine control of West Nile virus infection

(2011) Jean K. Lim et al.   EXPERIMENTAL CELL RESEARCH

Maraviroc Can Improve Lipid Profiles in Dyslipidemic Patients with HIV: Results from the MERIT Trial

(2011) A. MacInnes et al.   HIV CLINICAL TRIALS

Inflammatory chemokine receptors regulate CD8+T cell contraction and memory generation following infection

(2011) Jacob E. Kohlmeier et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Novel 4,4-Disubstituted Piperidine-Based C–C Chemokine Receptor-5 Inhibitors with High Potency against Human Immunodeficiency Virus-1 and an Improved human Ether-a-go-go Related Gene (hERG) Profile

(2011) Wieslaw M. Kazmierski et al.   JOURNAL OF MEDICINAL CHEMISTRY

Prospective CCR5 Small Molecule Antagonist Compound Design Using a Combined Mutagenesis/Modeling Approach

(2011) Markus Metz et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

HIV-1 predisposed to acquiring resistance to maraviroc (MVC) and other CCR5 antagonists in vitro has an inherent, low-level ability to utilize MVC-bound CCR5 for entry

(2011) Michael Roche et al.   Retrovirology

HIV coreceptor tropism in antiretroviral treatment-naive patients newly diagnosed at a late stage of HIV infection

(2010) Benedikt Simon et al.   AIDS

HIV Type 1 from a Patient with Baseline Resistance to CCR5 Antagonists Uses Drug-Bound Receptor for Entry

(2010) John C. Tilton et al.   AIDS RESEARCH AND HUMAN RETROVIRUSES

Studies on the structure–activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents

(2010) Ben Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of N-benzyl-N′-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): Modification of the acyl portion

(2010) Maosheng Duan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series

(2010) Jutta Wanner et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists

(2010) Rémy C. Lemoine et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Evaluation of a 3-amino-8-azabicyclo[3.2.1]octane replacement in the CCR5 antagonist maraviroc

(2010) Rémy C. Lemoine et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists

(2010) David M. Rotstein et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Exploration of a new series of CCR5 antagonists: Multi-dimensional optimization of a sub-series containing N-substituted pyrazoles

(2010) Rémy C. Lemoine et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of N-benzyl-N′-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (I): Optimization of the amine portion

(2010) Maosheng Duan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of novel (S)-α-phenyl-γ-amino butanamide containing CCR5 antagonists via functionality inversion approach

(2010) Hu-Shan Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Evidence for the cure of HIV infection by CCR5 32/ 32 stem cell transplantation

(2010) K. Allers et al.   BLOOD

Efficient synthesis and identification of novel propane-1,3-diamino bridged CCR5 antagonists with variation on the basic center carrier

(2010) Xing Fan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Efficacy and Safety of Maraviroc Versus Efavirenz, Both With Zidovudine/Lamivudine: 96-Week Results From the MERIT Study

(2010) Juan Sierra-Madero et al.   HIV CLINICAL TRIALS

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

A Maraviroc-Resistant HIV-1 with Narrow Cross-Resistance to Other CCR5 Antagonists Depends on both N-Terminal and Extracellular Loop Domains of Drug-Bound CCR5

(2010) John C. Tilton et al.   JOURNAL OF VIROLOGY

HIV-1 Resistance to CCR5 Antagonists Associated with Highly Efficient Use of CCR5 and Altered Tropism on Primary CD4+ T Cells

(2010) J. M. Pfaff et al.   JOURNAL OF VIROLOGY

CC and CXC chemokines are pivotal mediators of cerebral injury in ischaemic stroke

(2010) Giorgio Luciano Viviani et al.   THROMBOSIS AND HAEMOSTASIS

Clinical resistance to vicriviroc through adaptive V3 loop mutations in HIV-1 subtype D gp120 that alter interactions with the N-terminus and ECL2 of CCR5

(2010) Robert A. Ogert et al.   VIROLOGY

Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity

(2010) Chu-Biao Xue et al.   ACS Medicinal Chemistry Letters

HIV-1 coreceptor usage and CXCR4-specific viral load predict clinical disease progression during combination antiretroviral therapy

(2009) Barbara Weiser et al.   AIDS

[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring

(2009) Maosheng Duan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

1-Amido-1-phenyl-3-piperidinylbutanes — CCR5 antagonists for the treatment of HIV. Part 1

(2009) Christopher G. Barber et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

1-Amido-1-phenyl-3-piperidinylbutanes – CCR5 antagonists for the treatment of HIV: Part 2

(2009) Christopher G. Barber et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

4,4-Disubstituted cyclohexylamine based CCR5 chemokine receptor antagonists as anti-HIV-1 agents

(2009) Maosheng Duan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The design and discovery of novel amide CCR5 antagonists

(2009) David C. Pryde et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles

(2009) Rémy C. Lemoine et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The chemokine receptor antagonist, TAK-779, decreased experimental autoimmune encephalomyelitis by reducing inflammatory cell migration into the central nervous system, without affecting T cell function

(2009) Jia Ni et al.   BRITISH JOURNAL OF PHARMACOLOGY

Twenty-Six Years of Anti-HIV Drug Discovery: Where Do We Stand and Where Do We Go?

(2009) Youcef Mehellou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Long-Term Control of HIV byCCR5Delta32/Delta32 Stem-Cell Transplantation

(2009) Gero Hütter et al.   NEW ENGLAND JOURNAL OF MEDICINE

Resistance to CCR5 inhibitors caused by sequence changes in the fusion peptide of HIV-1 gp41

(2009) C. G. Anastassopoulou et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Reduced cardiac side-effect potential by introduction of polar groups: Discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo

(2008) Gebhard Thoma et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of a potent, selective and orally bioavailable 3,9-diazaspiro[5.5]undeca-2-one CCR5 antagonist

(2008) Hanbiao Yang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Maraviroc: A CCR5-receptor antagonist for the treatment of HIV-1 infection

(2008) Sharon S. Lieberman-Blum et al.   CLINICAL THERAPEUTICS

The Chemokine Receptor CCR5 Plays a Key Role in the Early Memory CD8+ T Cell Response to Respiratory Virus Infections

(2008) Jacob E. Kohlmeier et al.   IMMUNITY

HIV and Antiretroviral Therapy: Lipid Abnormalities and Associated Cardiovascular Risk in HIV-Infected Patients

(2008) Donald P Kotler   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

A Deletion in the Chemokine Receptor 5(CCR5)Gene Is Associated with Tickborne Encephalitis

(2008) Elin Kindberg et al.   JOURNAL OF INFECTIOUS DISEASES

Discovery of Bioavailable 4,4-Disubstituted Piperidines as Potent Ligands of the Chemokine Receptor 5 and Inhibitors of the Human Immunodeficiency Virus-1

(2008) Wieslaw M. Kazmierski et al.   JOURNAL OF MEDICINAL CHEMISTRY

In Vivo Emergence of Vicriviroc Resistance in a Human Immunodeficiency Virus Type 1 Subtype C-Infected Subject

(2008) A. M. N. Tsibris et al.   JOURNAL OF VIROLOGY

Discovery of a Novel CCR5 Antagonist Lead Compound Through Fragment Assembly

(2008) Yanqing Liu et al.   MOLECULES

Maraviroc for Previously Treated Patients with R5 HIV-1 Infection

(2008) Roy M. Gulick et al.   NEW ENGLAND JOURNAL OF MEDICINE

Mapping resistance to the CCR5 co-receptor antagonist vicriviroc using heterologous chimeric HIV-1 envelope genes reveals key determinants in the C2-V5 domain of gp120

(2008) Robert A. Ogert et al.   VIROLOGY

Anti-HIV-1 entry optimization of novel imidazopiperidine-tropane CCR5 antagonists

(2007) Justin Ernst et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS