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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• Zhou, N., Luo, Z., Luo, J., Liu, D., Hall, J. W., Pomerantz, R. J., Huang, Z. (2001). Structural and Functional Characterization of Human CXCR4 as a Chemokine Receptor and HIV-1 Co-receptor by Mutagenesis and Molecular Modeling Studies. J. Biol. Chem. 276: 42826-42833 [Abstract] [Full Text]  
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• Clapham, P. R, McKnight, A. (2001). HIV-1 receptors and cell tropism. Br Med Bull 58: 43-59 [Abstract] [Full Text]  
• Dragic, T. (2001). An overview of the determinants of CCR5 and CXCR4 co-receptor function. J. Gen. Virol. 82: 1807-1814 [Full Text]  
• Fenard, D., Lambeau, G., Maurin, T., Lefebvre, J.-C., Doglio, A. (2001). A Peptide Derived from Bee Venom-Secreted Phospholipase A2 Inhibits Replication of T-Cell Tropic HIV-1 Strains via Interaction with the CXCR4 Chemokine Receptor. Mol. Pharmacol. 60: 341-347 [Abstract] [Full Text]  
• Heveker, N., Tissot, M., Thuret, A., Schneider-Mergener, J., Alizon, M., Roch, M., Marullo, S. (2001). Pharmacological Properties of Peptides Derived from Stromal Cell-Derived Factor 1: Study on Human Polymorphonuclear Cells. Mol. Pharmacol. 59: 1418-1425 [Abstract] [Full Text]  
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• Holz-Smith, S. L., Sun, I-C., Jin, L., Matthews, T. J., Lee, K.-H., Chen, C. H. (2001). Role of Human Immunodeficiency Virus (HIV) Type 1 Envelope in the Anti-HIV Activity of the Betulinic Acid Derivative IC9564. Antimicrob. Agents Chemother. 45: 60-66 [Abstract] [Full Text]  
• Zaitseva, M., Lee, S., Lapham, C., Taffs, R., King, L., Romantseva, T., Manischewitz, J., Golding, H. (2000). Interferon gamma and interleukin 6 modulate the susceptibility of macrophages to human immunodeficiency virus type 1 infection. Blood 96: 3109-3117 [Abstract] [Full Text]  
• Xiao, H., Neuveut, C., Tiffany, H. L., Benkirane, M., Rich, E. A., Murphy, P. M., Jeang, K.-T. (2000). Selective CXCR4 antagonism by Tat: Implications for in vivo expansion of coreceptor use by HIV-1. Proc. Natl. Acad. Sci. USA 97: 11466-11471 [Abstract] [Full Text]  
• Rusconi, S., La Seta Catamancio, S., Citterio, P., Bulgheroni, E., Croce, F., Herrmann, S. H., Offord, R. E., Galli, M., Hirsch, M. S. (2000). Combination of CCR5 and CXCR4 Inhibitors in Therapy of Human Immunodeficiency Virus Type 1 Infection: In Vitro Studies of Mixed Virus Infections. J. Virol. 74: 9328-9332 [Abstract] [Full Text]  
• Koshiba, T., Hosotani, R., Miyamoto, Y., Ida, J., Tsuji, S., Nakajima, S., Kawaguchi, M., Kobayashi, H., Doi, R., Hori, T., Fujii, N., Imamura, M. (2000). Expression of Stromal Cell-derived Factor 1 and CXCR4 Ligand Receptor System in Pancreatic Cancer: A Possible Role for Tumor Progression. Clin. Cancer Res. 6: 3530-3535 [Abstract] [Full Text]  
• D'Souza, M. P., Cairns, J. S., Plaeger, S. F. (2000). Current Evidence and Future Directions for Targeting HIV Entry: Therapeutic and Prophylactic Strategies. JAMA 284: 215-222 [Abstract] [Full Text]  
• Owen, S. M., Masciotra, S., Novembre, F., Yee, J., Switzer, W. M., Ostyula, M., Lal, R. B. (2000). Simian Immunodeficiency Viruses of Diverse Origin Can Use CXCR4 as a Coreceptor for Entry into Human Cells. J. Virol. 74: 5702-5708 [Abstract] [Full Text]  
• Sei, S., Yang, Q.-e., O'Neill, D., Yoshimura, K., Nagashima, K., Mitsuya, H. (2000). Identification of a Key Target Sequence To Block Human Immunodeficiency Virus Type 1 Replication within the gag-pol Transframe Domain. J. Virol. 74: 4621-4633 [Abstract] [Full Text]  
• De Clercq, E. (2000). Inhibition of HIV Infection by Bicyclams, Highly Potent and Specific CXCR4 Antagonists. Mol. Pharmacol. 57: 833-839 [Abstract] [Full Text]  
• Murakami, T., Freed, E. O. (2000). Genetic Evidence for an Interaction between Human Immunodeficiency Virus Type 1 Matrix and alpha -Helix 2 of the gp41 Cytoplasmic Tail. J. Virol. 74: 3548-3554 [Abstract] [Full Text]  
• Murphy, P. M., Baggiolini, M., Charo, I. F., Hebert, C. A., Horuk, R., Matsushima, K., Miller, L. H., Oppenheim, J. J., Power, C. A. (2000). International Union of Pharmacology. XXII. Nomenclature for Chemokine Receptors. Pharmacol. Rev. 52: 145-176 [Abstract] [Full Text]  
• Hodohara, K., Fujii, N., Yamamoto, N., Kaushansky, K. (2000). Stromal cell-derived factor-1 (SDF-1) acts together with thrombopoietin to enhance the development of megakaryocytic progenitor cells (CFU-MK). Blood 95: 769-775 [Abstract] [Full Text]  
• Cheng, Z.-J., Zhao, J., Sun, Y., Hu, W., Wu, Y.-L., Cen, B., Wu, G.-X., Pei, G. (2000). beta -Arrestin Differentially Regulates the Chemokine Receptor CXCR4-mediated Signaling and Receptor Internalization, and This Implicates Multiple Interaction Sites between beta -Arrestin and CXCR4. J. Biol. Chem. 275: 2479-2485 [Abstract] [Full Text]  
• Murakami, T., Freed, E. O. (2000). The long cytoplasmic tail of gp41 is required in a cell type-dependent manner for HIV-1 envelope glycoprotein incorporation into virions. Proc. Natl. Acad. Sci. USA 97: 343-348 [Abstract] [Full Text]  
• Blanco, J., Barretina, J., Henson, G., Bridger, G., De Clercq, E., Clotet, B., Esté, J. A. (2000). The CXCR4 Antagonist AMD3100 Efficiently Inhibits Cell-Surface-Expressed Human Immunodeficiency Virus Type 1 Envelope-Induced Apoptosis. Antimicrob. Agents Chemother. 44: 51-56 [Abstract] [Full Text]  
• Schramm, B., Penn, M. L., Speck, R. F., Chan, S. Y., De Clercq, E., Schols, D., Connor, R. I., Goldsmith, M. A. (2000). Viral Entry through CXCR4 Is a Pathogenic Factor and Therapeutic Target in Human Immunodeficiency Virus Type 1 Disease. J. Virol. 74: 184-192 [Abstract] [Full Text]  
• Daelemans, D., Schols, D., Witvrouw, M., Pannecouque, C., Hatse, S., van Dooren, S., Hamy, F., Klimkait, T., de Clercq, E., VanDamme, A.-M. (2000). A Second Target for the Peptoid Tat/Transactivation Response Element Inhibitor CGP64222: Inhibition of Human Immunodeficiency Virus Replication by Blocking CXC-Chemokine Receptor 4-Mediated Virus Entry. Mol. Pharmacol. 57: 116-124 [Abstract] [Full Text]  
• Trkola, A., Matthews, J., Gordon, C., Ketas, T., Moore, J. P. (1999). A Cell Line-Based Neutralization Assay for Primary Human Immunodeficiency Virus Type 1 Isolates That Use either the CCR5 or the CXCR4 Coreceptor. J. Virol. 73: 8966-8974 [Abstract] [Full Text]  
• Nisole, S., Krust, B., Callebaut, C., Guichard, G., Muller, S., Briand, J.-P., Hovanessian, A. G. (1999). The Anti-HIV Pseudopeptide HB-19 Forms a Complex with the Cell-surface-expressed Nucleolin Independent of Heparan Sulfate Proteoglycans. J. Biol. Chem. 274: 27875-27884 [Abstract] [Full Text]  
• Wang, J. M., Oppenheim, J. J. (1999). Interference with the Signaling Capacity of CC Chemokine Receptor 5 Can Compromise Its Role as an HIV-1 Entry Coreceptor in Primary T Lymphocytes. J. Exp. Med. 190: 591-596 [Full Text]  
• Murakami, T., Zhang, T.-Y., Koyanagi, Y., Tanaka, Y., Kim, J., Suzuki, Y., Minoguchi, S., Tamamura, H., Waki, M., Matsumoto, A., Fujii, N., Shida, H., Hoxie, J. A., Peiper, S. C., Yamamoto, N. (1999). Inhibitory Mechanism of the CXCR4 Antagonist T22 against Human Immunodeficiency Virus Type 1 Infection. J. Virol. 73: 7489-7496 [Abstract] [Full Text]  
• Blanpain, C., Lee, B., Vakili, J., Doranz, B. J., Govaerts, C., Migeotte, I., Sharron, M., Dupriez, V., Vassart, G., Doms, R. W., Parmentier, M. (1999). Extracellular Cysteines of CCR5 Are Required for Chemokine Binding, but Dispensable for HIV-1 Coreceptor Activity. J. Biol. Chem. 274: 18902-18908 [Abstract] [Full Text]  
• Yang, O. O., Swanberg, S. L., Lu, Z., Dziejman, M., McCoy, J., Luster, A. D., Walker, B. D., Herrmann, S. H. (1999). Enhanced Inhibition of Human Immunodeficiency Virus Type 1 by Met-Stromal-Derived Factor 1beta Correlates with Down-Modulation of CXCR4. J. Virol. 73: 4582-4589 [Abstract] [Full Text]  
• Kawabata, K., Ujikawa, M., Egawa, T., Kawamoto, H., Tachibana, K., Iizasa, H., Katsura, Y., Kishimoto, T., Nagasawa, T. (1999). A cell-autonomous requirement for CXCR4 in long-term lymphoid and myeloid reconstitution. Proc. Natl. Acad. Sci. USA 96: 5663-5667 [Abstract] [Full Text]  
• Brelot, A., Heveker, N., Adema, K., Hosie, M. J., Willett, B., Alizon, M. (1999). Effect of Mutations in the Second Extracellular Loop of CXCR4 on Its Utilization by Human and Feline Immunodeficiency Viruses. J. Virol. 73: 2576-2586 [Abstract] [Full Text]  
• Doranz, B. J., Orsini, M. J., Turner, J. D., Hoffman, T. L., Berson, J. F., Hoxie, J. A., Peiper, S. C., Brass, L. F., Doms, R. W. (1999). Identification of CXCR4 Domains That Support Coreceptor and Chemokine Receptor Functions. J. Virol. 73: 2752-2761 [Abstract] [Full Text]  
• Arakaki, R., Tamamura, H., Premanathan, M., Kanbara, K., Ramanan, S., Mochizuki, K., Baba, M., Fujii, N., Nakashima, H. (1999). T134, a Small-Molecule CXCR4 Inhibitor, Has No Cross-Drug Resistance with AMD3100, a CXCR4 Antagonist with a Different Structure. J. Virol. 73: 1719-1723 [Abstract] [Full Text]  
• Esté, J. A., Cabrera, C., De Clercq, E., Struyf, S., Van Damme, J., Bridger, G., Skerlj, R. T., Abrams, M. J., Henson, G., Gutierrez, A., Clotet, B., Schols, D. (1999). Activity of Different Bicyclam Derivatives against Human Immunodeficiency Virus Depends on Their Interaction with the CXCR4 Chemokine Receptor. Mol. Pharmacol. 55: 67-73 [Abstract] [Full Text]  
• Sakaida, H., Hori, T., Yonezawa, A., Sato, A., Isaka, Y., Yoshie, O., Hattori, T., Uchiyama, T. (1998). T-Tropic Human Immunodeficiency Virus Type 1 (HIV-1)-Derived V3 Loop Peptides Directly Bind to CXCR-4 and Inhibit T-Tropic HIV-1 Infection. J. Virol. 72: 9763-9770 [Abstract] [Full Text]  
• Edinger, A. L., Hoffman, T. L., Sharron, M., Lee, B., Yi, Y., Choe, W., Kolson, D. L., Mitrovic, B., Zhou, Y., Faulds, D., Collman, R. G., Hesselgesser, J., Horuk, R., Doms, R. W. (1998). An Orphan Seven-Transmembrane Domain Receptor Expressed Widely in the Brain Functions as a Coreceptor for Human Immunodeficiency Virus Type 1 and Simian Immunodeficiency Virus. J. Virol. 72: 7934-7940 [Abstract] [Full Text]  
• Hoffman, T. L., Stephens, E. B., Narayan, O., Doms, R. W. (1998). HIV type I envelope determinants for use of the CCR2b, CCR3, STRL33, and APJ coreceptors. Proc. Natl. Acad. Sci. USA 95: 11360-11365 [Abstract] [Full Text]  
• Ganju, R. K., Brubaker, S. A., Meyer, J., Dutt, P., Yang, Y., Qin, S., Newman, W., Groopman, J. E. (1998). The alpha -Chemokine, Stromal Cell-derived Factor-1alpha , Binds to the Transmembrane G-protein-coupled CXCR-4 Receptor and Activates Multiple Signal Transduction Pathways. J. Biol. Chem. 273: 23169-23175 [Abstract] [Full Text]  
• Loetscher, P., Gong, J.-H., Dewald, B., Baggiolini, M., Clark-Lewis, I. (1998). N-terminal Peptides of Stromal Cell-derived Factor-1 with CXC Chemokine Receptor 4 Agonist and Antagonist Activities. J. Biol. Chem. 273: 22279-22283 [Abstract] [Full Text]  
• Labrosse, B., Brelot, A., Heveker, N., Sol, N., Schols, D., De Clercq, E., Alizon, M. (1998). Determinants for Sensitivity of Human Immunodeficiency Virus Coreceptor CXCR4 to the Bicyclam AMD3100. J. Virol. 72: 6381-6388 [Abstract] [Full Text]  
• Lee, B., Doranz, B. J., Ratajczak, M. Z., Doms, R. W. (1998). An Intricate Web: Chemokine Receptors, HIV-1 and Hematopoiesis. Stem Cells 16: 79-88 [Abstract] [Full Text]  
• Baggiolini, M., Moser, B. (1997). Blocking Chemokine Receptors. J. Exp. Med. 186: 1189-1191 [Full Text]  
• Dragic, T., Trkola, A., Thompson, D. A. D., Cormier, E. G., Kajumo, F. A., Maxwell, E., Lin, S. W., Ying, W., Smith, S. O., Sakmar, T. P., Moore, J. P. (2000). A binding pocket for a small molecule inhibitor of HIV-1 entry within the transmembrane helices of CCR5. Proc. Natl. Acad. Sci. USA 97: 5639-5644 [Abstract] [Full Text]  

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