1. Barré-Sinoussi F, Chermann JC, Rey F, et al. Isolation of a T-lymphotropic retrovirus from a patient at risk for acquired immune deficiency syndrome (AIDS). Science 1983;220(4599):868-71. (In eng). DOI:10.1126/science.6189183.
2. Deeks SG, Overbaugh J, Phillips A, Buchbinder S. HIV infection. Nat Rev Dis Primers 2015;1:15035. (In eng). DOI: 10.1038/nrdp.2015.35.
3. Okoye AA, Picker LJ. CD4(+) T-cell depletion in HIV infection: mechanisms of immunological failure. Immunol Rev 2013;254(1):54-64. (In eng). DOI: 10.1111/imr.12066.
4. Vidya Vijayan KK, Karthigeyan KP, Tripathi SP, Hanna LE. Pathophysiology of CD4+ T-Cell Depletion in HIV-1 and HIV-2 Infections. Front Immunol 2017;8:580. (In eng). DOI: 10.3389/fimmu.2017.00580.
5. Bbosa N, Kaleebu P, Ssemwanga D. HIV subtype diversity worldwide. Curr Opin HIV AIDS 2019;14(3):153-160. (In eng). DOI: 10.1097/coh.0000000000000534.
6. Taylor BS, Sobieszczyk ME, McCutchan FE, Hammer SM. The challenge of HIV-1 subtype diversity. N Engl J Med 2008;358(15):1590-602. (In eng). DOI: 10.1056/NEJMra0706737.
7. Nyamweya S, Hegedus A, Jaye A, Rowland-Jones S, Flanagan KL, Macallan DC. Comparing HIV-1 and HIV-2 infection: Lessons for viral immunopathogenesis. Rev Med Virol 2013;23(4):221-40. (In eng). DOI: 10.1002/rmv.1739.
8. Nkeze J, Li L, Benko Z, Li G, Zhao RY. Molecular characterization of HIV-1 genome in fission yeast Schizosaccharomyces pombe. Cell Biosci 2015;5:47. (In eng). DOI: 10.1186/s13578-015-0037-7.
9. Engelman A, Cherepanov P. The structural biology of HIV-1: mechanistic and therapeutic insights. Nat Rev Microbiol 2012;10(4):279-90. (In eng). DOI: 10.1038/nrmicro2747.
10. Pu J, Wang Q, Xu W, Lu L, Jiang S. Development of Protein- and Peptide- Based HIV Entry Inhibitors Targeting gp120 or gp41. Viruses 2019;11(8) (In eng). DOI: 10.3390/v11080705.
11. Grande F, Occhiuzzi MA, Rizzuti B, et al. CCR5/CXCR4 Dual Antagonism for the Improvement of HIV Infection Therapy. Molecules 2019;24(3) (In eng). DOI: 10.3390/molecules24030550.
12. Lusic M, Siliciano RF. Nuclear landscape of HIV-1 infection and integration. Nat Rev Microbiol 2017;15(2):69-82. (In eng). DOI: 10.1038/nrmicro.2016.162.
13. Engelman A, Mizuuchi K, Craigie R. HIV-1 DNA integration: mechanism of viral DNA cleavage and DNA strand transfer. Cell 1991;67(6):1211-21. (In eng). DOI: 10.1016/0092-8674(91)90297-c.
14. Cherepanov P, Ambrosio AL, Rahman S, Ellenberger T, Engelman A. Structural basis for the recognition between HIV-1 integrase and transcriptional coactivator p75. Proc Natl Acad Sci U S A 2005;102(48):17308-13. (In eng). DOI: 10.1073/pnas.0506924102.
15. van Nuland R, van Schaik FM, Simonis M, et al. Nucleosomal DNA binding drives the recognition of H3K36-methylated nucleosomes by the PSIP1- PWWP domain. Epigenetics Chromatin 2013;6(1):12. (In eng). DOI: 10.1186/1756-8935-6-12.
16. Eidahl JO, Crowe BL, North JA, et al. Structural basis for high-affinity binding of LEDGF PWWP to mononucleosomes. Nucleic Acids Res 2013;41(6):3924-36. (In eng). DOI: 10.1093/nar/gkt074.
17. Turlure F, Maertens G, Rahman S, Cherepanov P, Engelman A. A tripartite DNA-binding element, comprised of the nuclear localization signal and two AT-hook motifs, mediates the association of LEDGF/p75 with chromatin in vivo. Nucleic Acids Res 2006;34(5):1653-65. (In eng). DOI: 10.1093/nar/gkl052.
18. Symons J, Cameron PU, Lewin SR. HIV integration sites and implications for maintenance of the reservoir. Curr Opin HIV AIDS 2018;13(2):152-159. DOI: 10.1097/COH.0000000000000438.
19. Vranckx LS, Demeulemeester J, Saleh S, et al. LEDGIN-mediated Inhibition of Integrase-LEDGF/p75 Interaction Reduces Reactivation of Residual Latent HIV. EBioMedicine 2016;8:248-264. (In eng). DOI: 10.1016/j.ebiom.2016.04.039.
20. Ciuffi A, Llano M, Poeschla E, et al. A role for LEDGF/p75 in targeting HIV DNA integration. Nat Med 2005;11(12):1287-9. (In eng). DOI: 10.1038/nm1329.
21. Shun MC, Raghavendra NK, Vandegraaff N, et al. LEDGF/p75 functions downstream from preintegration complex formation to effect gene-specific HIV-1 integration. Genes Dev 2007;21(14):1767-78. (In eng). DOI: 10.1101/gad.1565107.
22. Pornillos O, Ganser-Pornillos BK, Yeager M. Atomic-level modelling of the HIV capsid. Nature 2011;469(7330):424-7. (In eng). DOI: 10.1038/nature09640.
23. McFadden WM, Snyder AA, Kirby KA, et al. Rotten to the core: antivirals targeting the HIV-1 capsid core. Retrovirology 2021;18(1):41. (In eng). DOI: 10.1186/s12977-021-00583-z.
24. Jurado KA, Wang H, Slaughter A, et al. Allosteric integrase inhibitor potency is determined through the inhibition of HIV-1 particle maturation. Proc Natl Acad Sci U S A 2013;110(21):8690-5. (In eng). DOI: 10.1073/pnas.1300703110.
25. Desimmie BA, Schrijvers R, Demeulemeester J, et al. LEDGINs inhibit late stage HIV-1 replication by modulating integrase multimerization in the virions. Retrovirology 2013;10:57. (In eng). DOI: 10.1186/1742-4690-10-57.
26. Balakrishnan M, Yant SR, Tsai L, et al. Non-catalytic site HIV-1 integrase inhibitors disrupt core maturation and induce a reverse transcription block in target cells. PLoS One 2013;8(9):e74163. (In eng). DOI: 10.1371/journal.pone.0074163.
27. Kessl JJ, Kutluay SB, Townsend D, et al. HIV-1 Integrase Binds the Viral RNA Genome and Is Essential during Virion Morphogenesis. Cell 2016;166(5):1257-1268.e12. (In eng). DOI: 10.1016/j.cell.2016.07.044.
28. Fadel HJ, Morrison JH, Saenz DT, et al. TALEN knockout of the PSIP1 gene in human cells: analyses of HIV-1 replication and allosteric integrase inhibitor mechanism. J Virol 2014;88(17):9704-17. (In eng). DOI: 10.1128/jvi.01397-14.
29. Saag MS, Gandhi RT, Hoy JF, et al. Antiretroviral Drugs for Treatment and Prevention of HIV Infection in Adults: 2020 Recommendations of the International Antiviral Society-USA Panel. Jama 2020;324(16):1651-1669. (In eng). DOI: 10.1001/jama.2020.17025.
30. Lai YT. Small Molecule HIV-1 Attachment Inhibitors: Discovery, Mode of Action and Structural Basis of Inhibition. Viruses 2021;13(5) (In eng). DOI: 10.3390/v13050843.
31. Xiao T, Cai Y, Chen B. HIV-1 Entry and Membrane Fusion Inhibitors. Viruses 2021;13(5) (In eng). DOI: 10.3390/v13050735.
32. Markham A. Ibalizumab: First Global Approval. Drugs 2018;78(7):781-785. (In eng). DOI: 10.1007/s40265-018-0907-5.
33. Rai MA, Pannek S, Fichtenbaum CJ. Emerging reverse transcriptase inhibitors for HIV-1 infection. Expert Opin Emerg Drugs 2018;23(2):149-157. (In eng). DOI: 10.1080/14728214.2018.1474202.
34. Dow DE, Bartlett JA. Dolutegravir, the Second-Generation of Integrase Strand Transfer Inhibitors (INSTIs) for the Treatment of HIV. Infect Dis Ther 2014;3(2):83-102. (In eng). DOI: 10.1007/s40121-014-0029-7.
35. Cocohoba J, Dong BJ. Raltegravir: the first HIV integrase inhibitor. Clin Ther 2008;30(10):1747-65. (In eng). DOI: 10.1016/j.clinthera.2008.10.012.
36. Unger NR, Worley MV, Kisgen JJ, Sherman EM, Childs-Kean LM. Elvitegravir for the treatment of HIV. Expert Opin Pharmacother 2016;17(17):2359-2370. (In eng). DOI: 10.1080/14656566.2016.1250885.
37. Hayashi H, Takamune N, Nirasawa T, et al. Dimerization of HIV-1 protease occurs through two steps relating to the mechanism of protease dimerization inhibition by darunavir. Proc Natl Acad Sci U S A 2014;111(33):12234-9. (In eng). DOI: 10.1073/pnas.1400027111.
38. Anstett K, Brenner B, Mesplede T, Wainberg MA. HIV drug resistance against strand transfer integrase inhibitors. Retrovirology 2017;14(1):36. (In eng). DOI: 10.1186/s12977-017-0360-7.
39. Kandel CE, Walmsley SL. Dolutegravir - a review of the pharmacology, efficacy, and safety in the treatment of HIV. Drug Des Devel Ther 2015;9:3547-55. (In eng). DOI: 10.2147/dddt.S84850.
40. Spagnuolo V, Castagna A, Lazzarin A. Bictegravir. Curr Opin HIV AIDS 2018;13(4):326-333. (In eng). DOI: 10.1097/coh.0000000000000468.
41. Clotet B, DeJesus E, Lazzarin A, Livrozet M, Morlat P, Vavro CL, Horton JH, Huang J, Sato A, Underwood MR. HIV Integrase Genotypic and Phenotypic Changes between Day 1 and Day 11 in Subjects with Raltegravir Resistant HIV Treated with S/GSK1349572: Results of Viking Study. abstr TUPE0130. 18th International AIDS Conference. Vienna, Austria 2010.
42. Marcus JL, Leyden WA, Alexeeff SE, et al. Comparison of Overall and Comorbidity-Free Life Expectancy Between Insured Adults With and Without HIV Infection, 2000-2016. JAMA Netw Open 2020;3(6):e207954. (In eng). DOI: 10.1001/jamanetworkopen.2020.7954.
43. Hoen B, Fournier I, Lacabaratz C, et al. Structured treatment interruptions in primary HIV-1 infection: the ANRS 100 PRIMSTOP trial. J Acquir Immune Defic Syndr 2005;40(3):307-16. (In eng). DOI: 10.1097/01.qai.0000182628.66713.31.
44. Castagna A, Muccini C, Galli L, et al. Analytical treatment interruption in chronic HIV-1 infection: time and magnitude of viral rebound in adults with 10 years of undetectable viral load and low HIV-DNA (APACHE study). J Antimicrob Chemother 2019;74(7):2039-2046. (In eng). DOI: 10.1093/jac/dkz138.
45. Hogg RS, Bangsberg DR, Lima VD, et al. Emergence of drug resistance is associated with an increased risk of death among patients first starting HAART. PLoS Med 2006;3(9):e356. (In eng). DOI: 10.1371/journal.pmed.0030356.
46. Clutter DS, Jordan MR, Bertagnolio S, Shafer RW. HIV-1 drug resistance and resistance testing. Infect Genet Evol 2016;46:292-307. (In eng). DOI: 10.1016/j.meegid.2016.08.031.
47. Christ F, Shaw S, Demeulemeester J, et al. Small-molecule inhibitors of the LEDGF/p75 binding site of integrase block HIV replication and modulate integrase multimerization. Antimicrob Agents Chemother 2012;56(8):4365-74. (In eng). DOI: 10.1128/aac.00717-12.
48. Kessl JJ, Jena N, Koh Y, et al. Multimode, cooperative mechanism of action of allosteric HIV-1 integrase inhibitors. J Biol Chem 2012;287(20):16801-11. (In eng). DOI: 10.1074/jbc.M112.354373.
49. Tsiang M, Jones GS, Niedziela-Majka A, et al. New class of HIV-1 integrase (IN) inhibitors with a dual mode of action. J Biol Chem 2012;287(25):21189-203. (In eng). DOI: 10.1074/jbc.M112.347534.
50. Fenwick C, Amad M, Bailey MD, et al. Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor. Antimicrob Agents Chemother 2014;58(6):3233-44. (In eng). DOI: 10.1128/aac.02719-13.
51. Gupta K, Turkki V, Sherrill-Mix S, et al. Structural Basis for Inhibitor- Induced Aggregation of HIV Integrase. PLoS Biol 2016;14(12):e1002584. (In eng). DOI: 10.1371/journal.pbio.1002584.
52. Amadori C, van der Velden YU, Bonnard D, et al. The HIV-1 integrase- LEDGF allosteric inhibitor MUT-A: resistance profile, impairment of virus maturation and infectivity but without influence on RNA packaging or virus immunoreactivity. Retrovirology 2017;14(1):50. (In eng). DOI: 10.1186/s12977-017-0373-2.
53. Maehigashi T, Ahn S, Kim UI, et al. A highly potent and safe pyrrolopyridine-based allosteric HIV-1 integrase inhibitor targeting host LEDGF/p75-integrase interaction site. PLoS Pathog 2021;17(7):e1009671. (In eng). DOI: 10.1371/journal.ppat.1009671.
54. Christ F, Voet A, Marchand A, et al. Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication. Nat Chem Biol 2010;6(6):442-8. (In eng). DOI: 10.1038/nchembio.370.
55. Engelman AN. Multifaceted HIV integrase functionalities and therapeutic strategies for their inhibition. J Biol Chem 2019;294(41):15137-15157. (In eng). DOI: 10.1074/jbc.REV119.006901.
56. Vansant G, Vranckx LS, Zurnic I, et al. Impact of LEDGIN treatment during virus production on residual HIV-1 transcription. Retrovirology 2019;16(1):8. (In eng). DOI: 10.1186/s12977-019-0472-3.
57. Sato M, Motomura T, Aramaki H, et al. Novel HIV-1 integrase inhibitors derived from quinolone antibiotics. J Med Chem 2006;49(5):1506-8. (In eng). DOI: 10.1021/jm0600139.
58. Shimura K, Kodama E, Sakagami Y, et al. Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137). J Virol 2008;82(2):764-74. (In eng). DOI: 10.1128/jvi.01534-07.
59. Adachi A, Gendelman HE, Koenig S, et al. Production of acquired immunodeficiency syndrome-associated retrovirus in human and nonhuman cells transfected with an infectious molecular clone. J Virol 1986;59(2):284-91. (In eng). DOI: 10.1128/jvi.59.2.284-291.1986.
60. Zhu B, Cai G, Hall EO, Freeman GJ. In-fusion assembly: seamless engineering of multidomain fusion proteins, modular vectors, and mutations. Biotechniques 2007;43(3):354-9. (In eng). DOI: 10.2144/000112536.
61. Japour AJ, Mayers DL, Johnson VA, et al. Standardized peripheral blood mononuclear cell culture assay for determination of drug susceptibilities of clinical human immunodeficiency virus type 1 isolates. The RV-43 Study Group, the AIDS Clinical Trials Group Virology Committee Resistance Working Group. Antimicrob Agents Chemother 1993;37(5):1095-101. (In eng). DOI: 10.1128/aac.37.5.1095.
62. Kimpton J, Emerman M. Detection of replication-competent and pseudotyped human immunodeficiency virus with a sensitive cell line on the basis of activation of an integrated beta-galactosidase gene. J Virol 1992;66(4):2232-9. (In eng). DOI: 10.1128/jvi.66.4.2232-2239.1992.
63. Tsiang M, Jones GS, Hung M, et al. Affinities between the binding partners of the HIV-1 integrase dimer-lens epithelium-derived growth factor (IN dimer-LEDGF) complex. J Biol Chem 2009;284(48):33580-99. (In eng). DOI: 10.1074/jbc.M109.040121.
64. Hazuda DJ, Hastings JC, Wolfe AL, Emini EA. A novel assay for the DNA strand-transfer reaction of HIV-1 integrase. Nucleic Acids Res 1994;22(6):1121-2. (In eng). DOI: 10.1093/nar/22.6.1121.
65. Kodama EI, Kohgo S, Kitano K, et al. 4'-Ethynyl nucleoside analogs: potent inhibitors of multidrug-resistant human immunodeficiency virus variants in vitro. Antimicrob Agents Chemother 2001;45(5):1539-46. (In eng). DOI: 10.1128/aac.45.5.1539-1546.2001.
66. Kobayashi M, Yoshinaga T, Seki T, et al. In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother 2011;55(2):813-21. (In eng). DOI: 10.1128/aac.01209-10.
67. Lataillade M, Chiarella J, Kozal MJ. Natural polymorphism of the HIV-1 integrase gene and mutations associated with integrase inhibitor resistance. Antivir Ther 2007;12(4):563-70. (In eng).
68. Rhee SY, Liu TF, Kiuchi M, et al. Natural variation of HIV-1 group M integrase: implications for a new class of antiretroviral inhibitors. Retrovirology 2008;5:74. (In eng). DOI: 10.1186/1742-4690-5-74.
69. Ceccherini-Silberstein F, Malet I, D'Arrigo R, Antinori A, Marcelin AG, Perno CF. Characterization and structural analysis of HIV-1 integrase conservation. AIDS Rev 2009;11(1):17-29. (In eng).
70. Bonnard D, Le Rouzic E, Eiler S, et al. Structure-function analyses unravel distinct effects of allosteric inhibitors of HIV-1 integrase on viral maturation and integration. J Biol Chem 2018;293(16):6172-6186. (In eng). DOI: 10.1074/jbc.M117.816793.
71. Eron JJ, Clotet B, Durant J, et al. Safety and efficacy of dolutegravir in treatment-experienced subjects with raltegravir-resistant HIV type 1 infection: 24-week results of the VIKING Study. J Infect Dis 2013;207(5):740-8. (In eng). DOI: 10.1093/infdis/jis750.
72. DHHS. Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents Living with HIV. Aug 16, 2021.
73. 日本エイズ学会 HIV 感染症治療委員会. HIV 感染症「治療の手引き」第 24 版. 2020 年 11 月.
74. Raffi F, Rachlis A, Stellbrink HJ, et al. Once-daily dolutegravir versus raltegravir in antiretroviral-naive adults with HIV-1 infection: 48 week results from the randomised, double-blind, non-inferiority SPRING-2 study. Lancet 2013;381(9868):735-43. (In eng). DOI: 10.1016/s0140- 6736(12)61853-4.
75. Lewin SR, Rouzioux C. HIV cure and eradication: how will we get from the laboratory to effective clinical trials? Aids 2011;25(7):885-97. (In eng). DOI: 10.1097/QAD.0b013e3283467041.
76. Durand CM, Blankson JN, Siliciano RF. Developing strategies for HIV-1 eradication. Trends Immunol 2012;33(11):554-62. (In eng). DOI: 10.1016/j.it.2012.07.001.
77. Fletcher CV, Staskus K, Wietgrefe SW, et al. Persistent HIV-1 replication is associated with lower antiretroviral drug concentrations in lymphatic tissues. Proc Natl Acad Sci U S A 2014;111(6):2307-12. DOI: 10.1073/pnas.1318249111.
78. Kim Y, Anderson JL, Lewin SR. Getting the "Kill" into "Shock and Kill": Strategies to Eliminate Latent HIV. Cell Host Microbe 2018;23(1):14-26. (In eng). DOI: 10.1016/j.chom.2017.12.004.
79. Spivak AM, Planelles V. Novel Latency Reversal Agents for HIV-1 Cure. Annu Rev Med 2018;69:421-436. DOI: 10.1146/annurev-med-052716- 031710.
80. Vansant G, Bruggemans A, Janssens J, Debyser Z. Block-And-Lock Strategies to Cure HIV Infection. Viruses 2020;12(1) (In eng). DOI: 10.3390/v12010084.
81. Leth S, Schleimann MH, Nissen SK, et al. Combined effect of Vacc-4x, recombinant human granulocyte macrophage colony-stimulating factor vaccination, and romidepsin on the HIV-1 reservoir (REDUC): a single-arm, phase 1B/2A trial. Lancet HIV 2016;3(10):e463-72. (In eng). DOI: 10.1016/s2352-3018(16)30055-8.
82. Tapia G, Højen JF, Ökvist M, et al. Sequential Vacc-4x and romidepsin during combination antiretroviral therapy (cART): Immune responses to Vacc-4x regions on p24 and changes in HIV reservoirs. J Infect 2017;75(6):555-571. (In eng). DOI: 10.1016/j.jinf.2017.09.004.
83. Bruggemans A, Vansant G, Balakrishnan M, et al. GS-9822, a preclinical LEDGIN candidate, displays a block-and-lock phenotype in cell culture. Antimicrob Agents Chemother 2021;65(5) (In eng). DOI: 10.1128/aac.02328- 20.
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