Advances of CCR5 antagonists: From small molecules to macromolecules

PRO 140 Monoclonal Antibody to CCR5 Prevents Acute Xenogeneic Graft-versus-Host Disease in NOD- scid IL-2Ry null Mice

(2018) Denis R. Burger et al.   BIOLOGY OF BLOOD AND MARROW TRANSPLANTATION

The CCL5/CCR5 Axis Promotes Vascular Smooth Muscle Cell Proliferation and Atherogenic Phenotype Switching

(2018) Chin-Sheng Lin et al.   CELLULAR PHYSIOLOGY AND BIOCHEMISTRY

Gene Polymorphisms in the CCL5/CCR5 Pathway as a Genetic Biomarker for Outcome and Hand–Foot Skin Reaction in Metastatic Colorectal Cancer Patients Treated With Regorafenib

(2018) Mitsukuni Suenaga et al.   Clinical Colorectal Cancer

A CCR5 antagonist-based HIV entry inhibitor exhibited potent spermicidal activity: Potential application for contraception and prevention of HIV sexual transmission

(2018) Mingjun Yang et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Therapeutic inhibition of inflammatory monocyte recruitment reduces steatohepatitis and liver fibrosis

(2018) Oliver Krenkel et al.   HEPATOLOGY

CCR5Δ32 – A piece of protection in the inflammatory puzzle of multiple sclerosis susceptibility

(2018) Lian Lopes Troncoso et al.   HUMAN IMMUNOLOGY

Inhibition of the CCL5/CCR5 Axis against the Progression of Gastric Cancer

(2018) Donatella Aldinucci et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Do CCR5 antagonists improve the overall survival of patients with AIDS-related progressive multifocal leucoencephalopathy?

(2018) Edouard Januel et al.   JOURNAL OF NEUROLOGY NEUROSURGERY AND PSYCHIATRY

Clinicopathological significance of chemokine receptor (CCR1, CCR3, CCR4, CCR5, CCR7 and CXCR4) expression in head and neck squamous cell carcinomas

(2018) Wilfredo A. González-Arriagada et al.   JOURNAL OF ORAL PATHOLOGY & MEDICINE

Marginal Effects of Systemic CCR5 Blockade with Maraviroc on Oral Simian Immunodeficiency Virus Transmission to Infant Macaques

(2018) Egidio Brocca-Cofano et al.   JOURNAL OF VIROLOGY

The dual CCR2/CCR5 chemokine receptor antagonist Cenicriviroc reduces macrophage infiltration and disease severity in Duchenne muscular dystrophy (Dmdmdx-4Cv) mice

(2018) Feng Liang et al.   PLoS One

The return of PRO 140, a CCR5-directed mAb

(2018) Melanie A. Thompson   Current Opinion in HIV and AIDS

CCR5/CCL5 axis interaction promotes migratory and invasiveness of pancreatic cancer cells

(2018) Santosh Kumar Singh et al.   Scientific Reports

Addition of maraviroc to antiretroviral therapy decreased interferon-γ mRNA in the CD4+ T cells of patients with suboptimal CD4+ T-cell recovery

(2017) Rumi Minami et al.   JOURNAL OF INFECTION AND CHEMOTHERAPY

Individual and combined effect of TP53, MDM2, MDM4, MTHFR, CCR5, and CASP8 gene polymorphisms in lung cancer

(2017) Ausra Stumbryte et al.   Oncotarget

Maraviroc-intensified combined antiretroviral therapy improves cognition in virally suppressed HIV-associated neurocognitive disorder

(2016) Thomas M. Gates et al.   AIDS

A 48-week randomized phase 2b study evaluating cenicriviroc versus efavirenz in treatment-naive HIV-infected adults with C-C chemokine receptor type 5-tropic virus

(2016) Melanie Thompson et al.   AIDS

A Pharmacokinetic and Pharmacodynamic Study of Maraviroc as Acute Graft-versus-Host Disease Prophylaxis in Pediatric Allogeneic Stem Cell Transplant Recipients with Nonmalignant Diagnoses

(2016) Pooja Khandelwal et al.   BIOLOGY OF BLOOD AND MARROW TRANSPLANTATION

Tumoral Immune Cell Exploitation in Colorectal Cancer Metastases Can Be Targeted Effectively by Anti-CCR5 Therapy in Cancer Patients

(2016) Niels Halama et al.   CANCER CELL

Efficacy and safety study of cenicriviroc for the treatment of non-alcoholic steatohepatitis in adult subjects with liver fibrosis: CENTAUR Phase 2b study design

(2016) Scott Friedman et al.   Contemporary Clinical Trials

Pharmacokinetics, Safety, and CCR2/CCR5 Antagonist Activity of Cenicriviroc in Participants With Mild or Moderate Hepatic Impairment

(2016) E Lefebvre et al.   CTS-Clinical and Translational Science

Chemokine (C-C motif) receptor 2-positive monocytes aggravate the early phase of acetaminophen-induced acute liver injury

(2016) Jana C. Mossanen et al.   HEPATOLOGY

Targeting tumour-associated macrophages with CCR2 inhibition in combination with FOLFIRINOX in patients with borderline resectable and locally advanced pancreatic cancer: a single-centre, open-label, dose-finding, non-randomised, phase 1b trial

(2016) Timothy M Nywening et al.   LANCET ONCOLOGY

Temporary CXCR3 and CCR5 Antagonism Following Vaccination Enhances Memory CD8 T Cell Immune Responses

(2016) Rui Li et al.   MOLECULAR MEDICINE

Beneficial properties of maraviroc on neuropathic pain development and opioid effectiveness in rats

(2016) Klaudia Kwiatkowski et al.   PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY

Maraviroc Reduces Arterial Stiffness in PI-Treated HIV-infected Patients

(2016) Stefania Piconi et al.   Scientific Reports

Maraviroc decreases CCL8-mediated migration of CCR5+ regulatory T cells and reduces metastatic tumor growth in the lungs

(2016) E. C. Halvorsen et al.   OncoImmunology

Antifibrotic Effects of the Dual CCR2/CCR5 Antagonist Cenicriviroc in Animal Models of Liver and Kidney Fibrosis

(2016) Eric Lefebvre et al.   PLoS One

Maraviroc Clinical Test (MCT) as an alternative tool to decide CCR5-antagonists prescription in naïve HIV-infected patients

(2015) Miguel Genebat et al.   ANTIVIRAL RESEARCH

Pathobiology of liver fibrosis: a translational success story

(2015) Youngmin A Lee et al.   GUT

Specificity for a CCR5 Inhibitor Is Conferred by a Single Amino Acid Residue

(2015) Gloria Lau et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

P0906 : Inhibition of HCV replication by CCR5 blockade with cenicriviroc and maraviroc

(2015) K.E. Sherman et al.   JOURNAL OF HEPATOLOGY

P0146 : Oral, once-daily, cenicriviroc leads to rapid and potent CCR2 and CCR5 blockade in subjects with advanced liver disease, similar to effects seen in healthy volunteers and HIV-1 infected subjects

(2015) N.S. Utay et al.   JOURNAL OF HEPATOLOGY

Inhibition of Inflammatory and Neuropathic Pain by Targeting a Mu Opioid Receptor/Chemokine Receptor5 Heteromer (MOR-CCR5)

(2015) Eyup Akgün et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cenicriviroc, a Novel CCR5 (R5) and CCR2 Antagonist, Shows In Vitro Activity against R5 Tropic HIV-2 Clinical Isolates

(2015) Benoit Visseaux et al.   PLoS One

Roles for Chemokines in Liver Disease

(2014) Fabio Marra et al.   GASTROENTEROLOGY

Treatment intensification with maraviroc (CCR5 antagonist) leads to declines in CD16-expressing monocytes in cART-suppressed chronic HIV-infected subjects and is associated with improvements in neurocognitive test performance: implications for HIV-associated neurocognitive disease (HAND)

(2014) Lishomwa C. Ndhlovu et al.   JOURNAL OF NEUROVIROLOGY

HIV-1 induces cytoskeletal alterations and Rac1 activation during monocyte-blood–brain barrier interactions: modulatory role of CCR5

(2014) Shawna M Woollard et al.   Retrovirology

Effect of the CCR5 antagonist maraviroc on the occurrence of immune reconstitution inflammatory syndrome in HIV (CADIRIS): a double-blind, randomised, placebo-controlled trial

(2014) Juan G Sierra-Madero et al.   Lancet HIV

Maraviroc, a CCR5 Antagonist, Prevents Development of Hepatocellular Carcinoma in a Mouse Model

(2013) Laura Ochoa-Callejero et al.   PLoS One

A possible role for CCR5 in the progression of atherosclerosis in HIV-infected patients: a cross-sectional study

(2013) Laura Fernández-Sender et al.   AIDS Research and Therapy

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 potential role of anibamine, a natural product CCR5 antagonist, and its analogues as leads toward development of anti-ovarian cancer agents

(2012) Yan Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

CCR5 Antagonist Blocks Metastasis of Basal Breast Cancer Cells

(2012) M. Velasco-Velazquez et al.   CANCER RESEARCH

The Role of Chemokines in Acute Liver Injury

(2012) Yedidya Saiman et al.   Frontiers in Physiology

Pharmacokinetics and Pharmacodynamics of TBR-652, a Novel CCR5 Antagonist, in HIV-1-Infected, Antiretroviral Treatment-Experienced, CCR5 Antagonist-Naïve Patients

(2011) Jean-Francois Marier et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Safety, Efficacy, and Pharmacokinetics of TBR-652, a CCR5/CCR2 Antagonist, in HIV-1–Infected, Treatment-Experienced, CCR5 Antagonist–Naive Subjects

(2011) Jacob Lalezari et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

Allosteric Model of Maraviroc Binding to CC Chemokine Receptor 5 (CCR5)

(2011) Javier Garcia-Perez et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

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

CCR2 promotes hepatic fibrosis in mice

(2009) Ekihiro Seki et al.   HEPATOLOGY

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

In Vitro and Clinical Investigation of the Relationship Between CCR5 Receptor Occupancy and Anti-HIV Activity of Aplaviroc

(2008) James F. Demarest et al.   JOURNAL OF CLINICAL PHARMACOLOGY

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

Targeting Chemokine Receptors in HIV: A Status Report

(2007) Shawn E. Kuhmann et al.   Annual Review of Pharmacology and Toxicology