-
Baba M, Nishimura O, Kanzaki N. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity[J]. Proc Natl Acad Sci USA, 1999, 96(): 5698-5703. doi: 10.1073/pnas.96.10.5698
-
Baba M, Takashima K, Miyake H. TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmaco-kinetics in humans[J]. Antimicrob Agents Chemother, 2005, 49(): 4584-4591. doi: 10.1128/AAC.49.11.4584-4591.2005
-
Berger E A, Murphy P M, Farber J M. Chemokine receptors as HIV-1 coreceptors: roles in viral entry, tropism, and disease[J]. Annu Rev Immunol, 1999, 17(): 657-700. doi: 10.1146/annurev.immunol.17.1.657
-
Bleul C C, Farzan M, Choe H. The lymphocyte chemoattractant SDF-1 is a ligand for LESTR/ fusin and blocks HIV-1 entry[J]. Nature, 1996, 382(): 829-833. doi: 10.1038/382829a0
-
Boshoff C, Endo Y, Collins P D. Angiogenic and HIV-inhibitory functions of KSHV-encoded che-mokines[J]. Science, 1997, 278(): 290-294. doi: 10.1126/science.278.5336.290
-
Chan D C, Chutkowski C T, Kim P S. Evidence that a prominent cavity in the coiled coil of HIV type 1 gp41 is an attractive drug target[J]. Proc Natl Acad Sci USA, 1998, 95(): 15613-15617. doi: 10.1073/pnas.95.26.15613
-
Chan D C, Fass D, Berger J M. Core structure of gp41 from the HIV envelope glycoprotein[J]. Cell, 1997, 89(): 263-273. doi: 10.1016/S0092-8674(00)80205-6
-
Clapham P R, Weber J N, Whitby D. Soluble CD4 blocks the infectivity of diverse strains of HIV and SIV for T cells and monocytes but not for brain and muscle cells[J]. Nature, 1989, 337(): 368-370. doi: 10.1038/337368a0
-
Cocchi F, DeVico A L, Garzino-Demo A. Identification of RANTES, MIP-1 alpha, and MIP-1 beta as the major HIV-suppressive factors produced by CD8+ T cells [see comments][J]. Science, 1995, 270(): 1811-1815. doi: 10.1126/science.270.5243.1811
-
Connor R I, Sheridan K E, Ceradini D. Change in coreceptor use correlates with disease pro-gression in HIV-1--infected individuals[J]. J Exp Med, 1997, 185(): 621-628. doi: 10.1084/jem.185.4.621
-
Daar E S, Li X L, Moudgil T. High concentrations of recombinant soluble CD4 are required to neutralize primary human immunodeficiency virus type 1 isolates[J]. Proc Natl Acad Sci USA, 1990, 87(): 6574-6578. doi: 10.1073/pnas.87.17.6574
-
Dalgleish A G, Beverley P C, Clapham P R. The CD4 (T4) antigen is an essential component of the receptor for the AIDS retrovirus[J]. Nature, 1984, 312(): 763-767. doi: 10.1038/312763a0
-
Deng Y, Zheng Q, Ketas T J. Protein design of a bacterially expressed HIV-1 gp41 fusion inhibitor[J]. Biochemistry, 2007, 46(): 4360-4369. doi: 10.1021/bi7001289
-
Donzella G A, Schols D, Lin S W. AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor[J]. Nat Med, 1998, 4(): 72-77. doi: 10.1038/nm0198-072
-
Doranz B J, Grovit-Ferbas K, Sharron M P. A small-molecule inhibitor directed against the chemokine receptor CXCR4 prevents its use as an HIV-1 coreceptor[J]. J Exp Med, 1997, 186(): 1395-1400. doi: 10.1084/jem.186.8.1395
-
Dragic T, Trkola A, Thompson D A. A binding pocket for a small molecule inhibitor of HIV-1 entry within the transmembrane helices of CCR5[J]. Proc Natl Acad Sci USA, 2000, 97(): 5639-5644. doi: 10.1073/pnas.090576697
-
Elias C J, Coggins C. Female-controlled methods to prevent sexual transmission of HIV[J]. Aids, 1996, 10(Suppl 3): S43-51.
-
Fichorova R N, Tucker L D, Anderson D J. The molecular basis of nonoxynol-9-induced vaginal inflame-mation and its possible relevance to human immunode-ficiency virus type 1 transmission[J]. J Infect Dis, 2001, 184(): 418-428. doi: 10.1086/jid.2001.184.issue-4
-
Gallo S A, Finnegan C M, Viard M. The HIV Env-mediated fusion reaction[J]. Biochim Biophys Acta, 2003, 1614(): 36-50. doi: 10.1016/S0005-2736(03)00161-5
-
Geijtenbeek T B, Kwon D S, Torensma R. DC-SIGN, a dendritic cell-specific HIV-1-binding protein that enhances trans-infection of T cells[J]. Cell, 2000, 100(): 587-597. doi: 10.1016/S0092-8674(00)80694-7
-
Hatse S, Princen K, De Clercq E. AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor[J]. Biochem Pharmacol, 2005, 70(): 752-761. doi: 10.1016/j.bcp.2005.05.035
-
Ho H T, Fan L, Nowicka-Sans B. Envelope conformational changes induced by human immunode-ficiency virus type 1 attachment inhibitors prevent CD4 binding and downstream entry events[J]. J Virol, 2006, 80(): 4017-4025. doi: 10.1128/JVI.80.8.4017-4025.2006
-
Hu Q, Barry A P, Wang Z. Evolution of the human immunodeficiency virus type 1 envelope during infection reveals molecular corollaries of specificity for coreceptor utilization and AIDS pathogenesis[J]. J Virol, 2000, 74(): 11858-11872. doi: 10.1128/JVI.74.24.11858-11872.2000
-
Hu Q, Frank I, Williams V. Blockade of attachment and fusion receptors inhibits HIV-1 infection of human cervical tissue[J]. J Exp Med, 2004, 199(): 1065-1075. doi: 10.1084/jem.20022212
-
Hu Q, Mahmood N, Shattock R J. High-mannose-specific deglycosylation of HIV-1 gp120 induced by resistance to cyanovirin-N and the impact on antibody neutralization[J]. Virology, 2007, 368(): 145-154. doi: 10.1016/j.virol.2007.06.029
-
Hu Q, Napier K B, Trent J O. Restricted variable residues in the C-terminal segment of HIV-1 V3 loop regulate the molecular anatomy of CCR5 utilization[J]. J Mol Biol, 2005, 350(): 699-712. doi: 10.1016/j.jmb.2005.05.024
-
Hu Q, Trent J O, Tomaras G D. Identification of Env determinants in V3 that influence the molecular anatomy of CCR5 utilization[J]. J Mol Biol, 2000, 302(): 359-375. doi: 10.1006/jmbi.2000.4076
-
Hu Q, Younson J, Griffin G E. Pertussis toxin and its binding unit inhibit HIV-1 infection of human cervical tissue and macrophages involving a CD14 pathway[J]. J Infect Dis, 2006, 194(): 1547-1556. doi: 10.1086/jid.2006.194.issue-11
-
Hussey R E, Richardson N E, Kowalski M. A soluble CD4 protein selectively inhibits HIV replication and syncytium formation[J]. Nature, 1988, 331(): 78-81. doi: 10.1038/331078a0
-
Ichiyama K, Yokoyama-Kumakura S, Tanaka Y. A duodenally absorbable CXC chemokine receptor 4 antagonist, KRH-1636, exhibits a potent and selective anti-HIV-1 activity[J]. Proc Natl Acad Sci USA, 2003, 100(): 4185-4190. doi: 10.1073/pnas.0630420100
-
Jacobson J M, Lowy I, Fletcher C V. Single-dose safety, pharmacology, and antiviral activity of the human immunodeficiency virus (HIV) type 1 entry inhibitor PRO 542 in HIV-infected adults[J]. J Infect Dis, 2000, 182(): 326-329. doi: 10.1086/jid.2000.182.issue-1
-
Jiang S, Zhao Q, Debnath A K. Peptide and non-peptide HIV fusion inhibitors[J]. Curr Pharm Des, 2002, 8(): 563-580. doi: 10.2174/1381612024607180
-
Kadow J, Wang H G, Lin P F. Small-molecule HIV-1 gp120 inhibitors to prevent HIV-1 entry: an emerging opportunity for drug development[J]. Curr Opin Investig Drugs, 2006, 7(): 721-726.
-
Kawamura T, Cohen S S, Borris D L. Candidate microbicides block HIV-1 infection of human immature Langerhans cells within epithelial tissue explants[J]. J Exp Med, 2000, 192(): 1491-1500. doi: 10.1084/jem.192.10.1491
-
Kawamura T, Gulden F O, Sugaya M. R5 HIV productively infects Langerhans cells, and infection levels are regulated by compound CCR5 polymorphisms[J]. Proc Natl Acad Sci USA, 2003, 100(): 8401-8406. doi: 10.1073/pnas.1432450100
-
Kilby J M, Hopkins S, Venetta T M. Potent suppression of HIV-1 replication in humans by T-20, a peptide inhibitor of gp41-mediated virus entry[J]. Nat Med, 1998, 4(): 1302-1307. doi: 10.1038/3293
-
Klatzmann D, Champagne E, Chamaret S. T-lymphocyte T4 molecule behaves as the receptor for human retrovirus LAV[J]. Nature, 1984, 312(): 767-768. doi: 10.1038/312767a0
-
Kledal T N, Rosenkilde M M, Coulin F. A broad-spectrum chemokine antagonist encoded by Kaposi's sarcoma-associated herpesvirus[J]. Science, 1997, 277(): 1656-1659. doi: 10.1126/science.277.5332.1656
-
Lalezari J P, Henry K, O'Hearn M. Enfuvirtide, an HIV-1 fusion inhibitor, for drug-resistant HIV infection in North and South America[J]. N Engl J Med, 2003, 348(): 2175-2185. doi: 10.1056/NEJMoa035026
-
Lazzarin A, Clotet B, Cooper D. Efficacy of enfuvirtide in patients infected with drug-resistant HIV-1 in Europe and Australia[J]. N Engl J Med, 2003, 348(): 2186-2195. doi: 10.1056/NEJMoa035211
-
Lederman M M, Veazey R S, Offord R. Prevention of vaginal SHIV transmission in rhesus macaques through inhibition of CCR5[J]. Science, 2004, 306(): 485-487. doi: 10.1126/science.1099288
-
Lehner T. The role of CCR5 chemokine ligands and antibodies to CCR5 coreceptors in preventing HIV infection[J]. Trends Immunol, 2002, 23(): 347-351. doi: 10.1016/S1471-4906(02)02252-4
-
Lehner T, Doyle C, Wang Y. Immunogenicity of the extracellular domains of C-C chemokine receptor 5 and the in vitro effects on simian immunodeficiency virus or HIV infectivity[J]. J Immunol, 2001, 166(): 7446-7455. doi: 10.4049/jimmunol.166.12.7446
-
Lin P F, Blair W, Wang T. A small molecule HIV-1 inhibitor that targets the HIV-1 envelope and inhibits CD4 receptor binding[J]. Proc Natl Acad Sci USA, 2003, 100(): 11013-11018. doi: 10.1073/pnas.1832214100
-
Liu S, Jing W, Cheung B. HIV gp41 C-terminal heptad repeat contains multifunctional domains. Relation to mechanisms of action of anti-HIV peptides[J]. J Biol Chem, 2007, 282(): 9612-9620. doi: 10.1074/jbc.M609148200
-
Liu S, Lu H, Niu J. Different from the HIV fusion inhibitor C34, the anti-HIV drug Fuzeon (T-20) inhibits HIV-1 entry by targeting multiple sites in gp41 and gp120[J]. J Biol Chem, 2005, 280(): 11259-11273. doi: 10.1074/jbc.M411141200
-
Ma D, Yu S, Li B. Synthesis and Biological Evaluation of 1, 3, 3, 4-Tetrasubstituted Pyrrolidine CCR5 Receptor Antagonists. Discovery of a Potent and Orally Bioavailable Anti-HIV Agent[J]. ChemMedChem, 2007, 2(): 187-193. doi: 10.1002/(ISSN)1860-7187
-
Mack M, Luckow B, Nelson P J. Aminooxypentane-RANTES induces CCR5 internalization but inhibits recycling: a novel inhibitory mechanism of HIV infectivity[J]. J Exp Med, 1998, 187(): 1215-1224. doi: 10.1084/jem.187.8.1215
-
McKnight A, Weiss R A. Blocking the docking of HIV-1[J]. Proc Natl Acad Sci USA, 2003, 100(): 10581-10582. doi: 10.1073/pnas.2035071100
-
McMichael A J, Hanke T. HIV vaccines 1983-2003[J]. Nat Med, 2003, 9(): 874-880. doi: 10.1038/nm0703-874
-
Moench T R, Chipato T, Padian N S. Preventing disease by protecting the cervix: the unexplored promise of internal vaginal barrier devices[J]. Aids, 2001, 15(): 1595-1602. doi: 10.1097/00002030-200109070-00001
-
Moore J P, Doms R W. The entry of entry inhibitors: a fusion of science and medicine[J]. Proc Natl Acad Sci USA, 2003, 100(): 10598-10602. doi: 10.1073/pnas.1932511100
-
Moore J P, Stevenson M. New targets for inhibitors of HIV-1 replication[J]. Nature Reviews, Molecular Cell Biology, 2000, 1(): 40-49. doi: 10.1038/35036060
-
Mosier D E, Picchio G R, Gulizia R J. Highly potent RANTES analogues either prevent CCR5-using human immunodeficiency virus type 1 infection in vivo or rapidly select for CXCR4-using variants[J]. J Virol, 1999, 73(): 3544-3550.
-
Munch J, Standker L, Adermann K. Discovery and optimization of a natural HIV-1 entry inhibitor targeting the gp41 fusion peptide[J]. Cell, 2007, 129(): 263-275. doi: 10.1016/j.cell.2007.02.042
-
Murakami T, Nakajima T, Koyanagi Y. A small molecule CXCR4 inhibitor that blocks T cell line-tropic HIV-1 infection[J]. J Exp Med, 1997, 186(): 1389-1393. doi: 10.1084/jem.186.8.1389
-
O'Hara B M, Olson W C. HIV entry inhibitors in clinical development[J]. Curr Opin Pharmacol, 2002, 2(): 523-528. doi: 10.1016/S1471-4892(02)00196-0
-
Oberlin E, Amara A, Bachelerie F. The CXC chemokine SDF-1 is the ligand for LESTR/fusin and prevents infection by T-cell-line-adapted HIV-1[J]. Nature, 1996, 382(): 833-835. doi: 10.1038/382833a0
-
Olson W C, Rabut G E, Nagashima K A. Differential inhibition of human immunodeficiency virus type 1 fusion, gp120 binding, and CC-chemokine activity by monoclonal antibodies to CCR5[J]. J Virol, 1999, 73(): 4145-4155.
-
Pantophlet R, Burton D R. GP120: target for neutralizing HIV-1 antibodies[J]. Annu Rev Immunol, 2006, 24(): 739-769. doi: 10.1146/annurev.immunol.24.021605.090557
-
Pastore C, Picchio G R, Galimi F. Two mechanisms for human immunodeficiency virus type 1 inhibition by N-terminal modifications of RANTES[J]. Antimicrob Agents Chemother, 2003, 47(): 509-517. doi: 10.1128/AAC.47.2.509-517.2003
-
Reimann K A, Khunkhun R, Lin W. A humanized, nondepleting anti-CD4 antibody that blocks virus entry inhibits virus replication in rhesus monkeys chronically infected with simian immunodeficiency virus[J]. AIDS Res Hum Retroviruses, 2002, 18(): 747-755. doi: 10.1089/08892220260139486
-
Rodriguez-Frade J M, Del Real G, Serrano A. Blocking HIV-1 infection via CCR5 and CXCR4 receptors by acting in trans on the CCR2 chemokine receptor[J]. Embo J, 2004, 23(): 66-76. doi: 10.1038/sj.emboj.7600020
-
Root M J, Kay M S, Kim P S. Protein design of an HIV-1 entry inhibitor[J]. Science, 2001, 291(): 884-888. doi: 10.1126/science.1057453
-
Rowland-Jones S L. Timeline: AIDS pathogenesis: what have two decades of HIV research taught us?[J]. Nat Rev Immunol, 2003, 3(): 343-348. doi: 10.1038/nri1058
-
Schols D, Struyf S, Van Damme J. Inhibition of T-tropic HIV strains by selective antagonization of the chemokine receptor CXCR4[J]. J Exp Med, 1997, 186(): 1383-1388. doi: 10.1084/jem.186.8.1383
-
Schon A, Madani N, Klein J C. Thermodynamics of binding of a low-molecular-weight CD4 mimetic to HIV-1 gp120[J]. Biochemistry, 2006, 45(): 10973-10980. doi: 10.1021/bi061193r
-
Shattock R J, Moore J P. Inhibiting sexual transmission of HIV-1 infection[J]. Nat Rev Micro, 2003, 1(): 25-34. doi: 10.1038/nrmicro729
-
Shearer W T, Israel R J, Starr S. Recombinant CD4-IgG2 in human immunodeficiency virus type 1-infected children: phase 1/2 study. The Pediatric AIDS Clinical Trials Group Protocol 351 Study Team[J]. J Infect Dis, 2000, 182(): 1774-1779. doi: 10.1086/jid.2000.182.issue-6
-
Sia S K, Kim P S. Protein grafting of an HIV-1-inhibiting epitope[J]. Proc Natl Acad Sci USA, 2003, 100(): 9756-9761. doi: 10.1073/pnas.1733910100
-
Simmons G, Clapham P R, Picard L. Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist[J]. Science, 1997, 276(): 276-279. doi: 10.1126/science.276.5310.276
-
Stone A. Microbicides: a new approach to preventing HIV and other sexually transmitted infections[J]. Nat Rev Drug Discov, 2002, 1(): 977-985. doi: 10.1038/nrd959
-
Stone N D, Dunaway S B, Flexner C W. Multiple Dose Escalation Study of the Safety, Pharma-cokinetics, and Biologic Activity of Oral AMD070, a selective CXCR4 Receptor Inhibitor, in Human Subjects (ACTG A5191)[J]. Antimicrob Agents Chemother, 2007, 51(): 2351-2358. doi: 10.1128/AAC.00013-07
-
Strizki J M, Tremblay C, Xu S. Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodefi-ciency virus type 1[J]. Antimicrob Agents Chemother, 2005, 49(): 4911-4919. doi: 10.1128/AAC.49.12.4911-4919.2005
-
Strizki J M, Xu S, Wagner N E. 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[J]. Proc Natl Acad Sci USA, 2001, 98(): 12718-12723. doi: 10.1073/pnas.221375398
-
Sutor G C, Dreikhausen U, Vahning U. Neutralization of HIV-1 by anti-idiotypes to monoclonal anti-CD4. Potential for idiotype immunization against HIV[J]. J Immunol, 1992, 149(): 1452-1461.
-
Takashima K, Miyake H, Kanzaki N. Highly potent inhibition of human immunodeficiency virus type 1 replication by TAK-220, an orally bioavailable small-molecule CCR5 antagonist[J]. Antimicrob Agents Che-mother, 2005, 49(): 3474-3482. doi: 10.1128/AAC.49.8.3474-3482.2005
-
Tamamura H, Xu Y, Hattori T. A low-molecular-weight inhibitor against the chemokine receptor CXCR4: a strong anti-HIV peptide T140[J]. Biochem Biophys Res Commun, 1998, 253(): 877-882. doi: 10.1006/bbrc.1998.9871
-
Trkola A, Ketas T J, Nagashima K A. Potent, broad-spectrum inhibition of human immunodeficiency virus type 1 by the CCR5 monoclonal antibody PRO 140[J]. J Virol, 2001, 75(): 579-588. doi: 10.1128/JVI.75.2.579-588.2001
-
Trkola A, Kuhmann S E, Strizki J M. HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use[J]. Proc Natl Acad Sci USA, 2002, 99(): 395-400. doi: 10.1073/pnas.012519099
-
Tsamis F, Gavrilov S, Kajumo F. Analysis of the mechanism by which the small-molecule CCR5 antagonists SCH-351125 and SCH-350581 inhibit human immunodeficiency virus type 1 entry[J]. J Virol, 2003, 77(): 5201-5208. doi: 10.1128/JVI.77.9.5201-5208.2003
-
Turpin J A. Considerations and development of topical microbicides to inhibit the sexual transmission of HIV[J]. Expert Opin Investig Drugs, 2002, 11(): 1077-1097. doi: 10.1517/13543784.11.8.1077
-
UNAIDS. 2006. Joint United Nations Programme on HIV/AIDS (UNAIDS and World Health Organization (WHO). AIDS Epidemic Updated-December 2006 (www.unaids.org/en/HIV_data/epi2006/default.asp).
-
Veazey R S, Klasse P J, Ketas T J. Use of a Small Molecule CCR5 Inhibitor in Macaques to Treat Simian Immunodeficiency Virus Infection or Prevent Simian-Human Immunodeficiency Virus Infection[J]. J Exp Med, 2003, 198(): 1551-1562. doi: 10.1084/jem.20031266
-
Veazey R S, Klasse P J, Schader S M. Protection of macaques from vaginal SHIV challenge by vaginally delivered inhibitors of virus-cell fusion[J]. Nature, 2005, 438(): 99-102. doi: 10.1038/nature04055
-
Vermeire K, Princen K, Hatse S. CADA, a novel CD4-targeted HIV inhibitor, is synergistic with various anti-HIV drugs in vitro[J]. Aids, 2004, 18(): 2115-2125. doi: 10.1097/00002030-200411050-00003
-
Vermeire K, Zhang Y, Princen K. CADA inhibits human immunodeficiency virus and human herpesvirus 7 replication by down-modulation of the cellular CD4 receptor[J]. Virology, 2002, 302(): 342-353. doi: 10.1006/viro.2002.1624
-
Walker D K, Abel S, Comby P. Species differences in the disposition of the CCR5 antagonist, UK-427, 857, a new potential treatment for HIV[J]. Drug Metab Dispos, 2005, 33(): 587-595. doi: 10.1124/dmd.104.002626
-
Watson C, Jenkinson S, Kazmierski W. The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor[J]. Mol Pharmacol, 2005, 67(): 1268-1282. doi: 10.1124/mol.104.008565
-
Weissenhorn W, Dessen A, Harrison S C. Atomic structure of the ectodomain from HIV-1 gp41 [see comments][J]. Nature, 1997, 387(): 426-430. doi: 10.1038/387426a0
-
Wilkinson D, Tholandi M, Ramjee G. Nonoxynol-9 spermicide for prevention of vaginally acquired HIV and other sexually transmitted infections: systematic review and meta-analysis of randomised controlled trials including more than 5000 women[J]. Lancet Infect Dis, 2002, 2(): 613-617. doi: 10.1016/S1473-3099(02)00396-1
-
Yang Q E, Stephen A G, Adelsberger J W. Discovery of small-molecule human immunodeficiency virus type 1 entry inhibitors that target the gp120-binding domain of CD4[J]. J Virol, 2005, 79(): 6122-6133. doi: 10.1128/JVI.79.10.6122-6133.2005
-
Zaitseva M, Peden K, Golding H. HIV coreceptors: role of structure, posttranslational modifications, and internalization in viral-cell fusion and as targets for entry inhibitors[J]. Biochim Biophys Acta, 2003, 1614(): 51-61. doi: 10.1016/S0005-2736(03)00162-7
-
Zhao Q, Ma L, Jiang S. Identification of N-phenyl-N'-(2, 2, 6, 6-tetramethyl-piperidin-4-yl)-oxalamid es as a new class of HIV-1 entry inhibitors that prevent gp120 binding to CD4[J]. Virology, 2005, 339(): 213-225. doi: 10.1016/j.virol.2005.06.008