ArticleAntimicrobial agents and chemotherapy2009
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.
Article in Antimicrobial agents and chemotherapy, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
22 citing papers in PubMed, 58 citations in OpenAlex.
- Targeting the chemokine receptor CXCR4 for cancer therapies.Biomarker research · 2025Review
- CD4Science (New York, N.Y.) · 2021Article
- At the Bench: Pre-clinical evidence for multiple functions of CXCR4 in cancer.Journal of leukocyte biology · 2021Review
- CXCL12 Signaling in the Tumor Microenvironment.Advances in experimental medicine and biology · 2021Review
- Discoveries and developments of CXCR4-targeted HIV-1 entry inhibitors.Experimental biology and medicine (Maywood, N.J.) · 2020Review
- Dual-action CXCR4-targeting liposomes in leukemia: function blocking and drug delivery.Blood advances · 2019Article
- Targeting CXCL12/CXCR4 Axis in Tumor Immunotherapy.Current medicinal chemistry · 2019Review
- CXCR4, the master regulator of neutrophil trafficking in homeostasis and disease.European journal of clinical investigation · 2018Review
- Two distinct CXCR4 antagonists mobilize progenitor cells in mice by different mechanisms.Blood advances · 2017Article
- Structural Analysis of Chemokine Receptor-Ligand Interactions.Journal of medicinal chemistry · 2017Review
- Oncogenic roles and drug target of CXCR4/CXCL12 axis in lung cancer and cancer stem cell.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2016Review
- Enhancement of the CXCL12/CXCR4 axis due to acquisition of gemcitabine resistance in pancreatic cancer: effect of CXCR4 antagonists.BMC cancer · 2016Article
- AMD3100/CXCR4 Inhibitor.Frontiers in immunology · 2015Review
- Effectiveness of AMD3100 in treatment of leukemia and solid tumors: from original discovery to use in current clinical practice.Experimental hematology & oncology · 2015Review
- Pharmacologically antagonizing the CXCR4-CXCL12 chemokine pathway with AMD3100 inhibits sunlight-induced skin cancer.The Journal of investigative dermatology · 2014Article
- Targeting chemokine receptor CXCR4 for treatment of HIV-1 infection, tumor progression, and metastasis.Current topics in medicinal chemistry · 2014Review
- 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
- Mobilization of hematopoietic stem and progenitor cells using inhibitors of CXCR4 and VLA-4.Leukemia · 2012Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
12 authors at 4 institutions in 2 countries.
Funding
Abstract
The previously reported CXCR4 antagonist KRH-1636 was a potent and selective inhibitor of CXCR4-using (X4) human immunodeficiency virus type 1 (HIV-1) but could not be further developed as an anti-HIV-1 agent because of its poor oral bioavailability. Newly developed KRH-3955 is a KRH-1636 derivative that is bioavailable when administered orally with much more potent anti-HIV-1 activity than AMD3100 and KRH-1636. The compound very potently inhibits the replication of X4 HIV-1, including clinical isolates in activated peripheral blood mononuclear cells from different donors. It is also active against recombinant X4 HIV-1 containing resistance mutations in reverse transcriptase and protease and envelope with enfuvirtide resistance mutations. KRH-3955 inhibits both SDF-1alpha binding to CXCR4 and Ca(2+) signaling through the receptor. KRH-3955 inhibits the binding of anti-CXCR4 monoclonal antibodies that recognize the first, second, or third extracellular loop of CXCR4. The compound shows an oral bioavailability of 25.6% in rats, and its oral administration blocks X4 HIV-1 replication in the human peripheral blood lymphocyte-severe combined immunodeficiency mouse system. Thus, KRH-3955 is a new promising agent for HIV-1 infection and AIDS.
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What OpenQuestion holds
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.