A small-molecule inhibitor directed against the chemokine receptor CXCR4 prevents its use as an HIV-1 coreceptor

Journal of Experimental Medicine

Volumn 186, Issue 8, 1997, Pages 1395-1400

  Doranz, Benjamin J ^a   Grovit Ferbas, Kathie ^b,c   Sharron, Matthew P ^a   Mao, Si Hua ^b,c   Goetz, Matthew Bidwell ^b,c   Daar, Eric S ^c,d   Doms, Robert W ^a   O'Brien, William A ^e,f  

^a UNIVERSITY OF PENNSYLVANIA   (United States)

^b VETERANS AFFAIRS MEDICAL CENTER   (United States)

^c UNIVERSITY OF CALIFORNIA   (United States)

^d CEDARS SINAI MEDICAL CENTER   (United States)

^e University of Texas Medical Branch School of Medicine   (United States)

^f UNIVERSITY OF TEXAS MEDICAL BRANCH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALPHA N ACETYLNONA DEXTRO ARGININE AMIDE; CALCIUM; CHEMOKINE RECEPTOR; MONOCLONAL ANTIBODY; POLYPEPTIDE; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; CONTROLLED STUDY; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; MEMBRANE FUSION; PRIORITY JOURNAL;

ANTI-HIV AGENTS; HIV INFECTIONS; HIV-1; HUMANS; LYMPHOMA, T-CELL; OLIGOPEPTIDES; PROTEIN BINDING; RECEPTORS, CXCR4; T-LYMPHOCYTES; TUMOR CELLS, CULTURED;

EID: 0030773515     PISSN: 00221007     EISSN: None     Source Type: Journal    
DOI: 10.1084/jem.186.8.1395     Document Type: Article

References (34)

1. Ho, D.D., A.U. Neumann, A.S. Perelson, W. Chen, J.M. Leonard, and M. Markowitz. 1995. Rapid turnover of plasma virions and CD4 lymphocytes in HIV-1 infection. Nature (Lond.). 373:123-126.
2. Wei, X., S.K. Ghosh, M.E. Taylor, V.A. Johnson, E.A. Emini, P. Deutsch, J.D. Lifson, S. Bonhoeffer, M.A. Nowak, B.H. Hahn, et al. 1995. Viral dynamics in human immunodeficiency virus type 1 infection. Nature (Lond.). 373:117-122.
3. Gulick, R.M., J.W. Mellors, D. Havlir, J.J. Eron, C. Gonzalez, D. McMahon, D.D. Richman, F.T. Valentine, L. Jonas, A. Meibohm et al. 1997. Treatment with indinavir, zidovudine and lamivudine in adults with human immunodeficiency virus infection and prior antiretroviral therapy. N. Engl. J. Med. 337:734-739.
4. Alkhatib, G., C. Combadiere, C.C. Broder, Y. Feng, P.E. Kennedy, P.M. Murphy, and E.A. Berger. 1996. CC CKR5: a RANTES, MIP-1α, MIP-1β receptor as a fusion cofactor for macrophage-tropic HIV-1. Science (Wash. DC). 272: 1955-1958.
5. Choe, H., M. Farzan, Y. Sun, N. Sullivan, B. Rollins, P.D. Ponath, L. Wu, C.R. Mackay, G. LaRosa, W. Newman, et al. 1996. The β-chemokine receptors CCR3 and CCR5 facilitate infection by primary HIV-1 isolates. Cell. 85:1135-1148.
6. Deng, H., K. Liu, W. Ellmeier, S. Choe, D. Unutmaz, M. Burkhart, P.D. Marzio, S. Marmon, R.E. Sutton, C.M. Hill, et al. 1996. Identification of a major co-receptor for primary isolates of HIV-1. Nature (Lond.). 381:661-666.
7. Doranz, B.J., J. Rucker, Y. Yi, R.J. Smyth, M. Samson, S.C. Peiper, M. Parmentier, R.G. Collman, and R.W. Doms. 1996. A dual-tropic primary HIV-1 isolate that uses fusin and the β-chemokme receptors CKR-5, CKR-3, and CKR-2b as fusion cofactors. Cell. 85:1 149-1158.
8. Dragic, T., V. Litwin, G.P. Allaway, S.R. Martin, Y. Huang, K.A. Nagashima, C. Cayanan, P.J. Maddon, R.A. Koup, J.P. Moore, and W.A. Paxton. 1996. HIV-1 entry into CD4+ cells is mediated by the chemokine receptor CC-CKR-5. Nature (Lond.). 381:667-673.
9. Feng, Y., C.C. Broder, P.E. Kennedy, and E.A. Berger. 1996. HIV-1 entry cofactor: functional cDNA cloning of a seven-transmembrane domain, G-protein coupled receptor. Science (Wash. DC). 272:872-877.
10. Samson, M., F. Libert, B.J. Doranz, J. Rucker, C. Liesnard, C.-M. Farber, S. Saragosti, C. Lapoumèroulie, J. Cogniaux, C. Forceille, et al. 1996. Resistance to HIV-1 infection of Caucasian individuals bearing mutant alleles of the CCR5 chemokine receptor gene. Nature (Lond.). 382:722-725.
11. Liu, R., W.A. Paxton, S. Choe, D. Ceradini, S.R. Martin, R. Horuk, M.E. MacDonald, H. Stuhlmann, R.A. Koup, and N.R. Landau. 1996. Homozygous defect in HIV-1 coreceptor accounts for resistance of some multiply-exposed individuals to HIV-1 infection. Cell. 86:367-377.
12. Dean, M., M. Carrington, C. Winkler, G.A. Huttley, M.W. Smith, R. Allikmets, J.J. Goedert, S.P. Buchbinder, E. Vittinghoff, E. Gomperts, et al. 1996. Genetic resistance of HIV-1 infection and progression to AIDS by a deletion allele of the CKR5 structural gene. Science (Wash. DC). 273:1856-1862.
13. Bleul, C.C., M. Farazan, H. Choe, C. Parolin, I. Clark-Lewis, J. Sodroski, and T.A. Springer. 1996. The lymphocyte chemoattractant SDF-1 is a ligand for LESTR/fusin and blocks HIV-1 entry. Nature (Lond.). 382:829-833.
14. Oberlin, E., A. Amara, F. Bachelerie, C. Bessia, J.-L. Virelizier, F. Arenzana-Seisdedos, O. Schwartz, J.-M. Heard, I. Clark-Lewis, D. F. Legler, et al. 1996. The CXC chemokine SDF-1 is the ligand for LESTR/fusin and prevents infection by T-cell line-adapted HIV-1. Nature (Lond.). 382:833-835.
15. Paxton, W.A., S.R. Martin, D. Tse, T.R. O'Brien, J. Skurnick, N.L. VanDevanter, N. Padian, J.F. Braun, D.P. Kotler, S.M. Wolinsky, and R.A. Koup. 1996. Relative resistance to HIV-1 infection of CD4 lymphocytes from persons who remain uninfected despite multiple high-risk sexual exposures. Nat. Med. 2:412-417.
16. Cocchi, F., A.L. DeVico, A. Garzino-Demo, S.K. Arya, R.C. Gallo, and P. Lusso. 1995. Identification of RANTES. MIP-1α, and MIP-1β as the major HIV suppressive factors produced by CD8+ T cells. Science (Wash. DC). 270:1811-1815.
17. Arenzanaseisdos, F., J.L. Virelizier, D. Rousset, I. Clark-Lewis, P. Loetscher, B. Moser, and M. Baggiolini. 1996. HIV blocked by chemokine antagonist. Nature (Lond.). 383:400.
18. Simmons, G., P.R. Clapham, L. Picard, R.E. Offord, M.M. Rosenkilde, T.W. Schwartz, R. Buser, T.N.C. Wells, and W.E.I. Proudfoot. 1997. Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist. Science (Wash. DC). 276:276-279.
19. Broder, C.C., and E.A. Berger. 1995. Fusogenic selectivity of the envelope glycoprotein is a major determinant of human immunodeficiency virus type 1 tropism for CD4+ T-cell lines vs. primary macrophages. Proc. Natl. Acad. Sci. USA. 92: 9004-9008.
20. Daar, E.S., T. Chernyavskiy, J.Q. Zhao, P. Krogstad, I.S. Chen, and J. A. Zack. 1995. Sequential determination of viral load and phenotype in human immunodeficiency virus type 1 infection. AIDS Res. Hum. Retroviruses. 11:3-9.
21. O'Brien, W.A., M. Simmer-Smith, S.-H. Mao, S. Sadeghi, J.-Q. Zhao, and I.S.Y. Chen. 1996. Anti-human immunodeficiency virus type 1 activity of an oligocationic compound mediated via gp120 V3 interactions. J. Virol. 70:2825-2831.
22. Connor, R.I., B.K. Chen, S. Choe, and N.R. Landau. 1995. Vpr is required for efficient replication of human immunodeficiency virus type-1 in mononuclear phagocytes. Virology. 206:935-944.
23. Nussbaum, O., C.C. Broder, and E.A. Berger. 1994. Fusogenic mechanisms of enveloped-virus glycoproteins analyzed by a novel recombinant vaccinia virus-based assay quantitating cell fusion-dependent reporter gene activation. J. Virol. 68:5411-5422.
24. Simmons, G., D. Wilkinson, J.D. Reeves, M.T. Ditttnan, S. Beddows, J. Weber, G. Carnegis, U. Gesselberger, P.W. Gray, R.A. Weiss, and P.R. Clapham. 1996. Primary, syncytium-inducing human immunodeficiency virus type 1 isolates are dual-tropic and most can use either Lestr or CCR5 as coreceptors for virus entry. J. Virol. 70:8355-8360.
25. Doranz, B.J., Z. Lu, J. Rucker, T. Zhang, M. Sharron, Y. Cen, Z. Wang, H. Guo, J. Du, M.A. Accavitti, et al. 1997. Two distinct CCR5 domains can mediate coreceptor usage by human immunodeficiency virus type 1. J. Virol. 71:6305-6314.
26. Lu, Z., J.F. Berson, Y. Chen, J.D. Turner, T. Zhang, M. Sharron, M.H. Jenks, Z. Wang, J. Kim, J. Rucker, et al. 1997. Evolution of HIV-1 coreceptor usage through interactions with distinct CCR5 and CXCR4 domains. Proc. Natl. Acad. Sci. USA. 94:6426-6431.
27. Atchison, R.E., J. Gosling, F.S. Monteclaro, C. Franci, L. Digilio, I.F. Charo, and M. Goldsmith. 1996. Multiple extra-cellular elements of CCR5 and HIV-1 entry: dissociation from response to chemokines. Science (Wash. DC). 274:1924-1926.
28. Bieniasz, P.D., R.A. Fridell, I. Aramori, S.S.G. Ferguson, M.G. Caron, and B.R. Cullen. 1997. HIV-1 induced cell tusion is mediated by multiple regions within both the viral envelope and the CCR-5 coreceptor. EMBO (Em. Mol. Biol. Organ.) J. 16:2599-2609.
29. Endres, M.J., P.R. Clapham, M. Marsh, M. Ahuja, J.D. Turner, A. McKnight, J.F. Thomas, B. Stoebenau-Haggarty, P.J.V.S. Choe, T.N.C. Wells, et al. 1996. CD4-independent infection by HIV-2 is mediated by fusin/CXCR4. Cell. 87: 745-765.
30. Brelot, A., N. Heveker, O. Pleskoff, N. Sol, and M. Alizon. 1997. Role of the first and third extracellular domains of CXCR-4 in human immunodeficiency virus coreceptor activity. J. Virol. 71:4744-4751.
31. Dejong, J.-J., J. Goudsmit, W. Keulen, B. Klaver, W. Krone, M. Tersmette, and A. deRonde. 1992. Human immunodeficiency virus type 1 clones chimeric for the envelope V3 domain differ in syncytium formation and replication capacity. J. Virol. 66:757-765.
32. Fouchier, R.A.M., M. Groenink, N.A. Kootstra, M. Tersmette, H.G. Huisman, F. Miedema, and H. Schuitemaker. 1992. Phenotype-associated sequence variation in the third variable domain of the human immunodeficiency virus type 1 gp120 molecule. J. Virol. 66:3183-3187.
33. Sumner-Smith, M., Y. Zheng, Y.P. Zhang, E.M. Twist, and S.C. Climie. 1995. Antiherpetic activities of N-α-acetylnona-D-arginine amide acetate. Drugs Exp. Clin. Res. 21:1-6.
34. Connor, R.I., H. Mohri, Y. Cao, and D.D. Ho. 1993. Increased viral burden and cytopathicity correlate temporally with CD4+ T-lymphocyte decline and clinical progression in human immunodeficiency virus type 1-infected individuals. J. Virol. 67:1772-1777.