NDLI: A duodenally absorbable CXC chemokine receptor 4 antagonist, KRH-1636, exhibits a potent and selective anti-HIV-1 activity.

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A duodenally absorbable CXC chemokine receptor 4 antagonist, KRH-1636, exhibits a potent and selective anti-HIV-1 activity.

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A duodenally absorbable CXC chemokine receptor 4 antagonist, KRH-1636, exhibits a potent and selective anti-HIV-1 activity.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Yokoyama-kumakura, Sei Yamamoto, Naoki Ichiyama, Kozi Tanaka, Reiko Niitani, Yoshiaki Takaku, Hiroshi Koyanagi, Yoshio Bannai, Kenji Miyano-kurosaki, Naoko Yanaka, Mikiro Tanaka, Yuetsu Edamatsu, Takeo Hirose, Kunitaka
Description	Author Affiliation: Ichiyama K ( Department of Molecular Virology, Bio-Response, Graduate School, Tokyo Medical and Dental University, Tokyo 113-8519, Japan.);
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.
ISSN	00278424
e-ISSN	10916490
Journal	Proceedings of the National Academy of Sciences of the United States of America
Issue Number	7
Volume Number	100
Language	English
Publisher	National Academy of Sciences
Publisher Date	2003-04-01
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Anti-HIV Agents Pharmacology Arginine HIV-1 Drug Effects Lymphocytes Immunology Pyridines Receptors, CXCR4 Antagonists & Inhibitors Animals Administration & Dosage Analogs & Derivatives Intestinal Absorption Mice Mice, SCID Rats, Wistar T-Lymphocytes Tumor Cells, Cultured Research Support, Non-U.S. Gov't Multidisciplinary
Content Type	Text
Resource Type	Article
Subject	Multidisciplinary

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