Experimental Hematology
Volume 34, Issue 11 , Pages 1553-1562 , November 2006

Cloning and characterizing mutated human stromal cell-derived factor-1 (SDF-1): C-terminal α-helix of SDF-1α plays a critical role in CXCR4 activation and signaling, but not in CXCR4 binding affinity

  • Yi Tan

      Affiliations

    • Department of Clinical Pharmacology, Pharmacy School of Jinan University, Guangzhou, China
    • College of Bioengineering, Key Laboratory for Biomechanics and Tissue Engineering of the State Ministry of Education, Chongqing University, Chongqing, China
    • Bioengineering Medicine Research Center of the State Ministry of Education, Jinan University, Guangzhou, China
    • School of Pharmaceutical Sciences, Wenzhou Medical College, Wenzhou, China
    • ,
  • Jun Du

      Affiliations

    • School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China
    • ,
  • Shaoxi Cai

      Affiliations

    • College of Bioengineering, Key Laboratory for Biomechanics and Tissue Engineering of the State Ministry of Education, Chongqing University, Chongqing, China
    • ,
  • Xiaokun Li

      Affiliations

    • Bioengineering Medicine Research Center of the State Ministry of Education, Jinan University, Guangzhou, China
    • School of Pharmaceutical Sciences, Wenzhou Medical College, Wenzhou, China
    • ,
  • Weifeng Ma

      Affiliations

    • College of Bioengineering, Key Laboratory for Biomechanics and Tissue Engineering of the State Ministry of Education, Chongqing University, Chongqing, China
    • ,
  • Zhigang Guo

      Affiliations

    • College of Bioengineering, Key Laboratory for Biomechanics and Tissue Engineering of the State Ministry of Education, Chongqing University, Chongqing, China
    • ,
  • Hongyuan Chen

      Affiliations

    • College of Bioengineering, Key Laboratory for Biomechanics and Tissue Engineering of the State Ministry of Education, Chongqing University, Chongqing, China
    • ,
  • Zhifeng Huang

      Affiliations

    • School of Pharmaceutical Sciences, Wenzhou Medical College, Wenzhou, China
    • ,
  • Jian Xiao

      Affiliations

    • Department of Clinical Pharmacology, Pharmacy School of Jinan University, Guangzhou, China
    • School of Pharmaceutical Sciences, Wenzhou Medical College, Wenzhou, China
    • ,
  • Lu Cai

      Affiliations

    • School of Pharmaceutical Sciences, Wenzhou Medical College, Wenzhou, China
    • Departments of Medicine, Radiation Oncology and Pharmacology and Toxicology, University of Louisville, Ky., USA
    • Corresponding Author InformationOffprint requests to: Lu Cai, M.D., Ph.D., Departments of Medicine, Radiation Oncology and Pharmacology and Toxicology, University of Louisville, 511 South Floyd Street, MDR 533, Louisville, KY 40202
    • ,
  • Shaohui Cai

      Affiliations

    • Department of Clinical Pharmacology, Pharmacy School of Jinan University, Guangzhou, China
    • Corresponding Author InformationOffprint requests to: Shaohui Cai, M.D., Ph.D., Departments of Medicine, Radiation Oncology and Pharmacology and Toxicology, University of Louisville, 511 South Floyd Street, MDR 533, Louisville, KY 40202

Received 9 June 2006 ,Revised 28 June 2006 ,Accepted 10 July 2006.

References 

  1. Baggiolini M, Dewald B, Moser B. Human chemokines: an update. Annu Rev Immunol. 1997;15:675–705
  2. Aiuti A, Webb IJ, Bleul C, Springer T, Gutierrez-Ramos JC. The chemokine SDF-1 is a chemoattractant for human CD34+ hematopoietic progenitor cells and provides a new mechanism to explain the mobilization of CD34+ progenitors to peripheral blood. J Exp Med. 1997;185:111–120
  3. Nagasawa T, Hirota S, Tachibana K, et al. Defects of B-cell lymphopoiesis and bone-marrow myelopoiesis in mice lacking the CXC chemokine PBSF/SDF-1. Nature. 1996;382:635–638
  4. Tachibana K, Hirota S, Iizasa H, et al. The chemokine receptor CXCR4 is essential for vascularization of the gastrointestinal tract. Nature. 1998;393:591–594
  5. Bleul CC, Fuhlbrigge RC, Casasnovas JM, Aiuti A, Springer TA. A highly efficacious lymphocyte chemoattractant, stromal cell-derived factor 1 (SDF-1). J Exp Med. 1996;184:1101–1109
  6. Loetscher M, Geiser T, O'Reilly T, Zwahlen R, Baggiolini M, Moser B. Cloning of a human seven-transmembrane domain receptor, LESTR, that is highly expressed in leukocytes. J Biol Chem. 1994;269:232–237
  7. Federsppiel B, Melhado IG, Duncan AM, et al. Molecular cloning of the cDNA and chromosomal localization of the gene for a putative seven-transmembrane segment (7-TMS) receptor isolated from human spleen. Genomics. 1993;16:707–712
  8. Feng Y, Broder CC, Kennedy PE, Berger EA. HIV-1 entry cofactor: functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor. Science. 1996;272:872–877
  9. Aiuti A, Tavian M, Cipponi A, et al. Expression of CXCR4, the receptor for stromal cell-derived factor-1 on fetal and adult human lympho-hematopoietic progenitors. Eur J Immunol. 1999;29:1823–1831
  10. Moore MA, Hattori K, Heissig B, et al. Mobilization of endothelial and hematopoietic stem and progenitor cells by adenovector-mediated elevation of serum levels of SDF-1, VEGF, and angiopoietin-1. Ann N Y Acad Sci. 2001;938:36–45
  11. Perez LE, Alpdogan O, Shieh JH, et al. Increased plasma levels of stromal-derived factor-1 (SDF-1/CXCL12) enhance human thrombopoiesis and mobilize human colony-forming cells (CFC) in NOD/SCID mice. Exp Hematol. 2004;32:300–307
  12. Muller A, Homey B, Soto H, et al. A. Involvement of chemokine receptors in breast cancer metastasis. Nature. 2001;410:50–56
  13. Kucia M, Reca R, Miekus K, et al. Trafficking of normal stem cells and metastasis of cancer stem cells involve similar mechanisms: pivotal role of the SDF-1-CXCR4 axis. Stem Cells. 2005;23:879–894
  14. Balabanian K, Lagane B, Infantino S, et al. The chemokine SDF-1/CXCL12 binds to and signals through the orphan receptor RDC1 in T lymphocytes. J Biol Chem. 2005;280:35760–35766
  15. Jones SW, Brockbank SM, Mobbs ML, et al. The orphan G-protein coupled receptor RDC1: evidence for a role in chondrocyte hypertrophy and articular cartilage matrix turnover. Osteoarthritis Cartilage. 2006;14:597–608
  16. Liles WC, Broxmeyer HE, Rodger E, et al. Mobilization of hematopoietic progenitor cells in healthy volunteers by AMD3100, a CXCR4 antagonist. Blood. 2003;102:2728–2730
  17. Zhong R, Law P, Wong D, Merzouk A, Salari H, Ball ED. Small peptide analogs to stromal derived factor-1 enhance chemotactic migration of human and mouse hematopoietic cells. Exp Hematol. 2004;32:470–475
  18. Broxmeyer HE, Orschell CM, Clapp DW, et al. Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist. J Exp Med. 2005;201:1307–1318
  19. Pelus LM, Bian H, Fukuda S, Wong D, Merzouk A, Salari H. The CXCR4 agonist peptide, CTCE-0021, rapidly mobilizes polymorphonuclear neutrophils and hematopoietic progenitor cells into peripheral blood and synergizes with granulocyte colony-stimulating factor. Exp Hematol. 2005;33:295–307
  20. Sun YX, Schneider A, Jung Y, et al. Skeletal localization and neutralization of the SDF-1(CXCL12)/CXCR4 axis blocks prostate cancer metastasis and growth in osseous sites in vivo. J Bone Miner Res. 2005;20:318–329
  21. Tamamura H, Hori A, Kanzaki N, et al. T140 analogs as CXCR4 antagonists identified as anti-metastatic agents in the treatment of breast cancer. FEBS Lett. 2003;550:79–83
  22. Crump MP, Gong JH, Loetscher P, et al. Solution structure and basis for functional activity of stromal cell-derived factor-1; dissociation of CXCR4 activation from binding and inhibition of HIV-1. EMBO J. 1997;16:6996–7007
  23. Luo J, Luo Z, Zhou N, Hall JW, Huang Z. Attachment of C-terminus of SDF-1 enhances the biological activity of its N-terminal peptide. Biochem Biophys Res Commun. 1999;264:42–47
  24. Tudan C, Willick GE, Chahal S, et al. C-terminal cyclization of an SDF-1 small peptide analogue dramatically increases receptor affinity and activation of the CXCR4 receptor. J Med Chem. 2002;45:2024–2031
  25. Gozansky EK, Louis JM, Caffrey M, Clore GM. Mapping the binding of the N-terminal extracellular tail of the CXCR4 receptor to stromal cell-derived factor-1alpha. J Mol Biol. 2005;345:651–658
  26. Cai SH, Tan Y, Ren XD, Li XH, Cai SX, Du J. Loss of C-terminal alpha-helix decreased SDF-1alpha-mediated signaling and chemotaxis without influencing CXCR4 internalization. Acta Pharmacol Sin. 2004;25:152–160
  27. Princen K, Hatse S, Vermeire K, De Clercq E, Schols D. Evaluation of SDF-1/CXCR4-induced Ca2+ signaling by fluorometric imaging plate reader (FLIPR) and flow cytometry. Cytometry A. 2003;51:35–45
  28. Bajetto A, Barbero S, Bonavia R, et al. Stromal cell-derived factor-1alpha induces astrocyte proliferation through the activation of extracellular signal-regulated kinases 1/2 pathway. J Neurochem. 2001;77:1226–1236
  29. Zhao M, Discipio RG, Wimmer AG, Schraufstatter IU. Regulation of CXCR4-mediated nuclear translocation of extracellular signal-related kinases 1 and 2. Mol Pharmacol. 2006;69:66–75
  30. Hesselgesser J, Liang M, Hoxie J, et al. Identification and characterization of the CXCR4 chemokine receptor in human T cell lines: ligand binding, biological activity, and HIV-1 infectivity. J Immunol. 1998;160:877–883
  31. Heveker N, Montes M, Germeroth L, et al. Dissociation of the signalling and antiviral properties of SDF-1-derived small peptides. Curr Biol. 1998;8:369–376
  32. Roland J, Murphy BJ, Ahr B, et al. Role of the intracellular domains of CXCR4 in SDF-1-mediated signaling. Blood. 2003;101:399–406
  33. Haribabu B, Richardson RM, Fisher I, et al. Regulation of human chemokine receptors CXCR4. Role of phosphorylation in desensitization and internalization. J Biol Chem. 1997;272:28726–28731
  34. Hendrix CW, Collier AC, Lederman MM, et al. Safety, pharmacokinetics, and antiviral activity of AMD3100, a selective CXCR4 receptor inhibitor, in HIV-1 infection. J Acquir Immune Defic Syndr. 2004;37:1253–1262
  35. Este JA. Virus entry as a target for anti-HIV intervention. Curr Med Chem. 2003;10:1617–1632
  36. Castagna A, Biswas P, Beretta A, Lazzarin A. The appealing story of HIV entry inhibitors: from discovery of biological mechanisms to drug development. Drugs. 2005;65:879–904
  37. Dealwis C, Fernandez EJ, Thompson DA, Simon RJ, Siani MA, Lolis E. Crystal structure of chemically synthesized [N33A] stromal cell-derived factor 1alpha, a potent ligand for the HIV-1 “fusin” coreceptor. Proc Natl Acad Sci U S A. 1998;95:6941–6946

PII: S0301-472X(06)00430-9

doi: 10.1016/j.exphem.2006.07.001

Experimental Hematology
Volume 34, Issue 11 , Pages 1553-1562 , November 2006

Article Tools

* Image Usage & Resolution