HIV chemokine receptor inhibitors as novel anti-HIV drugs

Barre-Sinoussi, 1983, Isolation of a T-lymphotropic retrovirus from a patient at risk for acquired immune deficiency syndrome (AIDS), Science, 220, 868, 10.1126/science.6189183 Chermann, 1983, Isolation of a new retrovirus in a patient at risk for acquired immunodeficiency syndrome, Antibiot Chemother, 32, 48, 10.1159/000409704 Pomerantz, 2003, Twenty years of therapy for HIV-1 infection, Nat Med, 9, 867, 10.1038/nm0703-867 Hu, 1996, The emerging genetic diversity of HIV. The importance of global surveillance for diagnostics, research, and prevention, JAMA, 275, 210, 10.1001/jama.275.3.210 De Leys, 1990, Isolation and partial characterization of an unusual human immunodeficiency retrovirus from two persons of West-central African origin, J Virol, 64, 1207, 10.1128/JVI.64.3.1207-1216.1990 Erickson, 1998, Virology Weiss, 2001, Gulliver's travels in HIVland, Nature, 410, 963, 10.1038/35073632 Blankson, 2002, The challenge of viral reservoirs in HIV-1 infection, Annu Rev Med, 53, 557, 10.1146/annurev.med.53.082901.104024 Chun, 1999, Latent reservoirs of HIV: obstacles to the eradication of virus, Proc Natl Acad Sci USA, 96, 10958, 10.1073/pnas.96.20.10958 Aquaro, 2002, Macrophages and HIV infection: therapeutical approaches toward this strategic virus reservoir, Antiviral Res, 55, 209, 10.1016/S0166-3542(02)00052-9 Richman, 2001, HIV chemotherapy, Nature, 410, 995, 10.1038/35073673 Wei, 2002, Emergence of resistant human immunodeficiency virus type 1 in patients receiving fusion inhibitor (T-20) monotherapy, Antimicrob Agents Chemother, 46, 1896, 10.1128/AAC.46.6.1896-1905.2002 Doranz, 1997, Chemokine receptors as fusion cofactors for human immunodeficiency virus type 1 (HIV-1), Immunol Res, 16, 15, 10.1007/BF02786321 Feng, 1996, HIV-1 entry cofactor: functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor, Science, 272, 872, 10.1126/science.272.5263.872 Alkhatib, 1996, CC CKR5: a RANTES, MIP-1alpha, MIP-1beta receptor as a fusion cofactor for macrophage-tropic HIV-1, Science, 272, 1955, 10.1126/science.272.5270.1955 Deng, 1996, Identification of a major co-receptor for primary isolates of HIV-1, Nature, 381, 661, 10.1038/381661a0 Dragic, 1996, HIV-1 entry into CD4+ cells is mediated by the chemokine receptor CC-CKR-5, Nature, 381, 667, 10.1038/381667a0 Cocchi, 1995, Identification of RANTES, MIP-1α, and MIP-1β as the major HIV-suppressive factors produced by CD8+ T cells, Science, 270, 1811, 10.1126/science.270.5243.1811 Samson, 1996, Resistance to HIV-1 infection in caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene, Nature, 382, 722, 10.1038/382722a0 Liu, 1996, Homozygous defect in HIV-1 coreceptor accounts for resistance of some multiply-exposed individuals to HIV-1 infection, Cell, 86, 367, 10.1016/S0092-8674(00)80110-5 Dean, 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, 10.1126/science.273.5283.1856 Baggiolini, 1998, Chemokines and leukocyte traffic, Nature, 392, 565, 10.1038/33340 Murphy, 2002, International Union of Pharmacology. XXX. Update on chemokine receptor nomenclature, Pharmacol Rev, 54, 227, 10.1124/pr.54.2.227 Olson, 2002, Chemokines and chemokine receptors in leukocyte trafficking, Am J Physiol Regul Integr Comp Physiol, 283, R7, 10.1152/ajpregu.00738.2001 Lodi, 1994, High-resolution solution structure of the beta chemokine hMIP-1 beta by multidimensional NMR, Science, 263, 1762, 10.1126/science.8134838 Horuk, 1993, A receptor for the malarial parasite Plasmodium vivax: the erythrocyte chemokine receptor, Science, 261, 1182, 10.1126/science.7689250 Nibbs, 1997, Cloning and characterization of a novel promiscuous human beta-chemokine receptor D6, J Biol Chem, 272, 32078, 10.1074/jbc.272.51.32078 Townson, 2002, Characterization of mouse CCX-CKR, a receptor for the lymphocyte-attracting chemokines TECK/mCCL25, SLC/mCCL21 and MIP-3beta/mCCL19: comparison to human CCX-CKR, Eur J Immunol, 32, 1230, 10.1002/1521-4141(200205)32:5<1230::AID-IMMU1230>3.0.CO;2-L Luster, 1995, The IP-10 chemokine binds to a specific cell surface heparan sulfate site shared with platelet factor 4 and inhibits endothelial cell proliferation, J Exp Med, 182, 219, 10.1084/jem.182.1.219 Rot, 1992, Endothelial cell binding of NAP-1/IL-8: role in neutrophil emigration, Immunol Today, 13, 291, 10.1016/0167-5699(92)90039-A Kuschert, 1999, Glycosaminoglycans interact selectively with chemokines and modulate receptor binding and cellular responses, Biochemistry, 38, 12959, 10.1021/bi990711d Hoogewerf, 1997, Glycosaminoglycans mediate cell surface oligomerization of chemokines, Biochemistry, 36, 13570, 10.1021/bi971125s Dalgleish, 1984, The CD4 (T4) antigen is an essential component of the receptor for the AIDS retrovirus, Nature, 312, 763, 10.1038/312763a0 Klatzmann, 1984, T-lymphocyte T4 molecule behaves as the receptor for human retrovirus LAV, Nature, 312, 767, 10.1038/312767a0 Maddon, 1986, The T4 gene encodes the AIDS virus receptor and is expressed in the immune system and the brain, Cell, 47, 333, 10.1016/0092-8674(86)90590-8 Clapham, 1991, Specific cell surface requirements for the infection of CD4-positive cells by human immunodeficiency virus types 1 and 2 and by Simian immunodeficiency virus, Virology, 181, 703, 10.1016/0042-6822(91)90904-P Dragic, 1992, Complementation of murine cells for human immunodeficiency virus envelope/CD4-mediated fusion in human/murine heterokaryons, J Virol, 66, 4794, 10.1128/JVI.66.8.4794-4802.1992 James, 1996, The receptor for HIV: dissection of CD4 and studies on putative accessory factors, Curr Top Microbiol Immunol, 205, 137 Berger, 1999, Chemokine receptors as HIV-1 coreceptors: roles in viral entry, tropism, and disease, Ann Rev Immunol, 17, 657, 10.1146/annurev.immunol.17.1.657 Littman, 1998, Chemokine receptors: keys to AIDS pathogenesis?, Cell, 93, 677, 10.1016/S0092-8674(00)81429-4 Miedema, 1994, Changing virus-host interactions in the course of HIV-1 infection, Immunol Rev, 140, 35, 10.1111/j.1600-065X.1994.tb00864.x Berson, 1996, A seven-transmembrane domain receptor involved in fusion and entry of T-cell-tropic human immunodeficiency virus type 1 strains, J Virol, 70, 6288, 10.1128/JVI.70.9.6288-6295.1996 Combadiere, 1996, Cloning and functional expression of CC CKR5, a human monocyte CC chemokine receptor selective for MIP-1(alpha), MIP-1(beta), and RANTES, J Leukocyte Biol, 60, 147, 10.1002/jlb.60.1.147 Samson, 1996, Molecular cloning and functional expression of a new human CC-chemokine receptor gene, Biochemistry, 35, 3362, 10.1021/bi952950g Choe, 1996, The β-chemokine receptors CCR3 and CCR5 facilitate infection by primary HIV-1 isolates, Cell, 85, 1135, 10.1016/S0092-8674(00)81313-6 Bleul, 1996, The lymphocyte chemoattractant SDF-1 is a ligand for LESTR/fusin and blocks HIV-1 entry, Nature, 382, 829, 10.1038/382829a0 Oberlin, 1996, The CXC chemokine SDF-1 is the ligand for LESTR/fusin and prevents infection by T-cell-line-adapted HIV-1, Nature, 382, 833, 10.1038/382833a0 Sattentau, 1998, HIV gp120: double lock strategy foils host defences, Structure, 6, 945, 10.1016/S0969-2126(98)00096-3 Geijtenbeek, 2000, DC-SIGN, a dendritic cell-specific HIV-1-binding protein that enhances trans-infection of T cells, Cell, 100, 587, 10.1016/S0092-8674(00)80694-7 Turville, 2001, HIV gp120 receptors on human dendritic cells, Blood, 98, 2482, 10.1182/blood.V98.8.2482 Trkola, 1996, CD4-dependent, antibody-sensitive interactions between HIV-1 and its co-receptor CCR-5, Nature, 384, 184, 10.1038/384184a0 Wu, 1996, CD4-induced interaction of primary HIV-1 gp120 glycoproteins with the chemokine receptor CCR-5, Nature, 384, 179, 10.1038/384179a0 Hoffman, 1999, Stable exposure of the coreceptor-binding site in a CD4-independent HIV-1 envelope protein, Proc Natl Acad Sci USA, 96, 6359, 10.1073/pnas.96.11.6359 Cocchi, 1996, The V3 domain of the HIV-1 gp120 envelope glycoprotein is critical for chemokine-mediated blockade of infection, Nat Med, 2, 1244, 10.1038/nm1196-1244 Weissenhorn, 1997, Atomic structure of the ectodomain from HIV-1 gp41, Nature, 387, 426, 10.1038/387426a0 Barbouche, 2003, Protein-disulfide isomerase-mediated reduction of two disulfide bonds of HIV envelope glycoprotein 120 occurs post-CXCR4 binding and is required for fusion, J Biol Chem, 278, 3131, 10.1074/jbc.M205467200 Doms, 2000, Beyond receptor expression: the influence of receptor conformation, density, and affinity in HIV-1 infection, Virology, 276, 229, 10.1006/viro.2000.0612 Stent, 1997, Macrophage tropism: fact or fiction?, J Leukocyte Biol, 62, 4, 10.1002/jlb.62.1.4 Yi, 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, 10.1128/JVI.73.9.7117-7125.1999 Kristiansen, 1998, Chemokine receptors and their crucial role in human immunodeficiency virus infection: major breakthroughs in HIV research, Scand J Immunol, 48, 339, 10.1046/j.1365-3083.1998.00438.x De Clercq, 2001, Inhibition of HIV infection by CXCR4 and CCR5 chemokine receptor antagonists, Antiviral Chem Chemother, 12, 19 Jekle, 2002, Coreceptor phenotype of natural human immunodeficiency virus with nef deleted evolves in vivo, leading to increased virulence, J Virol, 76, 6966, 10.1128/JVI.76.14.6966-6973.2002 Jekle, 2003, In vivo evolution of human immunodeficiency virus type 1 toward increased pathogenicity through CXCR4-mediated killing of uninfected CD4 T cells, J Virol, 77, 5846, 10.1128/JVI.77.10.5846-5854.2003 Penn, 1999, CXCR4 utilization is sufficient to trigger CD4+ T cell depletion in HIV-1-infected human lymphoid tissue, Proc Natl Acad Sci USA, 96, 663, 10.1073/pnas.96.2.663 Scarlatti, 1997, In vivo evolution of HIV-1 co-receptor usage and sensitivity to chemokine-mediated suppression, Nat Med, 3, 1259, 10.1038/nm1197-1259 Mellors, 1996, Prognosis in HIV-1 infection predicted by the quantity of virus in plasma, Science, 272, 1167, 10.1126/science.272.5265.1167 Henrard, 1995, Virologic and immunologic characterization of symptomatic and asymptomatic primary HIV-1 infection, J Acquir Immune Defic Syndr Hum Retrovirol, 9, 305, 10.1097/00042560-199507000-00013 Ho, 1995, Rapid turnover of plasma virions and CD4 lymphocytes in HIV-1 infection, Nature, 373, 123, 10.1038/373123a0 Connor, 1997, Change in coreceptor use coreceptor use correlates with disease progression in HIV-1-infected individuals, J Exp Med, 185, 621, 10.1084/jem.185.4.621 Este, 1999, Shift of clinical human immunodeficiency virus type 1 isolates from X4 to R5 and prevention of emergence of the syncytium-inducing phenotype by blockade of CXCR4, J Virol, 73, 5577, 10.1128/JVI.73.7.5577-5585.1999 Glushakova, 1999, Preferential coreceptor utilization and cytopathicity by dual-tropic HIV-1 in human lymphoid tissue ex vivo, J Clin Invest, 104, R7, 10.1172/JCI7403 Schuitemaker, 1992, Biological phenotype of human immunodeficiency virus type 1 clones at different stages of infection: progression of disease is associated with a shift from monocytotropic to T-cell-tropic virus population, J Virol, 66, 1354, 10.1128/JVI.66.3.1354-1360.1992 Fouchier, 1992, Phenotype-associated sequence variation in the third variable domain of the human immunodeficiency virus type 1 gp120 molecule, J Virol, 66, 3183, 10.1128/JVI.66.5.3183-3187.1992 Fouchier, 1995, Simple determination of human immunodeficiency virus type 1 syncytium-inducing V3 genotype by PCR, J Clin Microbiol, 33, 906, 10.1128/JCM.33.4.906-911.1995 Jensen, 2003, Predicting HIV-1 coreceptor usage with sequence analysis, AIDS Rev, 5, 104 Bjorndal, 1997, Coreceptor usage of primary human immunodeficiency virus type 1 isolates varies according to biological phenotype, J Virol, 71, 7478, 10.1128/JVI.71.10.7478-7487.1997 Lin, 2003, Identification of gp120 binding sites on CXCR4 by using CD4-independent human immunodeficiency virus type 2 Env proteins, J Virol, 77, 931, 10.1128/JVI.77.2.931-942.2003 Hu, 2000, Evolution of the human immunodeficiency virus type 1 envelope during infection reveals molecular corollaries of specificity for coreceptor utilization and AIDS pathogenesis, J Virol, 74, 11858, 10.1128/JVI.74.24.11858-11872.2000 Amara, 1997, HIV coreceptor downregulation as antiviral principle: SDF-1alpha-dependent internalization of the chemokine receptor CXCR4 contributes to inhibition of HIV replication, J Exp Med, 186, 139, 10.1084/jem.186.1.139 Mack, 1998, Aminooxypentane-RANTES induces CCR5 internalization but inhibits recycling: a novel inhibitory mechanism of HIV infectivity, J Exp Med, 187, 1215, 10.1084/jem.187.8.1215 Marechal, 1999, Opposite effects of SDF-1 on human immunodeficiency virus type 1 replication, J Virol, 73, 3608, 10.1128/JVI.73.5.3608-3615.1999 Garzino-Demo, 1998, β-chemokines and protection from HIV type 1 disease, AIDS Res Hum Retrovir, 14, S177 Paxton, 1996, Relative resistance to HIV-1 infection of CD4 lymphocytes from persons who remain uninfected despite multiple high-risk sexual exposure, Nat Med, 2, 412, 10.1038/nm0496-412 Gordon, 1999, Enhancement of human immunodeficiency virus type 1 infection by the CC-chemokine RANTES is independent of the mechanism of virus–cell fusion, J Virol, 73, 684, 10.1128/JVI.73.1.684-694.1999 Kelly, 1998, Dichotomous effects of beta-chemokines on HIV replication in monocytes and monocyte-derived macrophages, J Immunol, 160, 3091, 10.4049/jimmunol.160.7.3091 Marozsan, 2001, Mechanisms involved in stimulation of human immunodeficiency virus type 1 replication by aminooxypentane RANTES, J Virol, 75, 8624, 10.1128/JVI.75.18.8624-8638.2001 Mosier, 1999, Highly potent RANTES analogues either prevent CCR5-using human immunodeficiency virus type 1 infection in vivo or rapidly select for CXCR4-using variants, J Virol, 73, 3544, 10.1128/JVI.73.5.3544-3550.1999 Trkola, 1999, The CC-chemokine RANTES increases the attachment of human immunodeficiency virus type 1 to target cells via glycosaminoglycans and also activates a signal transduction pathway that enhances viral infectivity, J Virol, 73, 6370, 10.1128/JVI.73.8.6370-6379.1999 Garred, 1997, Dual effect of CCR5 Δ32 gene deletion in HIV-1-infected patients. Copenhagen AIDS Study Group, Lancet, 349, 1884, 10.1016/S0140-6736(05)63874-3 Michael, 1998, Exclusive and persistent use of the entry coreceptor CXCR4 by human immunodeficiency virus type 1 from a subject homozygous for CCR5 Δ32, J Virol, 72, 6040, 10.1128/JVI.72.7.6040-6047.1998 Gonzalez, 2005, The influence of CCL3L1 gene-containing segmental duplications on HIV-1/AIDS susceptibility, Science, 307, 1434, 10.1126/science.1101160 Ma, 1998, Impaired B-lymphopoiesis, myelopoiesis, and derailed cerebellar neuron migration in CXCR4- and SDF-1-deficient mice, Proc Natl Acad Sci USA, 95, 9448, 10.1073/pnas.95.16.9448 Nagasawa, 1996, Defects of B-cell lymphopoiesis and bone-marrow myelopoiesis in mice lacking the CXC chemokine PBSF/SDF-1, Nature, 382, 635, 10.1038/382635a0 Zou, 1998, Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development, Nature, 393, 595, 10.1038/31269 Menten, 1999, The LD78β isoform of MIP-1α is the most potent CCR5 agonist and HIV-1-inhibiting chemokine, J Clin Invest, 104, R1, 10.1172/JCI7318 Aquaro, 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, 10.1128/JVI.75.9.4402-4406.2001 De Meester, 1999, CD26, let it cut or cut it down, Immunol Today, 20, 367, 10.1016/S0167-5699(99)01486-3 Schols, 1998, CD26-processed RANTES(3–68), but not intact RANTES, has potent anti-HIV-1 activity, Antiviral Res, 39, 175, 10.1016/S0166-3542(98)00039-4 Proost, 1998, Amino-terminal truncation of chemokines by CD26/dipeptidyl-peptidase. IV. Conversion of RANTES into a potent inhibitor of monocyte chemotaxis and HIV-1-infection, J Biol Chem, 273, 7222, 10.1074/jbc.273.13.7222 Arenzana-Seisdedos, 1996, HIV blocked by chemokine antagonist, Nature, 383, 400, 10.1038/383400a0 Simmons, 1997, Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist, Science, 276, 276, 10.1126/science.276.5310.276 Proudfoot, 1996, Extension of recombinant human RANTES by the retention of the initiating methionine produces a potent antagonist, J Biol Chem, 271, 2599, 10.1074/jbc.271.5.2599 Lederman, 2004, Prevention of vaginal SHIV transmission in rhesus macaques through inhibition of CCR5, Science, 306, 485, 10.1126/science.1099288 Townson, 2000, Aminooxypentane addition to the chemokine macrophage inflammatory protein-1alpha P increases receptor affinities and HIV inhibition, J Biol Chem, 275, 39254, 10.1074/jbc.M006768200 Yang, 1999, Enhanced inhibition of human immunodeficiency virus type 1 by Met-stromal-derived factor 1beta correlates with down-modulation of CXCR4, J Virol, 73, 4582, 10.1128/JVI.73.6.4582-4589.1999 De Clercq, 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, 10.1073/pnas.89.12.5286 De Clercq, 2003, The bicyclam AMD3100 story, Nat Rev Drug Discov, 2, 581, 10.1038/nrd1134 De Clercq, 1994, Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100, Antimicrob Agents Chemother, 38, 668, 10.1128/AAC.38.4.668 Bridger, 1995, 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, J Med Chem, 38, 366, 10.1021/jm00002a019 Joao, 1995, Quantitative structural activity relationship study of bis-tetraazacyclic compounds. A novel series of HIV-1 and HIV-2 inhibitors, J Med Chem, 38, 3865, 10.1021/jm00019a017 De Vreese, 1996, The molecular target of bicyclams, potent inhibitors of human immunodeficiency virus replication, J Virol, 70, 689, 10.1128/JVI.70.2.689-696.1996 De Vreese, 1997, Sensitivity of human immunodeficiency virus to bicyclam derivatives is influenced by the three-dimensional structure of gp120, Antimicrob Agents Chemother, 41, 2616, 10.1128/AAC.41.12.2616 Este, 1996, Antiviral activity of the bicyclam derivative JM3100 against drug-resistant strains of human immunodeficiency virus type 1, Antiviral Res, 29, 297, 10.1016/0166-3542(95)00936-1 Schols, 1997, Bicyclams, a class of potent anti-HIV agents, are targeted at the HIV coreceptor fusin/CXCR-4, Antiviral Res, 35, 147, 10.1016/S0166-3542(97)00025-9 Schols, 1997, Inhibition of T-tropic HIV strains by selective antagonization of the chemokine receptor CXCR4, J Exp Med, 186, 1383, 10.1084/jem.186.8.1383 Donzella, 1998, AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor, Nat Med, 4, 72, 10.1038/nm0198-072 Schramm, 2000, Viral entry through CXCR4 is a pathogenic factor and therapeutic target in human immunodeficiency virus type 1 disease, J Virol, 74, 184, 10.1128/JVI.74.1.184-192.2000 Hatse, 2002, Chemokine receptor inhibition by AMD3100 is strictly confined to CXCR4, FEBS Lett, 527, 255, 10.1016/S0014-5793(02)03143-5 Hendrix, 2000, Pharmacokinetics and safety of AMD-3100, a novel antagonist of the CXCR-4 chemokine receptor, in human volunteers, Antimicrob Agents Chemother, 44, 1667, 10.1128/AAC.44.6.1667-1673.2000 Hendrix, 2004, Safety, pharmacokinetics, and antiviral activity of AMD3100, a selective CXCR4 receptor inhibitor, in HIV-1 infection, J Acquir Immune Defic Syndr, 37, 1253, 10.1097/01.qai.0000137371.80695.ef Murakami, 1997, A small molecule CXCR4 inhibitor that blocks T cell line-tropic HIV-1 infection, J Exp Med, 186, 1389, 10.1084/jem.186.8.1389 Arakaki, 1999, T134, a small-molecule CXCR4 inhibitor, has no cross-drug resistance with AMD3100, a CXCR4 antagonist with a different structure, J Virol, 73, 1719, 10.1128/JVI.73.2.1719-1723.1999 Tamamura, 1998, A low-molecular-weight inhibitor against the chemokine receptor CXCR4: a strong anti-HIV peptide T140, Biochem Biophys Res Com, 253, 877, 10.1006/bbrc.1998.9871 Doranz, 1997, A small-molecule inhibitor directed against the chemokine receptor CXCR4 prevents its use as an HIV-1 coreceptor, J Exp Med, 186, 1395, 10.1084/jem.186.8.1395 Sumner-Smith, 1995, Antiherpetic activities of N-alpha-acetyl-nona-d-arginine amide acetate, Drugs Exp Clin Res, 21, 1 Doranz, 2001, Safe use of the CXCR4 inhibitor ALX40-4C in humans, AIDS Res Hum Retrovir, 17, 475, 10.1089/08892220151126508 Zhou, 2003, Binding of ALX40-4C to APJ, a CNS-based receptor, inhibits its utilization as a co-receptor by HIV-1, Virology, 312, 196, 10.1016/S0042-6822(03)00185-5 Daelemans, 2000, A second target for the peptoid Tat/transactivation response element inhibitor CGP64222: inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry, Mol Pharmacol, 57, 116 Hamy, 1997, An inhibitor of the Tat/TAR RNA interaction that effectively suppresses HIV-1 replication, Proc Natl Acad Sci USA, 94, 3548, 10.1073/pnas.94.8.3548 Ichiyama, 2003, A duodenally absorbable CXC chemokine receptor 4 antagonist, KRH-1636, exhibits a potent and selective anti-HIV-1 activity, Proc Natl Acad Sci USA, 100, 4185, 10.1073/pnas.0630420100 Schols, 2003, Anti-HIV activity profile of AMD070, an orally bioavailable CXCR4 antagonist Princen, 2004, Inhibition of human immunodeficiency virus replication by a dual CCR5/CXCR4 antagonist, J Virol, 78, 12996, 10.1128/JVI.78.23.12996-13006.2004 Baba, 1999, A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity, Proc Natl Acad Sci USA, 96, 5698, 10.1073/pnas.96.10.5698 Dragic, 2000, A binding pocket for a small molecule inhibitor of HIV-1 entry within the transmembrane helices of CCR5, Proc Natl Acad Sci USA, 97, 5639, 10.1073/pnas.090576697 Strizki, 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, 10.1073/pnas.221375398 Reynes, 2002, SCH C: Safety and antiviral effects of a CCR5 receptor antagonist in HIV-1 infected subjects Schurmann, 2004, SCH-D: Antiviral activity of CCR5 receptor antagonist Maeda, 2001, Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5, J Biol Chem, 276, 35194, 10.1074/jbc.M105670200 Maeda, 2003, AK602: a novel HIV-specific spirodiketopiperazine CCR5 inhibitor potent against a wide spectrum of R5-HIV Napier, 2003, The preclinical pharmacokinetics and safety pharmacology of the anti-HIV CCR5 antagonist, UK-427857 Trkola, 2001, Potent, broad-spectrum inhibition of human immunodeficiency virus type 1 by the CCR5 monoclonal antibody PRO 140, J Virol, 75, 579, 10.1128/JVI.75.2.579-588.2001 Franti, 2004, Control of HIV-1 replication in the hu-PBL-SCID mouse model by an anti-CCR5 monoclonal antibody Schols, 2002, AMD-3100, a CXCR4 antagonist, reduced HIV viral load and X4 virus levels in humans Nakata, 2003, Potent in vivo anti-R5-HIV effects of AK602, a novel spirodiketopiperazine (SDP)-containing HIV-specific CCR5 inhibitor, in hu-PBMC-NOD-SCID Mice Doranz, 1996, A dual-tropic primary HIV-1 isolate that uses fusin and the beta-chemokine receptors CKR-5, CKR-3, and CKR-2b as fusion cofactors, Cell, 85, 1149, 10.1016/S0092-8674(00)81314-8 Jinno, 1998, Identification of the chemokine receptor TER1/CCR8 expressed in brain-derived cells and T cells as a new coreceptor for HIV-1 infection, Biochem Biophys Res Commun, 243, 497, 10.1006/bbrc.1998.8130 Horuk, 1998, The CC chemokine I-309 inhibits CCR8-dependent infection by diverse HIV-1 strains, J Biol Chem, 273, 386, 10.1074/jbc.273.1.386 Choe, 1998, The orphan seven-transmembrane receptor apj supports the entry of primary T-cell-line-tropic and dualtropic human immunodeficiency virus type 1, J Virol, 72, 6113, 10.1128/JVI.72.7.6113-6118.1998 Combadiere, 1998, Identification of CX3CR1. A chemotactic receptor for the human CX3C chemokine fractalkine and a fusion coreceptor for HIV-1, J Biol Chem, 273, 23799, 10.1074/jbc.273.37.23799 Liao, 1997, STRL33, a novel chemokine receptor-like protein, functions as a fusion cofactor for both macrophage-tropic and T cell line-tropic HIV-1, J Exp Med, 185, 2015, 10.1084/jem.185.11.2015 Matloubian, 2000, A transmembrane CXC chemokine is a ligand for HIV-coreceptor Bonzo, Nat Immunol, 1, 298, 10.1038/79738 Edinger, 1998, An orphan seven-transmembrane domain receptor expressed widely in the brain functions as a coreceptor for human immunodeficiency virus type 1 and simian immunodeficiency virus, J Virol, 72, 7934, 10.1128/JVI.72.10.7934-7940.1998 Deng, 1997, Expression cloning of new receptors used by simian and human immunodeficiency viruses, Nature, 388, 296, 10.1038/40894 Heiber, 1996, A novel human gene encoding a G-protein-coupled receptor (GPR15) is located on chromosome 3, Genomics, 32, 462, 10.1006/geno.1996.0143