Targeting HIV Attachment and Entry for Therapy

Advances in Pharmacology

Volumn 56, Issue , 2008, Pages 93-120

  Strizki, Julie ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; HUMAN IMMUNODEFICIENCY VIRUS FUSION INHIBITOR; VIRUS RECEPTOR;

ANIMAL; DRUG EFFECT; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; REVIEW; VIROLOGY; VIRUS ATTACHMENT; VIRUS ENTRY;

ANIMALS; ANTI-HIV AGENTS; HIV; HIV FUSION INHIBITORS; HIV INFECTIONS; HUMANS; RECEPTORS, HIV; VIRUS ATTACHMENT; VIRUS INTERNALIZATION;

EID: 37249090226     PISSN: 10543589     EISSN: None     Source Type: Book Series    
DOI: 10.1016/S1054-3589(07)56004-7     Document Type: Review

References (129)

1. Alkhatib G., Combadiere C., Broder C.C., Feng Y., Kennedy P.E., Murphy P.M., and Berger E.A. CC CKR5: A RANTES, MIP-1alpha, MIP-1beta receptor as a fusion cofactor for macrophage-tropic HIV-1. Science 272 (1996) 1955-1958
2. 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., and McDougal J.S. Expression and characterization of CD4-IgG2, a novel heterotetramer that neutralizes primary HIV type 1 isolates. AIDS Res. Hum. Retroviruses 11 (1995) 533-539
3. Baba M., Nishimura O., Kanzaki N., Okamoto M., Sawada H., Iizawa Y., Shiraishi M., Aramaki Y., Okonogi K., Ogawa Y., Meguro K., and Fujino M. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. Proc. Natl. Acad. Sci. USA 96 (1999) 5698-5703
4. Baba M., Miyake H., Wang X., Okamoto M., and Takashima K. Isolation and characterization of human immunodeficiency virus type 1 resistant to the small-molecule CCR5 antagonist TAK-652. Antimicrob. Agents Chemother. 51 (2007) 707-715
5. Bleul C.C., Farzan M., Choe H., Parolin C., Clark-Lewis I., Sodroski J., and Springer T.A. The lymphocyte chemoattractant SDF-1 is a ligand for LESTR/fusin and blocks HIV-1 entry. Nature 382 (1996) 829-833
6. 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., Currens M.J., Cardellina J.H., et al. 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 (1997) 1521-1530
7. 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., et al. Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist. J. Exp. Med. 201 (2005) 1307-1318
8. Burkly L., Olson D., Shapiro R., Winkler G., Rosa J., Thomas D., Williams C., and Chisholm P. Inhibition of HIV infection by a novel CD4 domain 2-specific monoclonal antibody. Dissecting the basis for its inhibitory effect on HIV-induced cell fusion. J. Immunol. 149 (1992) 1779-1787
9. Butler I.F., Pandrea I., Marx P.A., and Apetrei C. HIV genetic diversity: Biological and public health consequences. Curr. HIV Res. 5 (2007) 23-45
10. Cashen A.F., Nervi B., and DiPersio J. AMD3100: CXCR4 antagonist and rapid stem cell-mobilizing agent. Future Oncol. 3 (2007) 19-27
11. Chan D.C., Fass D., Berger J.M., and Kim P.S. Core structure of gp41 from the HIV envelope glycoprotein. Cell 89 (1997) 263-273
12. Chan D.C., Chutkowski C.T., and Kim P.S. Evidence that a prominent cavity in the coiled coil of HIV type 1 gp41 is an attractive drug target. Proc. Natl. Acad. Sci. USA 95 (1998) 15613-15617
13. Chen B., Vogan E.M., Gong H., Skehel J.J., Wiley D.C., and Harrison S.C. Structure of an unliganded simian immunodeficiency virus gp120 core. Nature 433 (2005) 834-841
14. Clapham P.R., Weber J.N., Whitby D., McIntosh K., Dalgleish A.G., Maddon P.J., Deen K.C., Sweet R.W., and Weiss R.A. 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 (1989) 368-370
15. Cocchi F., DeVico A.L., Garzino-Demo A., Arya S.K., Gallo R.C., and Lusso P. Identification of RANTES, MIP-1 alpha, and MIP-1 beta as the major HIV-suppressive factors produced by CD8+ T cells. Science 270 (1995) 1811-1815
16. Cole A.L., Herasimtschuk A., Gupta P., Waring A.J., Lehrer R.I., and Cole A.M. The retrocyclin analogue RC-101 prevents human immunodeficiency virus type 1 infection of a model human cervicovaginal tissue construct. Immunology 121 (2007) 140-145
17. Connor R.I., Sheridan K.E., Ceradini D., Choe S., and Landau N.R. Change in coreceptor use coreceptor use correlates with disease progression in HIV-1-infected individuals. J. Exp. Med. 185 (1997) 621-628
18. Dean M., Carrington M., Winkler C., Huttley G.A., Smith M.W., Allikmets R., Goedert J.J., Buchbinder S.P., Vittinghoff E., Gomperts E., Donfield S., Vlahov D., et al. 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 (1996) 1856-1862
19. Deen K.C., McDougal J.S., Inacker R., Folena-Wasserman G., Arthos J., Rosenberg J., Maddon P.J., Axel R., and Sweet R.W. A soluble form of CD4 (T4) protein inhibits AIDS virus infection. Nature 331 (1988) 82-84
20. Delezay O., Koch N., Yahi N., Hammache D., Tourres C., Tamalet C., and Fantini J. Co-expression of CXCR4/fusin and galactosylceramide in the human intestinal epithelial cell line HT-29. AIDS 11 (1997) 1311-1318
21. Deng H., Liu R., Ellmeier W., Choe S., Unutmaz D., Burkhart M., Di Marzio P., Marmon S., Sutton R.E., Hill C.M., Davis C.B., Peiper S.C., et al. Identification of a major co-receptor for primary isolates of HIV-1. Nature 381 (1996) 661-666
22. Devine S.M., Flomenberg N., Vesole D.H., Liesveld J., Weisdorf D., Badel K., Calandra G., and DiPersio J.F. Rapid mobilization of CD34+ cells following administration of the CXCR4 antagonist AMD3100 to patients with multiple myeloma and non-Hodgkin's lymphoma. J. Clin. Oncol. 22 (2004) 1095-1102
23. Dey B., Lerner D.L., Lusso P., Boyd M.R., Elder J.H., and Berger E.A. 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 (2000) 4562-4569
24. Doms R.W. Chemokine receptors and HIV entry. AIDS 15 Suppl. 1 (2001) S34-S35
25. Doms R.W., and Moore J.P. HIV-1 membrane fusion: Targets of opportunity. J. Cell Biol. 151 (2000) F9-F14
26. Doncel G. "14th Conference on Retroviruses and Opportunistic Infections." Los Angeles, CA (2007) Abstract 106LB
27. Doranz B.J., Filion L.G., Diaz-Mitoma F., Sitar D.S., Sahai J., Baribaud F., Orsini M.J., Benovic J.L., Cameron W., and Doms R.W. Safe use of the CXCR4 inhibitor ALX40-4C in humans. AIDS Res. Hum. Retroviruses 17 (2001) 475-486
28. Dorr P., Westby M., Dobbs S., Griffin P., Irvine B., Macartney M., Mori J., Rickett G., Smith-Burchnell C., Napier C., Webster R., Armour D., et al. Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity. Antimicrob. Agents Chemother. 49 (2005) 4721-4732
29. Dragic T., Litwin V., Allaway G.P., Martin S.R., Huang Y., Nagashima K.A., Cayanan C., Maddon P.J., Koup R.A., Moore J.P., and Paxton W.A. HIV-1 entry into CD4+ cells is mediated by the chemokine receptor CC-CKR-5. Nature 381 (1996) 667-673
30. Dragic T., Trkola A., Thompson D.A., Cormier E.G., Kajumo F.A., Maxwell E., Lin S.W., Ying W., Smith S.O., Sakmar T.P., and Moore J.P. A binding pocket for a small molecule inhibitor of HIV-1 entry within the transmembrane helices of CCR5. Proc. Natl. Acad. Sci. USA 97 (2000) 5639-5644
31. Fatkenheuer G., Pozniak A.L., Johnson M.A., Plettenberg A., Staszewski S., Hoepelman A.I.M., Saag M.S., Goebel F.D., Rockstroh J.K., Dezube B.J., Jenkins T.M., Medhurst C., et al. Efficacy of short-term monotherapy with maraviroc, a new CCR5 antagonist, in patients infected with HIV-1. Nat. Med. 11 (2005) 1170-1172
32. Feil C., and Augustin H.G. Endothelial cells differentially express functional CXC-chemokine receptor-4 (CXCR-4/fusin) under the control of autocrine activity and exogenous cytokines. Biochem. Biophys. Res. Commun. 247 (1998) 38-45
33. Feng Y., Broder C.C., Kennedy P.E., and Berger E.A. HIV-1 entry cofactor: Functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor. Science 272 (1996) 872-877
34. Feng Y., Leavitt M., Tritz R., Duarte E., Kang D., Mamounas M., Gilles P., Wong-Staal F., Kennedy S., Merson J., Yu M., and Barber J.R. Inhibition of CCR5-dependent HIV-1 infection by hairpin ribozyme gene therapy against CC-chemokine receptor 5. Virology 276 (2000) 271-278
35. Frey G., Rits-Volloch S., Zhang X.-Q., Schooley R.T., Chen B., and Harrison S.C. Small molecules that bind the inner core of gp41 and inhibit HIV envelope-mediated fusion. Proc. Natl. Acad. Sci. USA 103 (2006) 13938-13943
36. Frost S.D.W., Wrin T., Smith D.M., Pond S.L.K., Liu Y., Paxinos E., Chappey C., Galovich J., Beauchaine J., Petropoulos C.J., Little S.J., and Richman D.D. Neutralizing antibody responses drive the evolution of human immunodeficiency virus type 1 envelope during recent HIV infection. Proc. Natl. Acad. Sci. USA 102 (2005) 18514-18519
37. Greenberg M.L., and Cammack N. Resistance to enfuvirtide, the first HIV fusion inhibitor. J. Antimicrob. Chemother. 54 (2004) 333-340
38. Guo Q., Ho H.-T., Dicker I., Fan L., Zhou N., Friborg J., Wang T., McAuliffe B.V., Wang H.-G.H., Rose R.E., Fang H., Scarnati H.T., et al. Biochemical and genetic characterizations of a novel human immunodeficiency virus type 1 inhibitor that blocks gp120-CD4 interactions. J. Virol. 77 (2003) 10528-10536
39. Hartley O., Gaertner H., Wilken J., Thompson D., Fish R., Ramos A., Pastore C., Dufour B., Cerini F., Melotti A., Heveker N., Picard L., et al. Medicinal chemistry applied to a synthetic protein: Development of highly potent HIV entry inhibitors. Proc. Natl. Acad. Sci. USA 101 (2004) 16460-16465
40. Hendrix C.W., Flexner C., MacFarland R.T., Giandomenico C., Fuchs E.J., Redpath E., Bridger G., and Henson G.W. Pharmacokinetics and safety of AMD-3100, a novel antagonist of the CXCR-4 chemokine receptor, in human volunteers. Antimicrob. Agents Chemother. 44 (2000) 1667-1673
41. Hendrix C.W., Collier A.C., Lederman M.M., Schols D., Pollard R.B., Brown S., Jackson J.B., Coombs R.W., Glesby M.J., Flexner C.W., Bridger G.J., Badel K., et al. Safety, pharmacokinetics, and antiviral activity of AMD3100, a selective CXCR4 receptor inhibitor, in HIV-1 infection. J. Acquir. Immune Defic. Syndr. 37 (2004) 1253-1262
42. Hillier S.L., Moench T., Shattock R., Black R., Reichelderfer P., and Veronese F. In vitro and in vivo: The story of nonoxynol 9. J. Acquir. Immune Defic. Syndr. 39 (2005) 1-8
43. Huang C.C., Tang M., Zhang M.Y., Majeed S., Montabana E., Stanfield R.L., Dimitrov D.S., Korber B., Sodroski J., Wilson I.A., Wyatt R., and Kwong P.D. Structure of a V3-containing HIV-1 gp120 core. Science 310 (2005) 1025-1028
44. Jacobson J.M., Israel R.J., Lowy I., Ostrow N.A., Vassilatos L.S., Barish M., Tran D.N.H., Sullivan B.M., Ketas T.J., O'Neill T.J., Nagashima K.A., Huang W., et al. Treatment of advanced human immunodeficiency virus type 1 disease with the viral entry inhibitor PRO 542. Antimicrob. Agents Chemother. 48 (2004) 423-429
45. Kadow J., Wang H.G., and Lin P.F. Small-molecule HIV-1 gp120 inhibitors to prevent HIV-1 entry: An emerging opportunity for drug development. Curr. Opin. Investig. Drugs 7 (2006) 721-726
46. Kahn J.O., Allan J.D., Hodges T.L., Kaplan L.D., Arri C.J., Fitch H.F., Izu A.E., Mordenti J., Sherwin J.E., and Groopman J.E. The safety and pharmacokinetics of recombinant soluble CD4 (rCD4) in subjects with the acquired immunodeficiency syndrome (AIDS) and AIDS-related complex. A phase 1 study. Ann. Intern. Med. 112 (1990) 254-261
47. Keller M.J., Zerhouni-Layachi B., Cheshenko N., John M., Hogarty K., Kasowitz A., Goldberg C.L., Wallenstein S., Profy A.T., Klotman M.E., and Herold B.C. PRO 2000 Gel inhibits HIV and herpes simplex virus infection following vaginal application: A double-blind placebo-controlled trial. J. Infect. Dis. 193 (2006) 27-35
48. Kilby J.M., Hopkins S., Venetta T.M., DiMassimo B., Cloud G.A., Lee J.Y., Alldredge L., Hunter E., Lambert D., Bolognesi D., Matthews T., Johnson M.R., et al. Potent suppression of HIV-1 replication in humans by T-20, a peptide inhibitor of gp41-mediated virus entry. Nat. Med. 4 (1998) 1302-1307
49. Klasse P.J. What is the role for entry inhibitors in microbicides for blocking transmission of HIV-1 via the cervico-vaginal or rectal musosa?. J. Viral Entry 2 (2006) 67-72
50. Klatzmann D.R., McDougal J.S., and Maddon P.J. The CD4 molecule and HIV infection. Immunodefic. Rev. 2 (1990) 43-66
51. Kong R., Tan J.J., Ma X.H., Chen W.Z., and Wang C.X. Prediction of the binding mode between BMS-378806 and HIV-1 gp120 by docking and molecular dynamics simulation. Biochim. Biophy. Acta (BBA) - Proteins and Proteomics 1764 (2006) 766-772
52. Kwong P.D., Wyatt R., Robinson J., Sweet R.W., Sodroski J., and Hendrickson W.A. Structure of an HIV gp120 envelope glycoprotein in complex with the CD4 receptor and a neutralizing human antibody. Nature 393 (1998) 648-659
53. Lalezari J., Thompson M., Kumar P., Piliero P., Davey R., Patterson K., Shachoy-Clark A., Adkison K., Demarest J., Lou Y., Berrey M., and Piscitelli S. Antiviral activity and safety of 873140, a novel CCR5 antagonist, during short-term monotherapy in HIV-infected adults. AIDS 19 (2005) 1443-1448
54. Lalezari J., Lewis S., Subramanian G.M., Krawiec R., and Delmedico M.K. Parenteral inhibitors of HIV entry in current development. J. Viral Entry 2 (2006) 48-56
55. Lalezari J., Goodrich J., DeJesus E., Lampiris H., Gulick R., Saag M., Ridgway C., McHale M., van der Ryst E., and Mayer H. Efficacy and safety of maraviroc plus optimized background therapy in viremic, ART-experienced patients infected with CCR5-tropic HIV-1: 24-week results of a Phase 2b/3 Study in the US and Canada. "14th Conference on Retroviruses and Opportunistic Infections." Feb. 25-28, Los Angeles, CA (2007) Abstract 104bLB
56. Lavi E., Strizki J.M., Ulrich A.M., Zhang W., Fu L., Wang Q., O'Connor M., Hoxie J.A., and Gonzalez-Scarano F. CXCR-4 (Fusin), a coreceptor for the type 1 human immunodeficiency virus (HIV-1), is expressed in the human brain in a variety of cell types, including microglia and neurons. Am. J. Pathol. 151 (1997) 1035-1042
57. Lederman M.M., Veazey R.S., Offord R., Mosier D.E., Dufour J., Mefford M., Piatak Jr. M., Lifson J.D., Salkowitz J.R., Rodriguez B., Blauvelt A., and Hartley O. Prevention of vaginal SHIV transmission in rhesus macaques through inhibition of CCR5. Science 306 (2004) 485-487
58. Lederman M.M., Offord R.E., and Hartley O. Microbicides and other topical strategies to prevent vaginal transmission of HIV. Nat. Rev. Immunol. 6 (2006) 371-382
59. Liao Z., Cimakasky L.M., Hampton R., Nguyen D.H., and Hildreth J.E.K. Lipid rafts and HIV pathogenesis: Host membrane cholesterol is required for infection by HIV type 1. AIDS Res. Hum. Retroviruses 17 (2001) 1009-1019
60. Liao Z., Graham D.R., and Hildreth J.E.K. Lipid rafts and HIV pathogenesis: Virion-associated cholesterol is required for fusion and infection of susceptible cells. AIDS Res. Hum. Retroviruses 19 (2003) 675-687
61. Lin P.-F., Robinson B., Gong Y.-F., Ricarrdi K., Guo Q., Deminie C., Rose R., Wang T., Meanwell N., Yang Z., Wang H., Zhang T., et al. Identification and characterization of a novel inhibitor or HIV Entry-I: Virology and resistance. 9th Conference on Retroviruses and Opportunistic Infections Feb. 24-28, Seattle, WA (2002) Abstract 9
62. Lin P.-F., Blair W., Wang T., Spicer T., Guo Q., Zhou N., Gong Y.-F., Wang H.-G.H., Rose R., Yamanaka G., Robinson B., Li C.-B., et al. A small molecule HIV-1 inhibitor that targets the HIV-1 envelope and inhibits CD4 receptor binding. Proc. Natl. Acad. Sci. USA 100 (2003) 11013-11018
63. Liu R., Paxton W.A., Choe S., Ceradini D., Martin S.R., Horuk R., MacDonald M.E., Stuhlmann H., Koup R.A., and Landau N.R. Homozygous defect in HIV-1 coreceptor accounts for resistance of some multiply-exposed individuals to HIV-1 infection. Cell 86 (1996) 367-377
64. Liu X., Lagenaur L.A., Simpson D.A., Essenmacher K.P., Frazier-Parker C.L., Liu Y., Tsai D., Rao S.S., Hamer D.H., Parks T.P., Lee P.P., and Xu Q. Engineered vaginal lactobacillus strain for mucosal delivery of the human immunodeficiency virus inhibitor cyanovirin-N. Antimicrob. Agents Chemother. 50 (2006) 3250-3259
65. Loutfy M.R., Raboud J.M., Montaner J.S., Antoniou T., Wynhoven B., Smaill F., Rouleau D., Gill J., Schlech W., Brumme Z.L., Mo T., Gough K., et al. Assay of HIV gp41 amino acid sequence to identify baseline variation and mutation development in patients with virologic failure on enfuvirtide. Antiviral Res. 75 (2006) 58-63
66. Ma Q., Jones D., Borghesani P.R., Segal R.A., Nagasawa T., Kishimoto T., Bronson R.T., and Springer T.A. Impaired B-lymphopoiesis, myelopoiesis, and derailed cerebellar neuron migration in CXCR4- and SDF-1-deficient mice. Proc. Natl. Acad. Sci. USA 95 (1998) 9448-9453
67. Mack M., Luckow B., Nelson P.J., Cihak J., Simmons G., Clapham P.R., Signoret N., Marsh M., Stangassinger M., Borlat F., Wells T.N., Schlondorff D., et al. Aminooxypentane-RANTES induces CCR5 internalization but inhibits recycling: A novel inhibitory mechanism of HIV infectivity. J. Exp. Med. 187 (1998) 1215-1224
68. Madani N., Perdigoto A.L., Srinivasan K., Cox J.M., Chruma J.J., LaLonde J., Head M., Smith III A.B., and Sodroski J.G. Localized changes in the gp120 envelope glycoprotein confer resistance to human immunodeficiency virus entry inhibitors BMS-806 and #155. J. Virol. 78 (2004) 3742-3752
69. Maeda K., Nakata H., Koh Y., Miyakawa T., Ogata H., Takaoka Y., Shibayama S., Sagawa K., Fukushima D., Moravek J., Koyanagi Y., and Mitsuya H. Spirodiketopiperazine-based CCR5 inhibitor which preserves CC-chemokine/CCR5 interactions and exerts potent activity against R5 human immunodeficiency virus type 1 in vitro. J. Virol. 78 (2004) 8654-8662
70. Maeda K., Nakata H., Ogata H., Koh Y., Miyakawa T., and Mitsuya H. The current status of, and challenges in, the development of CCR5 inhibitors as therapeutics for HIV-1 infection. Curr. Opin. Pharmacol. 4 (2004) 447-452
71. Maeda K., Das D., Ogata-Aoki H., Nakata H., Miyakawa T., Tojo Y., Norman R., Takaoka Y., Ding J., Arnold G.F., Arnold E., and Mitsuya H. Structural and molecular interactions of CCR5 inhibitors with CCR5. J. Biol. Chem. 281 (2006) 12688-12698
72. Markovic I., and Clouse K.A. Recent advances in understanding the molecular mechanisms of HIV-1 entry and fusion: Revisiting current targets and considering new options for therapeutic intervention. Curr. HIV Res. 2 (2004) 223-234
73. Marozsan A.J., Kuhmann S.E., Morgan T., Herrera C., Rivera-Troche E., Xu S., Baroudy B.M., Strizki J., and Moore J.P. Generation and properties of a human immunodeficiency virus type 1 isolate resistant to the small molecule CCR5 inhibitor, SCH-417690 (SCH-D). Virology 338 (2005) 182-199
74. McKnight A., Wilkinson D., Simmons G., Talbot S., Picard L., Ahuja M., Marsh M., Hoxie J., and Clapham P. Inhibition of human immunodeficiency virus fusion by a monoclonal antibody to a coreceptor (CXCR4) is both cell type and virus strain dependent. J. Virol. 71 (1997) 1692-1696
75. Moyle G., DeJesus E., Boffito M., Wong R., Coakley E., Gibney C., Badel K., Calandra G., Bridger G., and Becker S. CXCR4 antagonism: Proof of activity with AMD11070. "14th Conference on Retroviruses and Opportunistic Infections." (2007) Abstract 511
76. Moore J.P., Parren P.W.H.I., and Burton D.R. Genetic subtypes, humoral immunity, and human immunodeficiency virus type 1 vaccine development. J. Virol. 75 (2001) 5721-5729
77. Mori T., and Boyd M.R. 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 (2001) 664-672
78. Murakami T., Nakajima T., Koyanagi Y., Tachibana K., Fujii N., Tamamura H., Yoshida N., Waki M., Matsumoto A., Yoshie O., Kishimoto T., Yamamoto N., et al. A small molecule CXCR4 inhibitor that blocks T cell line-tropic HIV-1 infection. J. Exp. Med. 186 (1997) 1389-1393
79. Nelson M., Arasteh K., Clotet B., Cooper D.A., Henry K., Katlama C., Lalezari J.P., Lazzarin A., Montaner J.S., O'Hearn M., Piliero P.J., Reynes J., et al. Durable efficacy of enfuvirtide over 48 weeks in heavily treatment-experienced HIV-1-infected patients in the T-20 versus optimized background regimen only 1 and 2 clinical trials. J. Acquir. Immune Defic. Syndr. 40 (2005) 404-412
80. Nishikawa M., Takashima K., Nishi T., Furuta R.A., Kanzaki N., Yamamoto Y., and Fujisawa J.-I. Analysis of binding sites for the new small-molecule CCR5 antagonist TAK-220 on human CCR5. Antimicrob. Agents Chemother. 49 (2005) 4708-4715
81. Oberlin E., Amara A., Bachelerie F., Bessia C., Virelizier J.L., Arenzana-Seisdedos F., Schwartz O., Heard J.M., Clark-Lewis I., Legler D.F., Loetscher M., Baggiolini M., et al. The CXC chemokine SDF-1 is the ligand for LESTR/fusin and prevents infection by T-cell-line-adapted HIV-1. Nature 382 (1996) 833-835
82. Olson W.C., Rabut G.E., Nagashima K.A., Tran D.N., Anselma D.J., Monard S.P., Segal J.P., Thompson D.A., Kajumo F., Guo Y., Moore J.P., Maddon P.J., et al. Differential inhibition of human immunodeficiency virus type 1 fusion, gp120 binding, and CC-chemokine activity by monoclonal antibodies to CCR5. J. Virol. 73 (1999) 4145-4155
83. Owen S.M., Rudolph D.L., Wang W., Cole A.M., Waring A.J., Lal R.B., and Lehrer R.I. RC-101, a retrocyclin-1 analogue with enhanced activity against primary HIV type 1 isolates. AIDS Res. Hum. Retroviruses 20 (2004) 1157-1165
84. Pastore C., Picchio G.R., Galimi F., Fish R., Hartley O., Offord R.E., and Mosier D.E. Two mechanisms for human immunodeficiency virus type 1 inhibition by N-terminal modifications of RANTES. Antimicrob. Agents Chemother. 47 (2003) 509-517
85. Pastore C., Nedellec R., Ramos A., Pontow S., Ratner L., and Mosier D.E. Human immunodeficiency virus type 1 coreceptor switching: V1/V2 gain-of-fitness mutations compensate for V3 loss-of-fitness mutations. J. Virol. 80 (2006) 750-758
86. Pugach P., Marozsan A.J., Ketas T.J., Landes E.L., Moore J.P., and Kuhmann S.E. HIV-1 clones resistant to a small molecule CCR5 inhibitor use the inhibitor-bound form of CCR5 for entry. Virology 361 (2006) 212-228
87. Reeves J.D., Miamidian J.L., Biscone M.J., Lee F.-H., Ahmad N., Pierson T.C., and Doms R.W. Impact of mutations in the coreceptor binding site on human immunodeficiency virus type 1 fusion, infection, and entry inhibitor sensitivity. J. Virol. 78 (2004) 5476-5485
88. Reeves J.D., Lee F.-H., Miamidian J.L., Jabara C.B., Juntilla M.M., and Doms R.W. Enfuvirtide resistance mutations: Impact on human immunodeficiency virus envelope function, entry inhibitor sensitivity, and virus neutralization. J. Virol. 79 (2005) 4991-4999
89. Reimann K.A., Burkly L.C., Burrus B., Waite B.C., Lord C.I., and Letvin N.L. In vivo administration to rhesus monkeys of a CD4-specific monoclonal antibody capable of blocking AIDS virus replication. AIDS Res. Hum. Retroviruses 9 (1993) 199-207
90. Rizzuto C., and Sodroski J. Fine definition of a conserved CCR5-binding region on the human immunodeficiency virus type 1 glycoprotein 120. AIDS Res. Hum. Retroviruses 16 (2000) 741-749
91. Rizzuto C.D., Wyatt R., Hernandez-Ramos N., Sun Y., Kwong P.D., Hendrickson W.A., and Sodroski J. A conserved HIV gp120 glycoprotein structure involved in chemokine receptor binding. Science 280 (1998) 1949-1953
92. Sabbe R., Picchio G.R., Pastore C., Chaloin O., Hartley O., Offord R., and Mosier D.E. Donor- and ligand-dependent differences in C-C chemokine receptor 5 reexpression. J. Virol. 75 (2001) 661-671
93. Samson M., Labbe O., Mollereau C., Vassart G., and Parmentier M. Molecular cloning and functional expression of a new human CC-chemokine receptor gene. Biochemistry 35 (1996) 3362-3367
94. Schacker T., Coombs R.W., Collier A.C., Zeh J.E., Fox I., Alam J., Nelson K., Eggert E., and Corey L. The effects of high-dose recombinant soluble CD4 on human immunodeficiency virus type 1 viremia. J. Infect. Dis. 169 (1994) 37-40
95. Schols D. HIV co-receptors as targets for antiviral therapy. Curr. Top. Med. Chem. 4 (2004) 833-893
96. Schooley R.T., Merigan T.C., Gaut P., Hirsch M.S., Holodniy M., Flynn T., Liu S., Byington R.E., Henochowicz S., Gubish E., et al. 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 (1990) 247-253
97. Schurmann D., Fatkenheuer G., Reynes J., Michelet C., Raffi F., van Lier J., Caceres M., Keung A., Sansone-Parsons A., Dunkle L., and Hoffmann C. Antiviral activity, pharmacokinetics and safety of vicriviroc, an oral CCR5 antagonist, during 14-day monotherapy in HIV-infected adults. AIDS 21 10 (2007) 1293-1299
98. Schyler S., and Horuk R. I want a new drug: G-protein-coupled receptors in drug development. Drug Discov. Today 11 (2006) 481-493
99. Seibert C., Ying W., Gavrilov S., Tsamis F., Kuhmann S.E., Palani A., Tagat J.R., Clader J.W., McCombie S.W., Baroudy B.M., Smith S.O., Dragic T., et al. Interaction of small molecule inhibitors of HIV-1 entry with CCR5. Virology 349 (2006) 41-54
100. Seto M., Aikawa K., Miyamoto N., Aramaki Y., Kanzaki N., Takashima K., Kuze Y., Iizawa Y., Baba M., and Shiraishi M. Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: Synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety. J. Med. Chem. 49 (2006) 2037-2048
101. Shenoy S.R., O'Keefe B.R., Bolmstedt A.J., Cartner L.K., and Boyd M.R. Selective interactions of the human immunodeficiency virus-inactivating protein cyanovirin-N with high-mannose oligosaccharides on gp120 and other glycoproteins. J. Pharmacol. Exp. Ther. 297 (2001) 704-710
102. Si Z., Madani N., Cox J.M., Chruma J.J., Klein J.C., Schon A., Phan N., Wang L., Biorn A.C., Cocklin S., Chaiken I., Freire E., et al. Small-molecule inhibitors of HIV-1 entry block receptor-induced conformational changes in the viral envelope glycoproteins. Proc. Natl. Acad. Sci. USA 101 (2004) 5036-5041
103. Signoret N., Pelchen-Matthews A., Mack M., Proudfoot A.E., and Marsh M. Endocytosis and recycling of the HIV coreceptor CCR5. J. Cell Biol. 151 (2000) 1281-1294
104. Simmons G., Clapham P.R., Picard L., Offord R.E., Rosenkilde M.M., Schwartz T.W., Buser R., Wells T.N., and Proudfoot A.E. Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist. Science 276 (1997) 276-279
105. Sriram S., Carroll L., Fortin S., Cooper S., and Ranges G. In vivo immunomodulation by monoclonal anti-CD4 antibody. II. Effect on T cell response to myelin basic protein and experimental allergic encephalomyelitis. J. Immunol. 141 (1988) 464-468
106. Strizki J.M., Xu S., Wagner N.E., Wojcik L., Liu J., Hou Y., Endres M., Palani A., Shapiro S., Clader J.W., Greenlee W.J., Tagat J.R., et al. 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 (2001) 12718-12723
107. Strizki J.M., Tremblay C., Xu S., Wojcik L., Wagner N., Gonsiorek W., Hipkin R.W., Chou C.-C., Pugliese-Sivo C., Xiao Y., Tagat J.R., Cox K., et al. Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1. Antimicrob. Agents Chemother. 49 (2005) 4911-4919
108. Su C., Melby T., DeMasi R., Ravindran P., and Heilek-Snyder G. Genotypic changes in human immunodeficiency virus type 1 envelope glycoproteins on treatment with the fusion inhibitor enfuvirtide and their influence on changes in drug susceptibility in vitro. J. Clin. Virol. 36 (2006) 249-257
109. Tamamura H., Xu Y., Hattori T., Zhang X., Arakaki R., Kanbara K., Omagari A., Otaka A., Ibuka T., Yamamoto N., Nakashima H., and Fujii N. A low-molecular-weight inhibitor against the chemokine receptor CXCR4: A strong anti-HIV peptide T140. Biochem. Biophys. Res. Commun. 253 (1998) 877-882
110. Trkola A., Ketas T.J., Nagashima K.A., Zhao L., Cilliers T., Morris L., Moore J.P., Maddon P.J., and Olson W.C. Potent, broad-spectrum inhibition of human immunodeficiency virus type 1 by the CCR5 monoclonal antibody PRO 140. J. Virol. 75 (2001) 579-588
111. Trkola A., Kuhmann S.E., Strizki J.M., Maxwell E., Ketas T., Morgan T., Pugach P., Xu S., Wojcik L., Tagat J., Palani A., Shapiro S., et al. HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use. Proc. Natl. Acad. Sci. USA 99 (2002) 395-400
112. Trottier B., Walmsley S., Reynes J., Piliero P., O'Hearn M., Nelson M., Montaner J., Lazzarin A., Lalezari J., Katlama C., Henry K., Cooper D., et al. Safety of enfuvirtide in combination with an optimized background of antiretrovirals in treatment-experienced HIV-1-infected adults over 48 weeks. J. Acquir. Immune Defic. Syndr. 40 (2005) 413-421
113. Tsai C.-C., Emau P., Jiang Y., Agy M.B., Shattock R.J., Schmidt A., Morton W.R., Gustafson K.R., and Boyd M.R. Cyanovirin-N inhibits AIDS virus infections in vaginal transmission models. AIDS Res. Hum. Retroviruses 20 (2004) 11-18
114. Tsamis F., Gavrilov S., Kajumo F., Seibert C., Kuhmann S., Ketas T., Trkola A., Palani A., Clader J.W., Tagat J.R., McCombie S., Baroudy B., et al. Analysis of the mechanism by which the small-molecule CCR5 antagonists SCH-351125 and SCH-350581 inhibit human immunodeficiency virus type 1 entry. J. Virol. 77 (2003) 5201-5208
115. Veazey R.S., Klasse P.J., Ketas T.J., Reeves J.D., Piatak Jr. M., Kunstman K., Kuhmann S.E., Marx P.A., Lifson J.D., Dufour J., Mefford M., Pandrea I., et al. Use of a small molecule CCR5 inhibitor in macaques to treat simian immunodeficiency virus infection or prevent simian-human immunodeficiency virus infection. J. Exp. Med. 198 (2003) 1551-1562
116. Veazey R.S., Klasse P.J., Schader S.M., Hu Q., Ketas T.J., Lu M., Marx P.A., Dufour J., Colonno R.J., Shattock R.J., Springer M.S., and Moore J.P. Protection of macaques from vaginal SHIV challenge by vaginally delivered inhibitors of virus-cell fusion. Nature 438 (2005) 99-102
117. Vollmer T., Waldor M., Steinman L., and Conley F. Depletion of T-4+ lymphocytes with monoclonal antibody reactivates toxoplasmosis in the central nervous system: A model of superinfection in AIDS. J. Immunol. 138 (1987) 3737-3741
118. Wang J.-F., Liu Z.-Y., and Groopman J.E. The alpha-chemokine receptor CXCR4 is expressed on the megakaryocytic lineage from progenitor to platelets and modulates migration and adhesion. Blood 92 (1998) 756-764
119. Wang W., Cole A.M., Hong T., Waring A.J., and Lehrer R.I. Retrocyclin, an antiretroviral {theta}-defensin, is a lectin. J. Immunol. 170 (2003) 4708-4716
120. Wei X., Decker J.M., Wang S., Hui H., Kappes J.C., Wu X., Salazar-Gonzalez J.F., Salazar M.G., Kilby J.M., Saag M.S., Komarova N.L., Nowak M.A., et al. Antibody neutralization and escape by HIV-1. Nature 422 (2003) 307-312
121. Weissenhorn W., Dessen A., Harrison S.C., Skehel J.J., and Wiley D.C. Atomic structure of the ectodomain from HIV-1 gp41. Nature 387 (1997) 426-430
122. Westby M., Lewis M., Whitcomb J., Youle M., Pozniak A.L., James I.T., Jenkins T.M., Perros M., and van der Ryst E. Emergence of CXCR4-using human immunodeficiency virus type 1 (HIV-1) variants in a minority of HIV-1-infected patients following treatment with the CCR5 antagonist maraviroc is from a pretreatment CXCR4-using virus reservoir. J. Virol. 80 (2006) 4909-4920
123. Westby M., Smith-Burchnell C., Mori J., Lewis M., Mosley M., Stockdale M., Dorr P., Ciaramella G., and Perros M. Reduced maximal inhibition in phenotypic susceptibility assays indicates that viral strains resistant to the CCR5 antagonist maraviroc utilize inhibitor-bound receptor for entry. J. Virol. 81 (2007) 2359-2371
124. Wild C., Greenwell T., Shugars D., Rimsky-Clarke L., and Matthews T. The inhibitory activity of an HIV type 1 peptide correlates with its ability to interact with a leucine zipper structure. AIDS Res. Hum. Retroviruses 11 (1995) 323-325
125. Wild C.T., Shugars D.C., Greenwell T.K., McDanal C.B., and Matthews T.J. Peptides corresponding to a predictive alpha-helical domain of human immunodeficiency virus type 1 gp41 are potent inhibitors of virus infection. Proc. Natl. Acad. Sci. USA 91 (1994) 9770-9774
126. Wilkin T.J., Su Z., Kuritzkes D.R., Hughes M., Flexner C., Gross R., Coakley E., Greaves W., Godfrey C., Skolnik P.R., Timpone J., Rodriguez B., et al. HIV type 1 chemokine coreceptor use among antiretroviral-experienced patients screened for a clinical trial of a CCR5 inhibitor: AIDS clinical trial group A5211. Clin. Infect. Dis. 44 (2007) 591-595
127. Xu J., Lecanu L., Han Z., Yao Z., Greeson J., and Papadopoulos V. Inhibition of adrenal cortical steroid formation by procaine is mediated by reduction of the cAMP-induced 3-hydroxy-3-methylglutaryl-coenzyme A reductase messenger ribonucleic acid levels. J. Pharmacol. Exp. Ther. 307 (2003) 1148-1157
128. Youle M. The 16th international AIDS conference meeting report. J. Viral Entry 2 (2006) 77-92
129. Zou Y.R., Kottmann A.H., Kuroda M., Taniuchi I., and Littman D.R. Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development. Nature 393 (1998) 595-599