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Maraviroc (UK-427,857), a Potent, Orally Bioavailable, and Selective Small-Molecule Inhibitor of Chemokine Receptor CCR5 with Broad-Spectrum Anti-Human Immunodeficiency Virus Type 1 Activity

Data up to Jan 2025

Published2005
Citations1,109
References53

Total Citations Per Year

Abstract

References (53)

HIV-1 entry into CD4+ cells is mediated by the chemokine receptor CC-CKR-5

1996 • 3,189 citations

Homozygous Defect in HIV-1 Coreceptor Accounts for Resistance of Some Multiply-Exposed Individuals to HIV-1 Infection

1996 • 3,106 citations

Identification of RANTES, MIP-1α, and MIP-1β as the Major HIV-Suppressive Factors Produced by CD8 + T Cells

1995 • 2,890 citations

Resistance to HIV-1 infection in Caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene

1996 • 2,883 citations

Genetic Restriction of HIV-1 Infection and Progression to AIDS by a Deletion Allele of the CKR5 Structural Gene

1996 • 2,502 citations

CHEMOKINE RECEPTORS AS HIV-1 CORECEPTORS: Roles in Viral Entry, Tropism, and Disease

1999 • 2,174 citations

Rapid evolution of the neutralizing antibody response to HIV type 1 infection

2003 • 1,192 citations

Antiretroviral-Drug Resistance among Patients Recently Infected with HIV

2002 • 1,150 citations

Interferon–inducible T Cell Alpha Chemoattractant (I-TAC): A Novel Non-ELR CXC Chemokine with Potent Activity on Activated T Cells through Selective High Affinity Binding to CXCR3

1998 • 857 citations

A three-dimensional model to analyze drug-drug interactions

1990 • 535 citations

Aminooxypentane-RANTES Induces CCR5 Internalization but Inhibits Recycling: A Novel Inhibitory Mechanism of HIV Infectivity

1998 • 409 citations

Transmission of antiretroviral-drug-resistant HIV-1 variants

1999 • 401 citations

MHC class II tetramers identify peptide-specific human CD4+ T cells proliferating in response to influenza A antigen

1999 • 379 citations

A small molecule HIV-1 inhibitor that targets the HIV-1 envelope and inhibits CD4 receptor binding

2003 • 354 citations

SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infectionin vitroandin vivo

2001 • 307 citations

HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use

2002 • 305 citations

Cloning and functional expression of CC CKR5, a human monocyte CC chemokine receptor selective for MIP-1α, MIP-1β, and RANTES

1996 • 301 citations

The CCR5 Receptor-Based Mechanism of Action of 873140, a Potent Allosteric Noncompetitive HIV Entry Inhibitor

2005 • 297 citations

The effect of genetic variation in chemokines and their receptorson HIV transmission and progression to AIDS

2000 • 256 citations

Impaired Macrophage Function and Enhanced T Cell-Dependent Immune Response in Mice Lacking CCR5, the Mouse Homologue of the Major HIV-1 Coreceptor

1998 • 252 citations

Acute HIV infection: impact on the spread of HIV and transmission of drug resistance

2001 • 238 citations

Spirodiketopiperazine-Based CCR5 Inhibitor Which Preserves CC-Chemokine/CCR5 Interactions and Exerts Potent Activity against R5 Human Immunodeficiency Virus Type 1 In Vitro

2004 • 221 citations

Travel and the spread of HIV-1 genetic variants

2003 • 194 citations

Highly Potent RANTES Analogues either Prevent CCR5-Using Human Immunodeficiency Virus Type 1 Infection In Vivo or Rapidly Select for CXCR4-Using Variants

1999 • 185 citations

Sensitivity of Human Immunodeficiency Virus Type 1 to Fusion Inhibitors Targeted to the gp41 First Heptad Repeat Involves Distinct Regions of gp41 and Is Consistently Modulated by gp120 Interactions with the Coreceptor

2001 • 180 citations

Adherence to HAART among patients with HIV: Breakthroughs and barriers

2002 • 168 citations

Biochemical and Genetic Characterizations of a Novel Human Immunodeficiency Virus Type 1 Inhibitor That Blocks gp120-CD4 Interactions

2003 • 166 citations

Use of Inhibitors To Evaluate Coreceptor Usage by Simian and Simian/Human Immunodeficiency Viruses and Human Immunodeficiency Virus Type 2 in Primary Cells

2000 • 160 citations

Blockade of Human Cardiac Potassium Channel Human Ether-a-go-go-Related Gene (HERG) by Macrolide Antibiotics

2002 • 149 citations

Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. IV. Discovery of 1-[(4,6-Dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-{2-methoxy-1(R)-4-(trifluoromethyl)phenyl}ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a Potent, Highly Selective, and Orally Bioavailable CCR5 Antagonist

2004 • 139 citations

Novel Low Molecular Weight Spirodiketopiperazine Derivatives Potently Inhibit R5 HIV-1 Infection through Their Antagonistic Effects on CCR5

2001 • 130 citations

Natural Variation of Drug Susceptibility in Wild-Type Human Immunodeficiency Virus Type 1

2004 • 110 citations

Human Immunodeficiency Virus Type 1 Protease Genotypes and In Vitro Protease Inhibitor Susceptibilities of Isolates from Individuals Who Were Switched to Other Protease Inhibitors after Long-Term Saquinavir Treatment

1998 • 103 citations

Small-Molecule Antagonists of CCR5 and CXCR4: A Promising New Class of Anti-HIV-1 Drugs

2004 • 77 citations

Structure Modeling of the Chemokine Receptor CCR5: Implications for Ligand Binding and Selectivity

2002 • 74 citations

Identification of C-C Chemokine Receptor 1 (CCR1) as the Monocyte Hemofiltrate C-C Chemokine (HCC)-1 Receptor

1998 • 62 citations

Non-peptidic Chemokine Receptors Antagonists as Emerging Anti-HIV Agents

2002 • 54 citations

Subtype-specific stimulation of []GTPγS binding by recombinant α2-adrenoceptors

1998 • 53 citations

Pharmacological characterization of the chemokine receptor, CCR5

2002 • 52 citations

Depletion of CCR5-Expressing Cells with Bispecific Antibodies and Chemokine Toxins: A New Strategy in the Treatment of Chronic Inflammatory Diseases and HIV

2001 • 47 citations

Enfuvirtide

2002 • 39 citations

Development and Automation of a 384-Well Cell Fusion Assay to Identify Inhibitors of CCR5/CD4-Mediated HIV Virus Entry

2004 • 38 citations

Is Resistance Futile?

2003 • 31 citations

CCR5 antagonists for the treatment of HIV.

2004 • 30 citations

Inhibitors of the entry of HIV into host cells.

2003 • 26 citations

Pharmacokinetics and Short-Term Safety of 873140, a Novel CCR5 Antagonist, in Healthy Adult Subjects

2005 • 25 citations

α2-Adrenoceptor agonists stimulate high-affinity GTPase activity in a receptor subtype-selective manner

1999 • 24 citations

CCR5 Chemokine Receptors: Gatekeepers of HIV-1 Infection

2002 • 22 citations

The effects of the 32-bp CCR-5 deletion on HIV transmission and HIV disease progression in individuals with haemophilia

2000 • 19 citations

Causal Pathways for CCR5 Genotype and HIV Progression

2000 • 18 citations

The Emerging Role of Fusion Inhibitors in HIV Infection

1999 • 12 citations

Susceptibility of diverse primary HIV isolates with varying co‐receptor specificity's to CXCR4 antagonistic compounds

2002 • 8 citations

The effect of a synthetic 7‐thiaprostaglandin E1 derivative, TEI‐6122, on monocyte chemoattractant protein‐1 induced chemotaxis in THP‐1 cells

1995 • 6 citations

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Maraviroc (UK-427,857), a Potent, Orally Bioavailable, and Selective Small-Molecule… (2005) – Antimicrobial Agents and Chemotherapy | Metascience Observatory Explorer