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Chemical Compound Review

Mozobil     1-[[4-(1,4,8,11- tetrazacyclotetradec-1...

Synonyms: Plerixafor, Mozobil (TN), CHEMBL18442, SureCN19038, SID791, ...
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Disease relevance of SID791

  • AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor [1].
  • AMD3100 also mobilized murine long-term repopulating (LTR) cells that engrafted primary and secondary lethally-irradiated mice, and human CD34(+) cells that can repopulate nonobese diabetic-severe combined immunodeficiency (SCID) mice [2].
  • AMD3100, a CXCR4 antagonist, was active against HIV-2 and SHIV89.6, a finding consistent with the use of the CXCR4 co-receptor by these isolates, but was inactive against SIV strains [3].
  • AMD3100 was well tolerated and caused only mild, transient toxicity [4].
  • Collectively, these data suggest that monocytes mobilized into the blood by G-CSF or AMD3100 stimulate angiogenesis at sites of ischemia through a paracrine mechanism [5].

High impact information on SID791

  • Thus, AMD3100 prevents CXCR4 functioning as both a HIV-1 co-receptor and a CXC-chemokine receptor [1].
  • AMD3100 prevents monoclonal antibody 12G5 from binding to CXCR4, but has no effect on binding of monoclonal antibody 2D7 to CCR5 [1].
  • AMD3100, a selective antagonist of CXCL12 that binds to its receptor, CXCR4, was evaluated in murine and human systems for mobilizing capacity, alone and in combination with granulocyte colony-stimulating factor (G-CSF) [2].
  • Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist [2].
  • Human CD34(+) cells isolated after treatment with G-CSF plus AMD3100 expressed a phenotype that was characteristic of highly engrafting mouse HSCs [2].

Chemical compound and disease context of SID791

  • The bicyclam AMD3100 is a potent and selective inhibitor of the replication of human immunodeficiency virus type 1 and type 2 (HIV-1 and HIV-2) [6].
  • When primary FIV isolates were evaluated for their drug susceptibility in feline thymocytes, the bicyclams AMD3100 and its Zn2+ complex, AMD3479, inhibited all six primary isolates at equal potency [7].
  • The prototype, JM3100 (19a, isolated as the octahydrochloride salt), which contains a p-phenylenebis(methylene) moiety linking the cyclam rings, inhibited the replication of HIV-1 (IIIB) and HIV-2 (ROD) at EC50's of 4.2 and 5.9 nM, respectively, while remaining nontoxic to MT-4 cells at concentrations exceeding 421 microM [8].
  • HIV-1 strains resistant to two prototype bicyclams, JM2763 and SID791 (JM3100), were raised [9].

Biological context of SID791

  • The kinetics of angiogenic-cell mobilization by these agents appears to be distinct, with more rapid revascularization observed in AMD3100-treated mice [5].
  • Peripheral-blood mononuclear cells (PBMCs) mobilized with AMD3100, a CXCR4 antagonist, combined with granulocyte colony-stimulating factor (G-CSF) have reconstituted autologous hematopoiesis in cancer patients following myeloablative conditioning [10].
  • The chemokine CXCL12 induced chemotaxis in CXCR4-positive pancreatic carcinoma cell lines, which was inhibited by anti-CXCR4 monoclonal antibody and by the antagonist AMD3100 [11].
  • The absolute CD34+ cell counts observed at 4 and 6 hours following AMD3100 were higher in the 240 microg/kg group (19.3 +/- 6.9/microL and 20.4 +/- 7.6/microL, respectively) compared with the 160 microg/kg group (11.3 +/- 2.7/microL and 11.3 +/- 2.5/microL, respectively) [12].
  • Metal ion binding in the cyclam rings of AMD3100 increased its dependence on Asp(262) and provided a tighter molecular map of the binding site, where borderline mutational hits became clear hits for the Zn(II)-loaded analog [13].

Anatomical context of SID791

  • We show engraftment of transduced AMD3100-mobilized CD34(+) cells with Neo(R) gene marked myeloid and lymphoid cells up to 32 months after transplantation, demonstrating the ability of AMD3100 to mobilize true long-term repopulating hematopoietic stem cells [14].
  • G-CSF and AMD3100 mobilize monocytes into the blood that stimulate angiogenesis in vivo through a paracrine mechanism [5].
  • Combination treatment with G-CSF and AMD3100 resulted in the earliest and most complete recovery in blood flow to the ischemic hindlimb [5].
  • The cell line Hs766T produces high levels of CXCL12, and addition of the CXCR4 antagonist AMD3100 partially inhibited proliferation, indicating an autocrine loop [11].
  • We also showed that AMD3100 (a specific CXCR4 antagonist) effectively reduced tumor growth and ascitic fluid formation in nude mice inoculated with NUGC4 cells [15].

Associations of SID791 with other chemical compounds


Gene context of SID791

  • AMD3100 dose dependently inhibited the binding of a specific CXCR4 monoclonal antibody to SUP-T1 cells as measured by flow cytometry [21].
  • CXCL12 increased the growth in PES 41, PES 43, and PES 47 cells under suboptimal (1% serum) and serum-free culture conditions; AMD3100 (1 mumol/L) inhibited the spontaneous and CXCL12-induced proliferation [22].
  • Several strains replicated in Delta32/Delta32 CCR5 PBMCs with CXCR4 blocked by AMD3100 [23].
  • It was insensitive to eotaxin, vMIP-1 and I309 when tested individually, but was inhibited completely when vMIP-1 or I309 was combined with AMD3100 [24].
  • Early recruitment of adoptively transferred OVA-specific CTL into B16/OVA tumors expressing high levels of CXCL12 was significantly reduced in comparison to B16/OVA tumors, and this reduction was reversed when tumor-specific CTLs were pretreated with the specific CXCR4 antagonist, AMD3100 [25].

Analytical, diagnostic and therapeutic context of SID791

  • In addition, mobilization with AMD3100 may provide a safer preparative approach for HSC transplantation in genetic and other nonmalignant disorders [26].
  • These data show that AMD3100 is a potent and rapid mobilizer of angiogenic cells and demonstrate the feasibility of obtaining and storing large numbers of angiogenic cells by leukapheresis [27].
  • We investigated whether AMD3100, a selective CXCR4 antagonist, could mobilize hematopoietic progenitor cells from marrow to peripheral blood in healthy human volunteers [4].
  • CONCLUSION: AMD3100 appears to be a safe and effective agent for the rapid mobilization of CD34+ cells in patients who have received prior chemotherapy [12].
  • The small-molecule-mobilising drug AMD3100 was selected because mobilisation and apheresis can be done on the same day [28].


  1. AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor. Donzella, G.A., Schols, D., Lin, S.W., Esté, J.A., Nagashima, K.A., Maddon, P.J., Allaway, G.P., Sakmar, T.P., Henson, G., De Clercq, E., Moore, J.P. Nat. Med. (1998) [Pubmed]
  2. Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist. Broxmeyer, H.E., Orschell, C.M., Clapp, D.W., Hangoc, G., Cooper, S., Plett, P.A., Liles, W.C., Li, X., Graham-Evans, B., Campbell, T.B., Calandra, G., Bridger, G., Dale, D.C., Srour, E.F. J. Exp. Med. (2005) [Pubmed]
  3. Susceptibility of HIV-2, SIV and SHIV to various anti-HIV-1 compounds: implications for treatment and postexposure prophylaxis. Witvrouw, M., Pannecouque, C., Switzer, W.M., Folks, T.M., De Clercq, E., Heneine, W. Antivir. Ther. (Lond.) (2004) [Pubmed]
  4. Mobilization of hematopoietic progenitor cells in healthy volunteers by AMD3100, a CXCR4 antagonist. Liles, W.C., Broxmeyer, H.E., Rodger, E., Wood, B., Hübel, K., Cooper, S., Hangoc, G., Bridger, G.J., Henson, G.W., Calandra, G., Dale, D.C. Blood (2003) [Pubmed]
  5. G-CSF and AMD3100 mobilize monocytes into the blood that stimulate angiogenesis in vivo through a paracrine mechanism. Capoccia, B.J., Shepherd, R.M., Link, D.C. Blood (2006) [Pubmed]
  6. Determinants for sensitivity of human immunodeficiency virus coreceptor CXCR4 to the bicyclam AMD3100. Labrosse, B., Brelot, A., Heveker, N., Sol, N., Schols, D., De Clercq, E., Alizon, M. J. Virol. (1998) [Pubmed]
  7. Bicyclams, selective antagonists of the human chemokine receptor CXCR4, potently inhibit feline immunodeficiency virus replication. Egberink, H.F., De Clercq, E., Van Vliet, A.L., Balzarini, J., Bridger, G.J., Henson, G., Horzinek, M.C., Schols, D. J. Virol. (1999) [Pubmed]
  8. Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-tetraazamacrocycles that inhibit HIV replication. Effects of macrocyclic ring size and substituents on the aromatic linker. Bridger, G.J., Skerlj, R.T., Thornton, D., Padmanabhan, S., Martellucci, S.A., Henson, G.W., Abrams, M.J., Yamamoto, N., De Vreese, K., Pauwels, R. J. Med. Chem. (1995) [Pubmed]
  9. The bicyclams, a new class of potent human immunodeficiency virus inhibitors, block viral entry after binding. De Vreese, K., Reymen, D., Griffin, P., Steinkasserer, A., Werner, G., Bridger, G.J., Esté, J., James, W., Henson, G.W., Desmyter, J., Anné, J., De Clercq, I. Antiviral Res. (1996) [Pubmed]
  10. Durable engraftment of AMD3100-mobilized autologous and allogeneic peripheral-blood mononuclear cells in a canine transplantation model. Burroughs, L., Mielcarek, M., Little, M.T., Bridger, G., Macfarland, R., Fricker, S., Labrecque, J., Sandmaier, B.M., Storb, R. Blood (2005) [Pubmed]
  11. Increased survival, proliferation, and migration in metastatic human pancreatic tumor cells expressing functional CXCR4. Marchesi, F., Monti, P., Leone, B.E., Zerbi, A., Vecchi, A., Piemonti, L., Mantovani, A., Allavena, P. Cancer Res. (2004) [Pubmed]
  12. Rapid mobilization of CD34+ cells following administration of the CXCR4 antagonist AMD3100 to patients with multiple myeloma and non-Hodgkin's lymphoma. Devine, S.M., Flomenberg, N., Vesole, D.H., Liesveld, J., Weisdorf, D., Badel, K., Calandra, G., DiPersio, J.F. J. Clin. Oncol. (2004) [Pubmed]
  13. Molecular mechanism of AMD3100 antagonism in the CXCR4 receptor: transfer of binding site to the CXCR3 receptor. Rosenkilde, M.M., Gerlach, L.O., Jakobsen, J.S., Skerlj, R.T., Bridger, G.J., Schwartz, T.W. J. Biol. Chem. (2004) [Pubmed]
  14. AMD3100 mobilizes hematopoietic stem cells with long-term repopulating capacity in nonhuman primates. Larochelle, A., Krouse, A., Metzger, M., Orlic, D., Donahue, R.E., Fricker, S., Bridger, G., Dunbar, C.E., Hematti, P. Blood (2006) [Pubmed]
  15. Role of the CXCL12/CXCR4 axis in peritoneal carcinomatosis of gastric cancer. Yasumoto, K., Koizumi, K., Kawashima, A., Saitoh, Y., Arita, Y., Shinohara, K., Minami, T., Nakayama, T., Sakurai, H., Takahashi, Y., Yoshie, O., Saiki, I. Cancer Res. (2006) [Pubmed]
  16. Medical applications of macrocyclic polyamines. Liang, F., Wan, S., Li, Z., Xiong, X., Yang, L., Zhou, X., Wu, C. Current medicinal chemistry. (2006) [Pubmed]
  17. CXCR4 inhibition synergizes with cytotoxic chemotherapy in gliomas. Redjal, N., Chan, J.A., Segal, R.A., Kung, A.L. Clin. Cancer Res. (2006) [Pubmed]
  18. Macrophage tropism of human immunodeficiency virus type 1 isolates from brain and lymphoid tissues predicts neurotropism independent of coreceptor specificity. Gorry, P.R., Bristol, G., Zack, J.A., Ritola, K., Swanstrom, R., Birch, C.J., Bell, J.E., Bannert, N., Crawford, K., Wang, H., Schols, D., De Clercq, E., Kunstman, K., Wolinsky, S.M., Gabuzda, D. J. Virol. (2001) [Pubmed]
  19. Inhibition of human immunodeficiency virus replication by a dual CCR5/CXCR4 antagonist. Princen, K., Hatse, S., Vermeire, K., Aquaro, S., De Clercq, E., Gerlach, L.O., Rosenkilde, M., Schwartz, T.W., Skerlj, R., Bridger, G., Schols, D. J. Virol. (2004) [Pubmed]
  20. Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-azamacrocycles that inhibit HIV-1 and HIV-2 replication by antagonism of the chemokine receptor CXCR4. Bridger, G.J., Skerlj, R.T., Padmanabhan, S., Martellucci, S.A., Henson, G.W., Struyf, S., Witvrouw, M., Schols, D., De Clercq, E. J. Med. Chem. (1999) [Pubmed]
  21. Inhibition of T-tropic HIV strains by selective antagonization of the chemokine receptor CXCR4. Schols, D., Struyf, S., Van Damme, J., Esté, J.A., Henson, G., De Clercq, E. J. Exp. Med. (1997) [Pubmed]
  22. Human melanoma metastases express functional CXCR4. Scala, S., Giuliano, P., Ascierto, P.A., Ieranò, C., Franco, R., Napolitano, M., Ottaiano, A., Lombardi, M.L., Luongo, M., Simeone, E., Castiglia, D., Mauro, F., De Michele, I., Calemma, R., Botti, G., Caracò, C., Nicoletti, G., Satriano, R.A., Castello, G. Clin. Cancer Res. (2006) [Pubmed]
  23. Identification of a subset of human immunodeficiency virus type 1 (HIV-1), HIV-2, and simian immunodeficiency virus strains able to exploit an alternative coreceptor on untransformed human brain and lymphoid cells. Willey, S.J., Reeves, J.D., Hudson, R., Miyake, K., Dejucq, N., Schols, D., De Clercq, E., Bell, J., McKnight, A., Clapham, P.R. J. Virol. (2003) [Pubmed]
  24. Use of alternate coreceptors on primary cells by two HIV-1 isolates. Cilliers, T., Willey, S., Sullivan, W.M., Patience, T., Pugach, P., Coetzer, M., Papathanasopoulos, M., Moore, J.P., Trkola, A., Clapham, P., Morris, L. Virology (2005) [Pubmed]
  25. Murine B16 melanomas expressing high levels of the chemokine stromal-derived factor-1/CXCL12 induce tumor-specific T cell chemorepulsion and escape from immune control. Vianello, F., Papeta, N., Chen, T., Kraft, P., White, N., Hart, W.K., Kircher, M.F., Swart, E., Rhee, S., Palù, G., Irimia, D., Toner, M., Weissleder, R., Poznansky, M.C. J. Immunol. (2006) [Pubmed]
  26. Mobilization as a preparative regimen for hematopoietic stem cell transplantation. Chen, J., Larochelle, A., Fricker, S., Bridger, G., Dunbar, C.E., Abkowitz, J.L. Blood (2006) [Pubmed]
  27. Angiogenic cells can be rapidly mobilized and efficiently harvested from the blood following treatment with AMD3100. Shepherd, R.M., Capoccia, B.J., Devine, S.M., Dipersio, J., Trinkaus, K.M., Ingram, D., Link, D.C. Blood (2006) [Pubmed]
  28. The chemokine (C-X-C motif) receptor 4 inhibitor AMD3100 accelerates blood flow restoration in diabetic mice. Jiao, C., Fricker, S., Schatteman, G.C. Diabetologia (2006) [Pubmed]
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