| Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo. | |
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MedLine Citation:
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PMID: 19053768 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The interaction of the chemokine receptor CXCR4 with its ligand CXCL12 is involved in many biological processes such as hematopoesis, migration of immune cells, as well as in cancer metastasis. CXCR4 also mediates the infection of T-cells with X4-tropic HIV functioning as a coreceptor for the viral envelope protein gp120. Here, we describe highly potent, selective CXCR4 inhibitors that block CXCR4/CXCL12 interactions in vitro and in vivo as well as the infection of target cells by X4-tropic HIV. |
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Authors:
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Gebhard Thoma; Markus B Streiff; Jiri Kovarik; Fraser Glickman; Trixie Wagner; Christian Beerli; Hans-Günter Zerwes |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 51 ISSN: 1520-4804 ISO Abbreviation: J. Med. Chem. Publication Date: 2008 Dec |
Date Detail:
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Created Date: 2008-12-18 Completed Date: 2009-01-22 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: United States |
Other Details:
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Languages: eng Pagination: 7915-20 Citation Subset: IM |
Affiliation:
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Novartis Institutes for BioMedical Research, Forum 1, Novartis Campus, CH-4002 Basel, Switzerland. gebhard.thoma@novartis.com |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Animals Biological Availability Chemistry, Pharmaceutical / methods Chemokine CXCL12 / chemistry Chemokines / metabolism Drug Design HIV Envelope Protein gp120 / chemistry Humans Inhibitory Concentration 50 Models, Chemical Rats Receptors, CXCR4 / antagonists & inhibitors, chemistry* T-Lymphocytes / metabolism, virology Thiourea / chemistry* |
| Chemical | |
Reg. No./Substance:
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0/CXCL12 protein, human; 0/CXCR4 protein, human; 0/Chemokine CXCL12; 0/Chemokines; 0/HIV Envelope Protein gp120; 0/Receptors, CXCR4; 62-56-6/Thiourea |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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