ArticleAntimicrobial agents and chemotherapy2005
Analysis of binding sites for the new small-molecule CCR5 antagonist TAK-220 on human CCR5.
Article in Antimicrobial agents and chemotherapy, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 61 citations in OpenAlex.
- Novel small synthetic HIV-1 V3 crown variants: CCR5 targeting ligands.Journal of biochemistry · 2022Article
- Discovery of HIV entry inhibitors via a hybrid CXCR4 and CCR5 receptor pharmacophore-based virtual screening approach.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2020Article
- CCR5 Governs DNA Damage Repair and Breast Cancer Stem Cell Expansion.Cancer research · 2018Article
- Inhibition of Inflammatory and Neuropathic Pain by Targeting a Mu Opioid Receptor/Chemokine Receptor5 Heteromer (MOR-CCR5).Journal of medicinal chemistry · 2015Article
- Investigation of Inhibition Mechanism of Chemokine Receptor CCR5 by Micro-second Molecular Dynamics Simulations.Scientific reports · 2015Article
- Specificity for a CCR5 Inhibitor Is Conferred by a Single Amino Acid Residue: ROLE OF ILE198.The Journal of biological chemistry · 2015Article
- Targeting CCR5 for anti-HIV research.European journal of clinical microbiology & infectious diseases : official publication of the European Society of Clinical Microbiology · 2014Review
- Identifying chemicals with potential therapy of HIV based on protein-protein and protein-chemical interaction network.PloS one · 2013Article
- Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists.PloS one · 2013Article
- Molecular requirements for inhibition of the chemokine receptor CCR8--probe-dependent allosteric interactions.British journal of pharmacology · 2012Article
- Structural insights from binding poses of CCR2 and CCR5 with clinically important antagonists: a combined in silico study.PloS one · 2012Article
- A V3 loop-dependent gp120 element disrupted by CD4 binding stabilizes the human immunodeficiency virus envelope glycoprotein trimer.Journal of virology · 2010Article
- Structure-function analysis of human immunodeficiency virus type 1 gp120 amino acid mutations associated with resistance to the CCR5 coreceptor antagonist vicriviroc.Journal of virology · 2009Article
- A pièce de resistance: how HIV-1 escapes small molecule CCR5 inhibitors.Current opinion in HIV and AIDS · 2009Review
- 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.Journal of molecular biology · 2008Article
- Isolation and characterization of human immunodeficiency virus type 1 resistant to the small-molecule CCR5 antagonist TAK-652.Antimicrobial agents and chemotherapy · 2007Article
- Status Presens of Antiviral Drugs And Strategies: Part I: DNA Viruses and Retroviruses.Advances in antiviral drug design · 2007Review
- Potent antiviral synergy between monoclonal antibody and small-molecule CCR5 inhibitors of human immunodeficiency virus type 1.Antimicrobial agents and chemotherapy · 2006Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
G protein-coupled receptor CCR5 is the main coreceptor for macrophage-tropic human immunodeficiency virus type 1 (HIV-1), and various small-molecule CCR5 antagonists are being developed to treat HIV-1 infection. It has been reported that such CCR5 antagonists, including TAK-779, bind to a putative binding pocket formed by transmembrane domains (TMs) 1, 2, 3 and 7 of CCR5, indicating the importance of the conformational changes of the TMs during virus entry. In this report, using a single-round infection assay with human CCR5 and its substitution mutants, we demonstrated that a new CCR5 antagonist, TAK-220, shares the putative interacting amino acid residues Asn252 and Leu255 in TM6 with TAK-779 but also requires the distinct residues Gly163 and Ile198 in TMs 4 and 5, respectively, for its inhibitory effect. We suggested that, together with molecular models of the interactions between the drugs and CCR5, the inhibitory activity of TAK-220 could involve direct interactions with amino acid residues in TMs 4, 5, and 6 in addition to those in the previously postulated binding pocket. The possible interaction of drugs with additional regions of the CCR5 molecule would help to develop a new small-molecule CCR5 antagonist.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.