J. Exp. Med.
© The Rockefeller University Press
0022-1007/97/10/1389/05 $2.00
Volume 186, Number 8, October 20, 1997 1389-1393

BRIEF DEFINITIVE REPORT:
A Small Molecule CXCR4 Inhibitor that Blocks T Cell Line-tropic HIV-1 Infection

By Tsutomu Murakami,^* Toshihiro Nakajima, Yoshio Koyanagi,^* Kazunobu Tachibana,^§ Nobutaka Fujii, Hirokazu Tamamura, Nobuaki Yoshida,^§ Michinori Waki,^¶ Akiyoshi Matsumoto,^¶ Osamu Yoshie, Tadamitsu Kishimoto,^** Naoki Yamamoto,^* and Takashi Nagasawa^§

From the ^* Department of Microbiology, Tokyo Medical and Dental University School of Medicine, Bunkyo-ku, Tokyo 113, Japan;  Shionogi Institute for Medical Science, 2-5-1 Mishima, Settsu, Osaka 566, Japan; ^§ Department of Immunology, Research Institute, Osaka Medical Center for Maternal and Child Health, 840 Murodo-cho, Izumi, Osaka 590-02, Japan; and  Faculty of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606, Japan; ^¶ SEIKAGAKU Corp., Chyuo-ku, Tokyo 103, Japan; ^** Department of Medicine III, Osaka University Medical School, 2-2 Yamada-oka, Suita, Osaka 565, Japan

Several members of the chemokine receptor family have been shown to function in association with CD4 to permit human immunodeficiency virus type 1 (HIV-1) entry and infection. The CXC chemokine receptor CXCR4/fusin is a receptor for pre-B cell growth stimulating factor (PBSF)/stromal cell-derived factor 1 (SDF-1) and serves as a coreceptor for the entry of T cell line-tropic HIV-1 strains. Thus, the development of CXCR4 antagonists or agonists may be useful in the treatment of HIV-1 infection. T22 ([Tyr^5,12,Lys⁷]-polyphemusin II) is a synthesized peptide that consists of 18 amino acid residues and an analogue of polyphemusin II isolated from the hemocyte debris of American horseshoe crabs (Limulus polyphemus). T22 was found to specifically inhibit the ability of T cell line-tropic HIV-1 to induce cell fusion and infect the cell lines transfected with CXCR4 and CD4 or peripheral blood mononuclear cells. In addition, T22 inhibited Ca²⁺ mobilization induced by pre-B cell growth stimulating factor (PBSF)/SDF-1 stimulation through CXCR4. Thus, T22 is a small molecule CXCR4 inhibitor that blocks T cell line-tropic HIV-1 entry into target cells.

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