ArticleProceedings of the National Academy of Sciences of the United States of America2003
A duodenally absorbable CXC chemokine receptor 4 antagonist, KRH-1636, exhibits a potent and selective anti-HIV-1 activity.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
28 citing papers in PubMed, 156 citations in OpenAlex.
- Targeting the chemokine receptor CXCR4 for cancer therapies.Biomarker research · 2025Review
- CXC chemokine receptor 4 (CXCR4) blockade in cancer treatment.Journal of cancer research and clinical oncology · 2023Review
- Targeting CXCR4 and CD47 Receptors: An Overview of New and Old Molecules for a Biological Personalized Anticancer Therapy.International journal of molecular sciences · 2022Review
- At the Bench: Pre-clinical evidence for multiple functions of CXCR4 in cancer.Journal of leukocyte biology · 2021Review
- "Fusion and binding inhibition" key target for HIV-1 treatment and pre-exposure prophylaxis: targets, drug delivery and nanotechnology approaches.Drug delivery · 2017Review
- Structural Analysis of Chemokine Receptor-Ligand Interactions.Journal of medicinal chemistry · 2017Review
- Multi-objective active machine learning rapidly improves structure-activity models and reveals new protein-protein interaction inhibitors.Chemical science · 2016Article
- AMD3100/CXCR4 Inhibitor.Frontiers in immunology · 2015Review
- Single oral administration of the novel CXCR4 antagonist, KRH-3955, induces an efficient and long-lasting increase of white blood cell count in normal macaques, and prevents CD4 depletion in SHIV-infected macaques: a preliminary study.Medical microbiology and immunology · 2013Article
- Small molecule inhibitors of CXCR4.Theranostics · 2013Review
- Drug discovery research targeting the CXC chemokine receptor 4 (CXCR4).Journal of medicinal chemistry · 2012Review
- G protein-coupled receptors--recent advances.Acta biochimica Polonica · 2012Review
- Mobilization of hematopoietic stem and progenitor cells using inhibitors of CXCR4 and VLA-4.Leukemia · 2012Review
- PET imaging of CXCR4 receptors in cancer by a new optimized ligand.ChemMedChem · 2011Article
- Agonists for the Chemokine Receptor CXCR4.ACS medicinal chemistry letters · 2011Article
- Computational analysis of the structural mechanism of inhibition of chemokine receptor CXCR4 by small molecule antagonists.Experimental biology and medicine (Maywood, N.J.) · 2011Article
- Novel compounds containing multiple guanide groups that bind the HIV coreceptor CXCR4.Antimicrobial agents and chemotherapy · 2011Article
- Differential CXCR4 expression and function in subpopulations of the feline lymphoma cell line 3201 susceptible to feline immunodeficiency virus.Journal of feline medicine and surgery · 2010Article
- The novel CXCR4 antagonist KRH-3955 is an orally bioavailable and extremely potent inhibitor of human immunodeficiency virus type 1 infection: comparative studies with AMD3100.Antimicrobial agents and chemotherapy · 2009Article
- Efficient inhibition of SDF-1alpha-mediated chemotaxis and HIV-1 infection by novel CXCR4 antagonists.Cancer science · 2009Article
Corrections and comments
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Authors and funding
13 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A low molecular weight nonpeptide compound, KRH-1636, efficiently blocked replication of various T cell line-tropic (X4) HIV type 1 (HIV-1) in MT-4 cells and peripheral blood mononuclear cells through the inhibition of viral entry and membrane fusion via the CXC chemokine receptor (CXCR)4 coreceptor but not via CC chemokine receptor 5. It also inhibited binding of the CXC chemokine, stromal cell-derived factor 1alpha, to CXCR4 specifically and subsequent signal transduction. KRH-1636 prevented monoclonal antibodies from binding to CXCR4 without down-modulation of the coreceptor. The inhibitory effect against X4 viral replication by KRH-1636 was clearly reproduced in the human peripheral blood lymphocytesevere combined immunodeficiency mouse system. Furthermore, this compound was absorbed into the blood after intraduodenal administration as judged by anti-HIV-1 activity and liquid chromatography MS in the plasma. Thus, KRH-1636 seems to be a promising agent for the treatment of HIV-1 infection.
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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.