Specific CD4 down-modulating compounds with potent anti-HIV activity

Journal of Leukocyte Biology

Volumn 74, Issue 5, 2003, Pages 667-675

  Vermeire, Kurt ^a   Schols, Dominique ^a  

^a REGA INSTITUTE FOR MEDICAL RESEARCH   (Belgium)

Author keywords

CADA; CCR5; CD4 receptor down modulation; CXCR4 antagonists; HIV entry inhibitors

Indexed keywords

1,1' [1,4 PHENYLENEBIS(METHYLENE)]BIS(1,4,8,11 TETRAAZACYCLOTETRADECANE); AMD 2763; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; CD4 ANTIGEN; CD4 IMMUNOGLOBULIN G2; CHEMOKINE RECEPTOR ANTAGONIST; CHEMOKINE RECEPTOR CCR5; CHEMOKINE RECEPTOR CXCR4; ENFUVIRTIDE; GLYCOPROTEIN GP 120; LYMPHOCYTE RECEPTOR; N [4 [[[6,7 DIHYDRO 2 (4 METHYLPHENYL) 5H BENZOCYCLOHEPTEN 8 YL]CARBONYL]AMINO]BENZYL] N,N DIMETHYL 2H TETRAHYDROPYRAN 4 AMINIUM CHLORIDE; QJ 023; QJ 028; RECEPTOR BLOCKING AGENT; SULFONAMIDE; UNCLASSIFIED DRUG; VIRUS ENVELOPE PROTEIN;

ACQUIRED IMMUNE DEFICIENCY SYNDROME; ANTIVIRAL ACTIVITY; CONFERENCE PAPER; DOWN REGULATION; DRUG EFFECT; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG RECEPTOR BINDING; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; LYMPHOCYTE; MONOCYTE; NONHUMAN; PRIORITY JOURNAL; PROTEIN PROTEIN INTERACTION; VIRUS ADSORPTION; VIRUS INHIBITION;

ANTI-HIV AGENTS; ANTIGENS, CD4; CELL LINE; HIV ENVELOPE PROTEIN GP120; HIV-1; HUMANS; LYMPHOCYTES; MONOCYTES; RECEPTORS, HIV;

HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 0347320929     PISSN: 07415400     EISSN: None     Source Type: Journal    
DOI: 10.1189/jlb.0403177     Document Type: Conference Paper

References (113)

1. Dalgleish, A. G., Beverley, P. C., Clapham, P. R., Crawford, D. H., Greaves, M. F., Weiss, R. A. (1984) The CD4 (T4) antigen is an essential component of the receptor for the AIDS retrovirus. Nature 312, 763-767.
2. Klatzmann, D., Champagne, E., Chamaret, S., Gruest, J., Guetard, D., Hercend, T., Gluckman, J. C., Montagnier, L. (1984) T-lymphocyte T4 molecule behaves as the receptor for human retrovirus LAV. Nature 312, 767-768.
3. Feng, Y., Broder, C. C., Kennedy, P. E., Berger, E. A. (1996) HIV-1 entry cofactor: functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor. Science 272, 872-877.
4. Alkhatib, G., Combadiere, C., Broder, C. C., Feng, Y., Kennedy, P. E., Murphy, P. M., Berger, E. A. (1996) CC CKR5: a RANTES, MIP-1 α, MIP-1β receptor as a fusion cofactor for macrophage-tropic HIV-1. Science 272, 1955-1958.
5. Chan, D. C., Kim, P. S., (1998) HIV entry and its inhibition. Cell 93, 681-684.
6. Burton, D. R., Pyati, J., Koduri, R., Sharp, S. J., Thornton, G. B., Parren, P. W., Sawyer, L. S., Hendry, R. M., Dunlop, N., Nara, P. L. (1994) Efficient neutralization of primary isolates of HIV-1 by a recombinant human monoclonal antibody. Science 266, 1024-1027.
7. Saphire, E. O., Parren, P. W., Pantophlet, R., Zwick, M. B., Morris, G. M., Rudd, P. M., Dwek, R. A., Stanfield, R. L., Burton, D. R., Wilson, I. A. (2001) Crystal structure of a neutralizing human IgG against HIV-1: a template for vaccine design. Science 293, 1155-1159.
8. Trkola, A., Purtscher, M., Muster, T., Ballaun, C., Buchacher, A., Sullivan, N., Srinivasan, K., Sodroski, J., Moore, J. P., Katinger, H. (1996) Human monoclonal antibody 2G12 defines a distinctive neutralization epitope on the gp120 glycoprotein of human immunodeficiency virus type 1. J. Virol. 70, 1100-1108.
9. Sanders, R. W., Venturi, M., Schiffner, L., Kalyanaraman, R., Katinger, H., Lloyd, K. O., Kwong, P. D., Moore, J. P. (2002) The mannose-dependent epitope for neutralizing antibody 2G12 on human immunodeficiency virus type 1 glycoprotein gp120. J. Virol. 76, 7293-7305.
10. Muster, T., Steindl, F., Purtscher, M., Trkola, A., Klima, A., Himmler, G., Ruker, F., Katinger, H. (1993) A conserved neutralizing epitope on gp41 of human immunodeficiency virus type 1. J. Virol. 67, 6642-6647.
11. Parker, C. E., Deterding, L. J., Hager-Braun, C., Binley, J. M., Schulke, N., Katinger, H., Moore, J. P., Tomer, K. B. (2001) Fine definition of the epitope on the gp41 glycoprotein of human immunodeficiency virus type 1 for the neutralizing monoclonal antibody 2F5. J. Virol. 75, 10906-10911.
12. Smith, D. H., Byrn, R. A., Marsters, S. A., Gregory, T., Groopman, J. E., Capon, D. J. (1987) Blocking of HIV-1 infectivity by a soluble, secreted form of the CD4 antigen. Science 238, 1704-1707.
13. Fisher, R. A., Bertonis, J. M., Meier, W., Johnson, V. A., Costopoulos, D. S., Liu, T., Tizard, R., Walker, B. D., Hirsch, M. S., Schooley, R. T. (1988) HIV infection is blocked in vitro by recombinant soluble CD4. Nature 331, 76-78.
14. Deen, K. C., McDougal, J. S., Inacker, R., Folena-Wasserman, G., Arthos, J., Rosenberg, J., Maddon, P. J., Axel, R., Sweet, R. W. (1988) A soluble form of CD4 (T4) protein inhibits AIDS virus infection. Nature 331, 82-84.
15. Traunecker, A., Luke, W., Karjalainen, K. (1988) Soluble CD4 molecules neutralize human immunodeficiency virus type 1. Nature 331, 84-86.
16. Clapham, P. R., Weber, J. N., Whitby, D., McIntosh, K., Dalgleish, A. G., Maddon, P. J., Deen, K. C., Sweet, R. W., Weiss, R. A. (1989) Soluble CD4 blocks the infectivity of diverse strains of HIV and SIV for T cells and monocytes but not for brain and muscle cells. Nature 337, 368-370.
17. Schooley, R. T., Merigan, T. C., Gaut, P., Hirsch, M. S., Holodniy, M., Flynn, T., Liu, S., Byington, R. E., Henochowicz, S., Gubish, E. (1990) Recombinant soluble CD4 therapy in patients with the acquired immunodeficiency, syndrome (AIDS) and AIDS-related complex. A phase I-II escalating dosage trial. Ann. Intern. Med. 112, 247-253.
18. Schacker, T., Coombs, R. W., Collier, A. C., Zeh, J. E., Fox, I., Alam, J., Nelson, K., Eggert, E., Corey, L. (1994) The effects of high-dose recombinant soluble CD4 on human immunodeficiency virus type 1 viremia. J. Infect. Dis. 169, 37-40.
19. Schacker, T., Collier, A. C., Coombs, R., Unadkat, J. D., Fox, I., Alam, J., Wang, J. P., Eggert, E., Corey, L. (1995) Phase I study of high-dose, intravenous rsCD4 in subjects with advanced HIV-1 infection. J. Acquir. Immune Defic. Syndr. Hum. Retrovirol. 9, 145-152.
20. Allan, J. S. (1991) Receptor-mediated activation of inmmnodeficiency viruses in viral fusion. Science 252, 1322-1323.
21. Sullivan, N., Sun, Y., Li, J., Hofmann, W., Sodroski, J. (1995) Replicative function and neutralization sensitivity of envelope glycoproteins from primary and T-cell line-passaged human immunodeficiency virus type 1 isolates. J. Virol. 69, 4413-4422.
22. Schenten, D., Marcon, L., Karlsson, G. B., Parolin, C., Kodama, T., Gerard, N., Sodroski, J. (1999) Effects of soluble CD4 on simian immunodeficiency virus infection of CD4-positive and CD4-negative cells. J. Virol. 73, 5373-5380.
23. Daar, E. S., Li, X. L., Moudgil, T., Ho, D. D. (1990) High concentrations of recombinant soluble CD4 are required to neutralize primary human immunodeficiency virus type 1 isolates. Proc. Natl. Acad. Sci. USA 87, 6574-6578.
24. Moore, J. P., McKeating, J. A., Weiss, R. A., Sattentau, Q. J. (1990) Dissociation of gp120 from HIV-1 virions induced by soluble CD4. Science 250, 1139-1142.
25. Moore, J. P., McKeating, J. A., Huang, Y. X., Ashkenuzi, A., Ho, D. D. (1992) Virions of primary human immunodeficiency virus type 1 isolates resistant to soluble CD4 (sCD4) neutralization differ in sCD4 binding and glycoprotein gp120 retention from sCD4-sensitive isolates. J. Virol. 66, 235-243.
26. Salzwedel, K., Smith, E. D., Dey, B., Berger, E. A. (2000) Sequential CD4-coreceptor interactions in human immunodeficiency virus type 1 Env function: soluble CD4 activates Env for coreceptor-dependent fusion and reveals blocking activities of antibodies against cryptic conserved epitopes on gp120. J. Virol. 74, 326-333.
27. Sullivan, N., Sun, Y., Sattentau, Q., Thali, M., Wu, D. Denisova, G., Gershoni, J., Robinson, J., Moore, J., Sodroski, J. (1998) CD4-Induced conformational changes in the human immunodeficiency virus type 1 gp120 glycoprotein: consequences for virus entry and neutralization. J. Virol. 72, 4694-4703.
28. Capon, D. J., Chamow, S. M., Mordenti, J., Marsters, S. A., Gregory, T., Mitsuya, H., Byrn, R. A., Lucas, C., Wurm, F. M., Groopman, J. E. (1989) Designing CD4 immunoadhesins for AIDS therapy. Nature 337, 525-531.
29. Traunecker, A., Schneider, J., Kiefer, H., Karjalainen, K. (1989) Highly efficient neutralization of HIV with recombinant CD4-immunoglobulin molecules. Nature 339, 68-70.
30. Allaway, G. P., Davis-Bruno, K. L., Beaudry, G. A., Garcia, E. B., Wong, E. L., Ryder, A. M., Hasel, K. W., Gauduin, M. C., Koup, R. A., McDougal, J. S. (1995) Expression and characterization of CD4-IgG2, a novel heterotetramer thal neutralizes primary HIV type 1 isolates. AIDS Res. Hum. Retroviruses 11, 533-539.
31. Gauduin, M. C., Allaway, G. P., Maddon, P. J., Barbas, C. F., III, Burton, D. R., Koup, R. A. (1996) Effective ex vivo neutralization of human immunodeficiency virus type 1 in plasma by recombinant immunoglobulin molecules. J. Virol. 70, 2586-2592.
32. Gauduin, M. C., Allaway, G. P., Olson, W. C., Weir, R., Maddon, P. J., Koup, R. A. (1998) CD4-immunoglobulin G2 protects Hu-PBL-SCID mice against challenge by Primary human immunodeficiency virus type 1 isolates. J. Virol. 72, 3475-3478.
33. Ketas, T. J., Frank, I., Klasse, P. J., Sullivan, B. M., Gardner, J. P., Spenlehauer, C., Nesin, M., Olson, W. C., Moore, J. P., Pope, M. (2003) Human imnmnodeficiency virus type 1 attachment, coreceptor, and fusion inhibitors are active against both direct and trans infection of primary cells. J. Virol. 77, 2762-2767.
34. Nagashima, K. A., Thompson, D. A., Rosenfield, S. I., Maddon, P. J., Dragic, T., Olson, W. C. (2001) Human immunodeficiency virus type 1 entrv inhibitors PRO 542 and T-20 are potently synergistic in blocking virus-cell and cell-cell fusion. J. Infect. Dis. 183, 1121-1125.
35. Jacobson, J. M., Lowy, I., Fletcher, C. V., O'Neill, T. J., Tran, D. N., Ketas, T. J., Trkola, A., Klotman, M. E., Maddon, P. J., Olson, W. C., et al. (2000) Single-dose safety, pharmacology, and antiviral activity of the human immunodeficiency virus (HIV) type 1 entry inhibitor PRO 542 in HIV-infected adults. J. Inject. Dis. 182, 326-329.
36. Shearer, W. T., Israel, R. J., Starr, S., Fletcher, C. V., Wara, D., Rathore, M., Church, J., DeVille, J., Fenton, T., Graham, B., et al. (2000) Recombinant CD4-IgG2 in human immunodeficiency virus type 1-infected children: phase 1/2 study. J. Infect. Dis. 182, 1774-1779.
37. Dey, B., Del Castillo, C. S., Berger, E. A. (2003) Neutralization of human immunodeficiency virus type 1 by sCD4-17b, a single-chain chimeric protein, based on sequential interaction of gp120 with CD4 and coreceptor. J. Virol. 77, 2859-2865.
38. Baba, M., Pauwels, R., Balzarini, J., Arnout, J., Desmyter, J., De Clercq, E. (1988) Mechanism of inhibitory, effect of dextran sulfate and heparin on replication of human immunodeficiency virus in vitro. Proc. Natl. Acad. Sci. USA 85, 6132-6136.
39. Schols, D., Pauwels, R., Desmyter, J., De Clercq, E. (1990) Dextran sulfate and other polyanionic anti-HIV compounds specifically interact with the viral gp120 glycoprotein expressed by T-cells persistently infected with HIV-1. Virology 175, 556-561.
40. Baba, M., Schols, D., De Clereq, E., Pauwels, R., Nagy, M., Gyorgyi-Edelenyi, J., Low, M., Gorug, S. (1990) Novel sulfated polymers as highly potent and selective inhibitors of human immunodeficiency virus replication and giant cell formation. Antimicrob. Agents Chemother. 34, 134-138.
41. Esté, J. A., Schols, D., De Vreese, K., Van Laethem, K., Vandamme, A. M., Desmyter, J., De Clercq, E. (1997) Development of resistance of human immunodeficiency virus type 1 to dextran sulfate associated with the emergence of specific mutations in the envelope gp120 glycoprotein. Mol. Pharmacol. 52, 98-104.
42. Rusconi, S., Moonis, M., Merrill, D. P., Pallai, P. V., Neidhardt, E. A., Singh, S. K., Willis, K. J., Osburne, M. S., Profy, A. T., Jenson, J. C., et al. (1996) Naphthalene sulfonate polymers with CD4-blocking and anti-human immunodeficiency virus type 1 activities. Antimicrob. Agents Chemother. 40, 234-236.
43. Greenhead, P., Hayes, P., Watts, P. S., Laing, K. G., Griffin, G. E., Shattock, R. J. (2000) Parameters of human immunodeficiency virus infection of human cervical tissue and inhibition by vaginal virucides. J. Virol. 74, 5577-5586.
44. Weber, J., Nunn, A., O'Connor, T., Jeffries, D., Kitchen, V., McCormack, S., Stott, J., Almond, N., Stone, A., Darbyshire, J. (2001) 'Chemical condoms' for the prevention of HIV infection: evaluation of novel agents against SHIV89.6PD in vitro and in vivo. AIDS 15, 1563-1568.
45. Van Damme, L., Wright, A., Depraetere, K., Rosenstein, I., Vandersmissen, V., Poulter, L., McKinlay, M., Van Dyck, E., Weber, J., Profy, A., et al. (2000) A phase I study of a novel potential intravaginal microbicide, PRO 2000, in healthy sexually inactive women. Sex. Transm. Infect. 76, 126-130.
46. Mayer, K. H., Karim, S. A., Kelly, C., Maslankowski, L., Rees, H., Profy, A. T., Day, J., Welch, J., Rosenberg, Z. (2003) Safety and tolerability of vaginal PRO 2000 gel in sexually active HIV-uninfected and abstinent HIV-infected women. AIDS 17, 321-329.
47. Boyd, M. R., Gustafson, K. R., McMahon, J. B., Shoemaker, R. H., O'Keefe, B. R., Mori, T., Gulakowski, R. J., Wu, L., Rivera, M. I., Laurencot, C. M., et al. (1997) Discovery of cyanovirin-N, a novel human immunodeficiency virus-inactivating protein that binds viral surface envelope glycoprotein gp120: potential applications to microbicide development. Antimicrob. Agents Chemother. 41, 1521-1530.
48. Dey, B., Lerner, D. L., Lusso, P., Boyd, M. R., Elder, J. H., Berger, E. A. (2000) Multiple antiviral activities of cyanovirin-N: blocking of human immunodeficiency virus type 1 gp120 interaction with CD4 and coreceptor and inhibition of diverse enveloped viruses. J. Virol. 74, 4562-4569.
49. Esser, M. T., Mori, T., Mondor, I., Sallentau, Q. J., Dey, B., Berger, E. A., Boyd, M. R., Lifson, J. D. (1999) Cyanovirin-N binds to gp120 to interfere with CD4-dependent human immunodeficiency virus type 1 virion binding, fusion, and infectivity but does not affect the CD4 binding site on gp120 or soluble CD4-induced conformational changes in gp120. J. Virol. 73, 4360-4371.
50. Mori, T., Boyd, M. R. (2001) Cyanovirin-N, a potent human immunodeficiency virus-inactivating protein, blocks both CD4-dependent and CD4-independent binding of soluble gp120 (sgp120) to target cells, inhibits sCD4-induced binding of sgp120 to cell-associated CXCR4, and dissociates bound sgp120 from target cells. Antimicrob. Agents Chemother. 45, 664-672.
51. Shenoy, S. R., O'Keefe, B. R., Bolmstedt, A. J., Cartner, L. K., Boyd, M. R. (2001) Selective interactions of the human immunodeficiency virus-inactivating protein cyanovirin-N with high-mannose oligosaceharides on gp120 and other glycoproteins. J. Pharmacol. Exp. Ther. 297, 704-710.
52. Barrientos, L. G., Louis, J. M., Ratner, D. M., Seeberger, P. H., Gronenborn, A. M. (2003) Solution structure of a circular-permuted variant of the potent HIV-inactivating protein cyanovirin-N: structural basis for protein stability and oligosaceharide interaction. J. Mol. Biol. 325, 211-223.
53. Gulakowski, R. J., McMahon, J. B., Buckheit, R. W., Jr., Gustafson, K. R., Boyd, M. R. (1997) Antireplicative and anticytopathic activities of prostratin, a non-tumor-promoting phorbol ester, against human immunodeficiency virus (HIV). Antiviral Res. 33, 87-97.
54. Hezareh, M., Dudognon, P., Pondarzewski, M., Brown, S. J., Carpentier, J. L., Foti, M. (2003) Prostratin induces internalization and degradation of HIV-specific receptor and co-receptor through activation of novel PKCs. From: 10th Conference on Retroviruses and Opportunistic Infections: February 10-14, 2003; Boston, Massachusetts, USA.
55. Vermeire, K., Zhang, Y., Priucen, K., Hatse, S., Samala, M. F., Dey, K., Choi, H. J., Alm, Y., Sodoma, A., Snocck, R., et al. (2002) CADA inhibits human immunodeficiency virus and hunan herpesvirus 7 replication by down-modulation of the cellular CD4 receptor. Virology 302, 342-353.
56. Vermeire, K., Bell, T. W., Choi, H. J., Jin, Q., Samala, M. F., Sodoma, A., De Clereq, E., Schols, D. (2003) The anti-HIV potency of cyclotriazadisulfonamide analogs is directly correlated with their ability to down-modulate the CD4 receptor. Mol. Pharmacol. 63, 203-210.
57. Vermeire, K., De Clercq, E., Dey, K., Bell, T. W., Schols, D. (2003) In vitro synergy between the CD4 down-modulating compound, compound, CADA, and multiple anti-HIV drugs. From: 16th International Conference on Antiviral Research; April 27-May 1, 2003; Savannah, GA, USA.
58. Layne, S. P., Merges, M. J., Dembo, M., Spouge, J. L., Nara, P. L. (1990) HIV requires multiple gp120 molecules for CD4-mediated infection. Nature 346, 277-279.
59. Chesebro, B., Buller, R., Portis, J., Wehrly, K. (1990) Failure of human immunodeficiency virus entry and infection in CD4-positive human brain and skin cells. J. Virol. 64, 215-221.
60. Kabat, D., Kozak, S. L., Wehrly, K., Chesebro, B. (1994) Differences in CD4 dependence for infectivity of laboratory-adapted and primary patient isolates of human immunodeficiency virus type 1. J. Virol. 68, 2570-2577.
61. Kozak, S. L., Platt, E. J., Madani, N., Ferro, F. E., Jr., Peden, K., Kabat, D. (1997) CD4, CXCR-4, and CCR-5 dependencies for infections by primary, patient and laboratory-adapted isolates of human immunodeficiency virus type 1. J. Virol. 71, 873-882.
62. Platt, E. J., Madani, N., Kozak, S. L., Kabat, D. (1997) Infectious properties of human immunodeficiency virus type 1 mutants with distinct affinities for the CD4 receptor. J. Virol. 71, 883-890.
63. Platt, E. J., Wehrly, K., Kuhmann, S. E., Chesebro, B., Kabat, D. (1998) Effects of CCR5 and CD4 cell surface concentrations on infections by macrophagetropic isolates of human immunodeficiency virus type 1. J. Virol. 72, 2855-2864.
64. Platt, E. J., Kozak, S. L., Kabat, D. (2000) Critical role of enhanced CD4 affinity in laboratory adaptation of human immunodeficiency virus type 1. AIDS Res. Hum. Retroviruses 16, 871-882.
65. Naif, H. M., Li, S., Alali, M., Sloane, A., Wu, L., Kelly, M., Lynch, G., Lloyd, A., Cunningham, A. L. (1998) CCR5 expression correlates with susceptibility of maturing monocytes to human immunodeficiency virus type 1 infection. J. Virol. 72, 830-836.
66. Fear, W. R., Kesson, A. M., Naif, H., Lynch, G. W., Cunningham, A. L. (1998) Differential tropism and chemokine receptor expression of human immunodeficiency virus type 1 in neonatal monocytes, monocyte-derived macrophages and placental macrophages. J. Virol. 72, 1334-1344.
67. Dumonceaux, J., Nisole, S., Chanel, C., Quivet, L., Amara, A., Baleux, F., Briand, P., Hazan, U. (1998) Spontaneous mutations in the env gene of the human immunodeficiency virus type 1 NDK isolate are associated with a CD4-independent entry phenotype. J. Virol. 72, 512-519.
68. Hoffman, T. L., LaBranche, C. C., Zhang, W., Canziani, G., Robinson, J., Chaiken, I., Hoxie, J. A., Doms, R. W. (1999) Stable exposure of the coreceptor-binding site in a CD4-independent HIV-1 envelope protein. Proc. Natl. Acad. Sci. USA 96, 6359-6364.
69. Kolchinsky, P., Mirzabekov, T., Farzan, M., Kiprilov, E., Cayabyab, M., Mooney, L. J., Choe, H., Sodroski, J. (1999) Adaptation of a CCR5-using, primary human immunodeficiency virus type 1 isolate for CD4-independent replication. J. Virol. 73, 8120-8126.
70. LaBranche, C. C., Hoffman, T. L., Romano, J., Haggarty, B. S., Edwards, T. G., Matthews, T. J., Doms, R. W., Hoxie, J. A. (1999) Determinants of CD4 independence for a human immunodeficiency virus type 1 variant map outside regions required for coreceptor specificity. J. Virol. 73, 10310-10319.
71. Edwards, T. G., Hoffman, T. L., Baribaud, F., Wyss, S., LaBranche, C. C., Romano, J., Adkinson, J., Sharron, M., Hoxie, J. A., Doms, R. W. (2001) Relationships between CD4 independence, neutralization sensitivity, and exposure of a CD4-induced epitope in a human immunodeficiency virus type 1 envelope protein. J. Virol. 75, 5230-5239.
72. Kolchinsky, P., Kiprilov, E., Sodroski, J. (2001) Increased neutralization sensitivity of CD4-independent human immunodeficiency virus variants. J. Virol. 75, 2041-2050.
73. Poulin, L., Evans, L. A., Tang, S. B., Barboza, A., Legg, H., Littman, D. R., Levy, J. A. (1991) Several CD4 domains can play a role in human immunodeficiency virus infection in cells. J. Virol. 65, 4893-4901.
74. Berger, E. A., Doms, R. W., Fenyo, E. M., Korber, B. T., Littman, D. R., Moore, J. P., Sattentau, Q. J., Schuitemaker, H., Sodroski, J., Weiss, R. A. (1998) A new classification for HIV-1. Nature 391, 240.
75. Dean, M., Carrington, M., Winkler, C., Huttley, G. A., Smith, M. W., Allikmets, R., Goedert, J. J., Buchbinder, S. P., Vittinghoff, E., Gomperts, E., et al. (1996) Genetic restriction of HIV-1 infection and progression to AIDS by a deletion allele of the CKR5 structural gene. Hemophilia Growth and Development Study, Multicenter AIDS Cohort Study, Multicenter Hemophilia Cohort Study, San Francisco City Cohort, ALIVE Study. Science 273, 1856-1862.
76. Huang, Y., Paxton, W. A., Wolinsky, S. M., Neumann, A. U., Zhang, L., He, T., Kang, S., Ceradini, D., Jin, Z., Yazdanbakhsh, K., et al. (1996) The role of a mutant CCR5 allele in HIV-1 transmission and disease progression. Nat. Med. 2, 1240-1243.
77. Liu, R., Paxton, W. A., Choe, S., Ceradini, D., Martin, S. R., Horuk, R., MacDonald, M. E., Stuhlmann, H., Koup, R. A., Landau, N. R. (1996) Homozygous defect in HIV-1 coreceptor accounts for resistance of some mutiply-exposed to HIV-1 infection. Cell 86, 367-377.
78. Samson, M., Libert, F., Doranz, B. J., Rucker, J., Liesnard, C., Farber, C. M., Saragosti, S., Lapoumeroulie, C., Cognaux, J., Forceille, C., et al. (1996) Resistance to HIV-1 infection in caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene. Nature 382, 722-725.
79. Eugen-Olsen, J., Iversen, A. K., Garred, P., Koppelhus, U., Pedersen, C., Benfield, T. L., Sorensen, A. M., Katzenstein, T., Dickmeiss, E., Gersloft, J., et al. (1997) Heterozygosity for a deletion in the CKR-5 gene leads to prolonged AIDS-free survival and slower CD4 T-cell decline in a cohort of HIV-seropositive individuals. AIDS 11, 305-310.
80. Zlotnik, A., Yoshie, O. (2000) Chemokines: a new classification system and their role in immunity. Immunity 12, 121-127.
81. + T cells. Science 270, 1811-1815.
82. + T cells are associated with asymptomatic HIV-1 infection. Proc. Natl. Acad. Sci. USA 97, 13812-13817.
83. + lymphocytes correlates with host genotype and rates of human immunodeficiency virus type 1 disease progression. J. Infect. Dis. 183, 1678-1681.
84. Zagury, D., Lachgar, A., Chams, V., Fall, L. S., Bernard, J., Zagury, J. F., Bizzini, B., Gringeri, A., Santagostino, E., Rappaport, J., et al. (1998) C-C chemokines, pivotal in protection against HIV type 1 infection. Proc. Natl. Acad. Sci. USA 95, 3857-3861.
85. + cell count in human immunodeficiency virus type 1-infected individuals. AIDS Res. Hum. Retroviruses 15, 1063-1071.
86. Soriano, A., Martinez, C., Garcia, F., Plana, M., Palou, E., Lejeune, M., Arostegui, J. I., De Lazzari, E., Rodriguez, C., Barrasa, A., et al. (2002) Plasma stromal cell-derived factor (SDF)-1 levels, SDF1-3′A genotype, and expression of CXCR4 on T lymphocytes: their impact on resistance to human immunodeficiency virus type 1 infection and its progression. J. Infect. Dis. 186, 922-931.
87. Simmons, G., Clapham, P. R., Picard, L., Offord, R. E., Rosenkilde, M. M., Schwartz, T. W., Buser, R., Wells, T. N., Proudfoot, A. E. (1997) Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist. Science 276, 276-279.
88. Menten, P., Struyf, S., Schutyser, E., Wuyts, A., De Clercq, E., Schols, D., Proost, P., Van Damme, J. (1999) The LD78β isoform of MIP-1α is the most potent CCR5 agonist and HIV-1-inhibiting chemokine. J. Clin. Invest. 104, R1-R5.
89. Nibbs, R. J., Yang, J., Landau, N. R., Mao, J. H., Graham, G. J. (1999) LD78β, a non-allelic variant of human MIP-1α (LD78α), has enhanced receptor interactions and potent HIV suppressive activity. J. Biol. Chem. 274, 17478-17483.
90. Xin, X., Shioda, T., Kato, A., Liu, H., Sakai, Y., Nagai, Y. (1999) Enhanced anti-HIV-1 activity of CC-chemokine LD78β, a non-allelic variant of MIP-1α/LD78α. FEBS Lett. 457, 219-222.
91. Aquaro, S., Menten, P., Struyf, S., Proost, P., Van Damme, J., De Clercq, E., Schols, D. (2001) The LD78β isoform of MIP-1α is the most potent CC-chemokine in inhibiting CCR5-dependent human immunodeficiency virus type 1 replication in human macrophages. J. Virol. 75, 4402-4406.
92. Townson, J. R., Graham, G. J., Landau, N. R., Rasala, B., Nibbs, R. J. (2000) Aminooxypentane addition to the chemokine macrophage inflammatory protein-1αP increases receptor affinities and HIV inhibition. J. Biol. Chem. 275, 39254-39261.
93. Baba, M., Nishimura, O., Kanzaki, N., Okamoto, M., Sawada, H., Iizawa, Y., Shiraishi, M., Aramaki, Y., Okonogi, K., Ogawa, Y., et al. (1999) A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. Proc. Natl. Acad. Sci. USA 96, 5698-5703.
94. Strizki, J. M., Xu, S., Wagner, N. E., Wojcik L., Liu, J., Hou, Y., Endres, M., Palani, A., Shapiro, S., Clader, J. W., et al. (2001) SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo. Proc. Natl. Acad. Sci. USA 98, 12718-12723.
95. Aquaro, S., Hatse, S., Princen, K., Perno, C. F., De Clercq, E., Caliò, R., Schols, D. (2002) Potent anti-HIV-1 activity of TAK-779 in human primary macrophages. From: 5th International Workshop on HIV Cells of Macrophage/Dendritic Lineage and Other Reservoirs; October 13-15, 2002; Rome, ITALY.
96. De Clercq, E., Yamamoto, N., Pauwels R., Baba, M., Schols, D., Nakashima, H., Balzarini, J., Debyser, Z., Murrer, B. A., Schwartz, D. (1992) Potent and selective inhibition of human Immunodeficiency virus (HIV)-1 and HIV-2 replication by a class of bicyclams interacting with a viral uncoating event. Proc. Natl. Acad. Sci. USA 89, 5286-5290.
97. De Clercq, E., Yamamotu, N., Pauwels, R., Balzarini, J., Witvrouw, M., De Vreese, K., Debyser, Z., Rosenwirth, B., Peichl, P., Datema, R. (1994) Highly potent and selective inhibitiou of human immunodeficiency virus by the bicyclam derivative JM3100. Antimicrob. Agents Chemother. 38, 668-674.
98. Schols, D., Este, J. A., Henson, G., De Clercq, E. (1997) Bicyclams, a class of potent anti-HIV agents, are targeted at the HIV coreceptor fusin/CXCR-4. Antiviral Res. 35, 147-156.
99. Schols, D., Struyf, S., Van Damme, J., Este, J. A., Henson, G., De Clercq, E. (1997) Inhibition of T-tropie HIV strains by selective antagonization of the chemokine receptor CXCR4. J. Exp. Med. 186, 1383-1388.
100. Donzella, G. A., Schols, D., Lin, S. W., Este, J. A., Nagashima, K. A., Maddon, P. J., Allaway, G. P., Sakmar, T. P., Henson, G., De Clercq, E., et al. (1998) AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor. Nat. Med. 4, 72-77.
101. Simmons, C., Reeves, J. D., McKnight, A., Dejucq, N., Hibbitts, S., Power, C. A., Aarons, E., Schols, D., De Clercq, E., Proudfoot, A. E., et al. (1998) CXCR4 as a functional coreceptor for human immunodeficiency virus type 1 infection of primary macrophages. J. Virol. 72, 8453-8457.
102. Yi, Y., Isaacs, S. N., Williams, D. A., Frank, I., Schols, D., De Clercq, E., Kolson, D. L., Collman, R. G. (1999) Role of CXCR4 in cell-cell fusion and infection of monocyte-derived macrophages by primary human immunodeficiency virus type 1 (HIV-1) strains: two distinct mechanisms of HIV-1 dual tropism. J. Virol. 73, 7117-7125.
103. De Clercq, E. (2000) Inhibition of HIV infection by bicyclams, highly potent and specific CXCR4 antagonists. Mol. Pharmacol. 57, 833-839.
104. Schols, D., Claes, S., Hatse, S., Princen, K., Vermeire, K., De Clercq, E., Skerlj, R., Bridger, G., Calandra, G. (2003) Anti-HIV activity profile of AMD070, an orally bioavailable CXCR4 antagonist. From: 16th International Conference on Antiviral Research; April 27-May 1, 2003; Savannah, GA, USA.
105. Chen, R. Y., Kilby, J. M., Saag, M. S. (2002) Enfuvirtide. Expert Opin. Investig. Drugs 11, 1837-1843.
106. Cooley, L. A., Lewin, S. R. (2003) HIV-1 cell entry and advances in viral entry inhibitor therapy. J. Clin. Virol. 26, 121-132.
107. Lalezari, J. P., Henry, K., O'Hearn, M., Montaner, J. S., Piliero, P. J., Trottier, B., Walmsley, S., Cohen, C., Kuritzkes, D. R., Eron, J. J., Jr., et al. (2003) Enfuvirtide, an HIV-1 fusion inhibitor, for drug-resistant HIV infection in North and South America. N. Engl. J. Med. 348, 2175-2185.
108. Lazzarin, A., Clotet, B., Cooper, D., Reynes, J., Arastéh, K., Nelson, M., Katlama, C., Stellbrink, H. J., Delfraissy, J. F., Lange, J., et al. (2003) Efficacy of enfuvirtide in patients infected with drug-resistant HIV-1 in Europe and Australia. N. Engl. J. Med. 348, 2186-2195.
109. Tremblay, C. L., Kollmann, C., Giguel, F., Chou, T. C., Hirsch, M. S. (2000) Strong in vitro synergy between the fusion inhibitor T-20 and the CXCR4 blocker AMD-3100. J. Acquir. Immune Defic. Syndr. 25, 99-102.
110. Reynes, J., Rouzier, R., Kanouni, T., Baillat, V., Baroudy, B., Keung, A., Hogan, C., Markowitz, M., Laughlin, M. (2002) SCH C: Safety and antiviral effects of a CCR5 receptor antagonist in HIV-1 infected subjects. From: 9th Conference on Retroviruses and Opportunistic Infections; February 24-28, 2002; Seattle, WA, USA.
111. Schols, D., Claes, S., De Clercq, E., Hendrix, C., Bridger, G., Calandra, G., Henson, G. W., Fransen, S., Huang, W., Whitcomb, J. M., et al. AMD-3100 HIV study group (2002) AMD-3100, a CXCR4 antagonist, reduced HIV viral load and X4 virus levels in humans. From: 9th Conference on Retroviruses and Opportunistic Infections; February 24-28, 2002; Seattle, WA, USA.
112. De Vreese, K., Kofler-Mongold, V., Leutgeb, C., Weber, V., Vermeire, K., Schacht, S., Anné, J., De Clercq, E., Datema, R., Werner, G. (1996) The molecular target of bicyclams, potent inhibitors of human immunodeficiency virus replication. J. Virol. 70, 689-696.
113. Trkola, A., Kuhmann, S. E., Strizki, J. M., Maxwell, E., Ketas, T., Morgan, T., Pugach, P., Xu, S., Wojcik, L., Tagat, J., et al. (2002) HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use. Proc. Natl. Acad. Sci. USA 99, 395-400.