HIV-1 integrase: From biology to chemotherapeutics

Current HIV Research

Volumn 5, Issue 4, 2007, Pages 365-388

  Zeinalipour Loizidou, Eriketi ^a   Nicolaou, Christos ^a   Nicolaides, Athanasios ^a   Kostrikis, Leondios G ^a  

^a UNIVERSITY OF CYPRUS   (Cyprus)

Author keywords

Computer aided drug design; HIV 1 integrase; Inhibitors

Indexed keywords

1 [5 (4 FLUOROBENZYL) 2 FURYL] 3 (1,2,4 TRIAZOL 3 YL) 1,3 PROPANEDIONE; ANTIINFECTIVE AGENT; ANTIRETROVIRUS AGENT; ANTIVIRUS AGENT; CICHORIC ACID; CURCUMIN; DICAFFEOYLQUINIC ACID; FZ 41; GS 1937; GS 9137; INDOLICIDIN; INDOLICIDIN DERIVATIVE; INTEGRASE; INTEGRASE INHIBITOR; L 870712; L 870812; L 900612; MERCAPTOSALICYLHYDRAZIDE; N (4 FLUOROBENZYL) 8 HYDROXY 5 (TETRAHYDRO 2H 1,2 THIAZIN 2 YL) 1,6 NAPHTHYRIDINE 7 CARBOXAMIDE S,S DIOXIDE; PROTEIN GAP31; PROTEIN K159; PROTEIN MAP30; SALICYLHYDRAZIDE; SURAMIN; THALASSIOLIN A; THALASSIOLIN B; THALASSIOLIN C; UNCLASSIFIED DRUG; UNINDEXED DRUG; V 165; VIRUS DNA; VIRUS RNA; ZINTEVIR;

ANTIVIRAL ACTIVITY; CLINICAL TRIAL; COMPUTER AIDED DESIGN; DNA BINDING; DNA INTEGRATION; DRUG DESIGN; DRUG POTENCY; DRUG POTENTIATION; DRUG TARGETING; DRUG WITHDRAWAL; ENZYME ACTIVITY; ENZYME STRUCTURE; HIGH THROUGHPUT SCREENING; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; LIFE CYCLE; MOLECULAR MECHANICS; NONHUMAN; QUANTITATIVE STRUCTURE ACTIVITY RELATION; REAL TIME POLYMERASE CHAIN REACTION; REVIEW; VIRUS LOAD; VIRUS REPLICATION; X RAY CRYSTALLOGRAPHY;

ANTI-RETROVIRAL AGENTS; COMPUTER-AIDED DESIGN; DRUG DESIGN; HIV INTEGRASE; HIV INTEGRASE INHIBITORS; HUMANS;

EID: 34447280643     PISSN: 1570162X     EISSN: None     Source Type: Journal    
DOI: 10.2174/157016207781023965     Document Type: Review

References (322)

1. Abd-Elazem IS, Chen HS, Bates RB, Huang RCC. (2002). Isolation of two highly potent and non-toxic inhibitors of human immunodeficiency virus type 1 (HIV-1) integrase from Salvia miltiorrhiza. Antiviral Research. 55: 91-106.
2. Acel A, Udashkin BE, Wainberg MA, Faust EA. (1998). Efficient gap repair catalyzed in vitro by an intrinsic DNA polymerase activity of human immunodeficiency virus type 1 integrase. Journal of Virology. 72: 2062-2071.
3. Andrake MD, Skalka AM. (1996). Retroviral integrase, putting the pieces together. The Journal of Biological Chemistry. 271: 19633-19636.
4. Anthony NJ. (2004). HIV-1 integrase: A target for new AIDS chemotherapeutics. Current Topics in Medicinal Chemistry. 4: 979-990.
5. Artico M, Silvestri R, Massa S, Loi AG, Corrias S, Piras G, Colla PL. (1996). 2-Sulfonyl-4-chloroanilino moiety: A potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones. Journal of Medicinal Chemistry. 39: 522-530.
6. Asante-Appiah E, Skalka AM. (1997). A metal-induced conformational change and activation of HIV-1 integrase. The Journal of Biological Chemistry. 272: 16196-16205.
7. Barré-Sinoussi F. (1996). HIV as the cause of AIDS. Lancet. 348: 31-35.
8. Barreca ML, Rao A, Luca LD, Zappala M, Gurnari C, Monforte P, Clercq ED, Maele BV, Debyser Z, Witvrouw M, Briggs JM, Chimirri A. (2004). Efficient 3D database screening for novel HIV-1IN inhibitors. Journal of Chemical Information and Computer Sciences, 44: 1450-1455.
9. Barreca ML, Ferro S, Rao A, Luca LD, Zappala M, Monforte A-M, Debyser Z, Witvrouw M, Chimirri A. (2005). Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors. Journal of Medicinal Chemistry. 48: 7084-7088.
10. Berkhout B, Silverman RH, Jeang KT. (1989). Tat trans-activates the human immunodeficiency virus through a nascent RNA target. Cell. 59: 273-282.
11. Bernardi F, Bottoni A, DeVivo M, Garavelli M, Keseru G, Naray-Szabo G. (2002). A hypothetical mechanism for HIV-1 integrase catalytic action: DFT modelling of a bio-mimetic environment. Chemical Physics Letters. 362: 1-7.
12. Bissantz C, Folkers G, Rognan D. (2000). Virtual screening of chemical databases: Does the best docking/scoring method depend on the target? Rational Approaches to Drug Discovery. Proceedings of the 13th European Symposium on Quantitative Structure Activity Relationships. Prous Science. Hoeltje H.-D. and Sippl W. (editors).
13. Bonnenfart S, Thomas CM, Vita C, Subra F, Deprez E, Zouhiri F, Desmaele D, D'Angelo J, Mouscadet JF, Leh H. (2004). Styrylquinolines, Integrase inhibitors acting prior to integration: a new mechanism of action for anti-integrase agents. Journal of Virology. 78: 5728-5736.
14. Bor YC, Miller MD, Bushman FD, Orgel LE. (1996). Target-sequence preferences of HIV-1 integration complexes in vitro. Virology. 222: 283-288.
15. Brin E, Yi JZ, Skalka AM, Leis J. (2000). Modeling the late steps in HIV-1 retroviral integrase-catalyzed DNA integration. The Journal of Biological Chemistry. 275: 39287-39295.
16. Brodin P, Pinskaya M, Parsch U, Bischerour J, Leh H, Romanova E, Engels JW, Gottikh M, Mouscadet JF. (2001). 6-Oxocytidine containing oligonucleotides inhibit the HIV-1 integrase in vitro. Nucleosides Nucleotides & Nucleic Acids. 20: 481-486.
17. Brodin P, Pinskaya M, Buckle M, Parsch U, Romanova E, Engels J, Gottikh M, Mouscadet J-F. (2002). Disruption of HIV-1 integrase-DNA complexes by short 6-oxocytosine-containing oligonucleotides. Biochemistry. 41: 1529-1538.
18. Brooun A, Richman DD, Kornbluth RS. (2001). HIV-1 preintegration complexes preferentially integrate into longer target DNA molecules in solution as detected by a sensitive, polymerase chain reaction-based integration assay. The Journal of Biological Chemistry. 276: 46946-46952.
19. Brown N, McKay B, Gasteiger J. (2006). A novel workflow for the inverse QSPR problem using multiobjective optimization. Journal of Computer-Aided Molecular Design. 20: 333-341.
20. Bujacz G, Jaskolski M, Alexandratos J, Wlodawer A, Merkel G, Katz RA, Skalka AM. (1995). High-resolution structure of the catalytic domain of avian-sarcoma virus integrase. Journal of Molecular Biology. 253: 333-346.
21. Bujacz G, Alexandratos J, Qing Z, Clement-Mella C, Wlodawer A. (1996). The catalytic domain of human immunodeficiency virus integrase: Ordered active site in the F185H mutant. FEBS Letters. 398: 175-178.
22. Bukrinsky MI, Sharova N, Dempsey MP, Stanwick TL, Bukrinskaya AG, Haggerty S, Stevenson M. (1992). Active nuclear import of human-immunodeficiency-virus type-1 preintegration complexes. Proceedings of the National Academy of Sciences United States of America. 89: 6580-6584.
23. Bukrinsky MI, Sharova N, McDonald TL, Pushkarskaya T, Tarpley WG, Stevenson M. (1993). Association of integrase, matrix, and reverse-transcriptase antigens of human-immunodeficiency-virus type-1 with viral nucleic-acids following acute infection. Proceedings of the National Academy of Sciences United States of America. 90: 6125-6129.
24. Burke CJ, Sanyal G, Bruner MW, Ryan JA, LaFemina RL, Robbins HL, Zeft AS, Middaugh CR, Cordingley MG. (1992). Structural implications of spectroscopic characterization of a putative zinc finger peptide from HIV-1 integrase. The Journal of Biological Chemistry. 267: 9639-9644.
25. Bushman FD, Craigie R. (1991). Activities of human-immunodeficiency-virus (HIV) integration protein in vitro - specific cleavage and integration of HIV DNA. Proceedings of the National Academy of Sciences United States of America. 88: 1339-1343.
26. Bushman FD, Engelman A, Palmer I, Wingfield P, Craigie R. (1993). Domains of the integrase protein of human-immunodeficiency-virus type-1 responsible for polynucleotidyl transfer and zinc-binding. Proceedings of the National Academy of Sciences United States of America. 90: 3428-3432.
27. Butler SL, Hansen MST, Bushman FD. (2001). A quantitative assay for HIV DNA integration in vivo. Nature Medicine. 7: 631-634.
28. Cai M, Zheng R, Caffrey M, Craigie R, Clore GM, Gronenborn AM. (1997). Solution structure of the N-terminal zinc binding domain of HIV-1 integrase. Nature Structural Biology. 4: 567-577.
29. Cai M, Huang Y, Caffrey M, Zheng R, Craigie R, Clore GM, Gronenborn AM. (1998). Solution structure of the His12 -> Cys mutant of the N-terminal zinc binding domain of HIV-1 integrase complexed to cadmium. Protein Science. 7: 2669-2674.
30. Carlson HA, Masukawa KM, Rubins K, Bushman FD, Jorgensen WL, Lins RD, Briggs JM, McCammon JA. (2000). Developing a dynamic pharmacophore model for HIV-1 integrase. Journal of Medicinal Chemistry. 43: 2100-2114.
31. Carteau S, Mouscadet JF, Goulaouic H, Subra F, Auclair C. (1993). Inhibitory effect of the polyanionic drug suramin of the in vitro HIV DNA integration reaction. Archives of Biochemistry and Biophysics. 305: 606-610.
32. Carteau S, Mouscardet JF, Goulaouic H, Subra F, Auclair C. (1993). Effect of topoisomerase inhibitors of the in vitro HIV DNA integration reaction. Biochemical and Biophysical Research Communications. 192: 1409-1414.
33. Chen H, Engelman A. (1998). The barrier-to-autointegration protein is a host factor for HIV type 1 integration. Proceedings of the National Academy of Sciences United States of America. 95: 15270-15274.
34. Chen I-J, Neamati N, Nicklaus MC, Orr A, Anderson L, Jr. Barchi JJ, Kelley JA, Pommier Y, Jr. MacKerell AD. (2000). Identification of HIV-1 integrase inhibitors via three-dimensional database searching using ASV and HIV-1 integrases as targets. Bioorganic & Medicinal Chemistry. 8: 2385-2398.
35. Chen I-J, Neamati N, MacKerell JAD. (2002). Structure-based inhibitor design targeting HIV-1 integrase. Current Drug Targets: Infectious Disorders. 2: 217-234.
36. Chen JC, Krucinski J, Miercke LJ, Finer-Moore JS, Tang AH, Leavitt AD, Stroud RM. (2000). Crystal structure of the HIV-1 integrase catalytic core and C-terminal domains: A model for viral DNA binding. Proceedings of the National Academy of Sciences United States of America. 97: 8233-8238.
37. Chen ZG, Yan YW, Munshi S, Li Y, Zugay-Murphy J, Xu B, Witmer M, Felock P, Wolfe A, Sardana V, Emini EA, Hazuda D, Kuo LC. (2000). X-ray structure of simian immunodeficiency virus integrase containing the core and C-terminal domain (residues 50293) - An initial glance of the viral DNA binding platform. Journal of Molecular Biology. 296: 521-533.
38. Cherepanov P, Este JA, Rando RF, Ojwang JO, Reekmans G, Steinfeld R, David G, De Clercq E, Debyzer Z. (1997). Mode of Interaction of G-Quartets with the integrase of human Immunodeficiency Virus Type 1. Molecular Pharmacology. 52: 771-780.
39. Cherepanov P, Maertens G, Proost P, Devereese B, Beeumen JV, Engelborghs Y, De Clerq E, Debyser Z. (2003). HIV-1 integrase forms stable tetramers and associates with LEDGF/p75 protein in human cells. The Journal of Biological Chemistry. 278: 372-381.
40. Cherepanov P, Devroe E, Silver PA, Engelman A. (2004). Identification of an evolutionarily conserved domain in human lens epithelium-derived growth factor/transcriptional co-activator p75 (LEDGF/p75) that binds HIV-1 integrase. The Journal of Biological Chemistry. 279: 48883-48892.
41. Cherepanov P, Ambrosio ALB, Rahman S, Ellenberger T, Engelman A. (2005). Structural basis for the recognition between HIV-1 integrase and transcriptional coactivator p75. Proceedings of the National Academy of Sciences United States of America. 102: 17308-17313.
42. Cherepanov P, Sun Z-YJ, Rahman S, Maertens G, Wagner G, Engelman A. (2005). Solution structure of the HIV-1 integrase-binding domain in LEDGF/p75. Nature Structural & Molecular Biology. 12: 526-532.
43. Chiu TK, Davies DR. (2004). Structure and function of HIV-1 integrase. Current Topics in Medicinal Chemistry. 4: 965-977.
44. Chow SA, Vincent KA, Ellison V, Brown PO. (1992). Science. 255: 723-726.
45. Chow SA, Brown PO. (1994). Juxtaposition of 2 viral-DNA ends in a bimolecular disintegration reaction mediated by multimers of human-immunodeficiency-virus type-1 or murine leukemia-virus integrase. Journal of Virology. 68: 7869-7878.
46. Chun TW, Stuyver L, Mizell SB, Ehler LA, Mican JA, Baseler M, Lloyd AL, Nowak MA, Fauci AS. (1997). Presence of an inducible HIV-1 latent reservoir during highly active antiretroviral therapy. Proceedings of the National Academy of Sciences United States of America. 94: 13193-13197.
47. Chun TW, Engel D, Berrey MM, Shea T, Corey L, Fauci AS. (1998). Early establishment of a pool of latently infected, resting CD4(+) T cells during primary HIV-1 infection. Proceedings of the National Academy of Sciences United States of America. 95: 8869-8873.
48. Chun TW, Davey JRT, Ostrowski M, Justement JS, Engel D, Mullins JI, Fauci AS. (2000). Relationship between pre-existing viral reservoirs and the re-emergence of plasma viremia after discontinuation of highly active anti-retroviral therapy. Nature Medicine. 6: 757-761.
49. Chun TW, Nickle DC, Justement JS, Large D, Semerjian A, Curlin ME, O'Shea MA, Hallahan CW, Daucher M, Ward DJ, Moir S, Mullins JI, Kovacs C, Fauci AS. (2005). HIV-infected individuals receiving effective antiviral therapy for extended periods of time continually replenish their viral reservoir. Journal of Clinical Investigation. 115: 3250-3255.
50. Ciuffi A, Llano M, Poeschla E, Hoffmann C, Leipzig J, Shinn P, Ecker JR, Bushman F. (2005). A role for LEDGF/p75 in targeting HIV DNA integration. Nature Medicine. 11: 1287-1289.
51. Cojen J. (2006). RETROVIRUS MEETING: Novel attacks on HIV move closer to reality. Science. 311: 943-943.
52. Costi R, Santo RD, Artico M, Massa S, Ragno R, Loddo R, Colla ML, Tramontano E, Colla PL, Pani A. (2004). 2,6-Bis(3,4,5-trihydroxybenzylydene) derivatives of cyclohexanone: novel potent HIV-1 integrase inhibitors that prevent HIV-1 multiplication in cell-based assays. Bioorganic & Medicinal Chemistry. 12: 199-215.
53. Cowan JA. (1998). Metal activation of enzymes in nucleic acid biochemistry. Chemical Reviews. 98: 1067-1088.
54. Craigie R, Mizuuchi K, Bushman FD, Engelman A. (1991). A rapid in vitro assay for HIV DNA integration. Nucleic Acids Research. 19: 2729-2734.
55. Craigie R. (2001). HIV integrase, a brief overview from chemistry to therapeutics. The Journal of Biological Chemistry. 276: 23213-23216.
56. Cushman M, Sherman P. (1992). Inhibition of HIV-1 integration protein by aurintricarboxylic acid monomers, monomer analogs, and polymer fractions. Biochemical and Biophysical Research Communications. 185: 85-90.
57. Daniel R, Greger JG, Katz RA, Taganov KD, Wu X, Kappes JC, Skalka AM. (2004). Evidence that stable retroviral transduction and cell survival following DNA integration depend on components of the nonhomologous end joining repair pathway. Journal of Virology. 78: 8573-8581.
58. Dayam R, Neamati N. (2003). Small-molecule HIV-1 integrase inhibitors: the 2001-2002 update. Current Pharmaceutical Design. 9: 1789-1802.
59. Dayam R, Sanchez T, Neamati N. (2005). Diketo acid pharmacophore. 2. Discovery of structurally diverse inhibitors of HIV-1 integrase. Journal of Medicinal Chemistry. 48: 8009-8015.
60. De Clercq E. (2004). Antiviral drugs in current clinical use. Journal of Clinical Virology. 30: 115-133.
61. De Clercq E. (2004). HIV-chemotherapy and -prophylaxis: new drugs, leads and approaches. International Journal of Biochemistry & Cell Biology. 36:1800-1822.
62. De Luca L, Pedretti A, Vistoli G, Barreca ML, Villa L, Monforte P, Chimirri A. (2003). Analysis of the full-length integrase - DNA complex by a modified approach for DNA docking. Biochemical and Biophysical Research Communications. 310: 1083-1088.
63. De Luca L, Vistoli G, Pedretti A, Barreca ML, Chimirri A. (2005). Molecular dynamics studies of the full-length integrase-DNA complex. Biochemical and Biophysical Research Communications. 336: 1010-1016.
64. de Soultrait VR, Caumont A, Parissi V, Morellet N, Ventura M, Lenoir C, Litvak S, Fournier M, Roques B. (2002). A novel short peptide is a specific inhibitor of the human immunodeficiency virus type 1 integrase. Journal of Molecular Biology. 318: 45-58.
65. Deng H, Liu R, Ellmeier W, Choe S, Unutmaz D, Burkhart M, Marzio PD, Marmon S, Sutton RE, Hill CM, Davis CB, Peiper SC, Schall TJ, Littman DR, Landau NR. (1996). Identification of a major co-receptor for primary isolates of HIV-1. Nature. 381: 661-666.
66. Deng J, Lee KW, Sanchez T, Cui M, Neamati N, Briggs JM. (2005). Dynamic receptor-based pharmacophore model development and its application in designing novel HIV-1 integrase inhibitors. Journal of Medicinal Chemistry. 48: 1496-1505.
67. Deng J, Sanchez T, Neamati N, Briggs JM. (2006). Dynamic pharmacophore model optimization: Identification of novel HIV-1 integrase inhibitors. Journal of Medicinal Chemistry. 49: 1684-1692.
68. Deprez E, Barbe S, Kolaski M, Leh H, Zouhiri F, Auclair C, Brochon J-C, Le Bret M, Mouscadet J-F. (2004). Mechanism of HIV-1 integrase inhibition by styrylquinoline derivatives in vitro. Molecular Pharmacology. 65: 85-98.
69. Dragic T, Litwin V, Allaway GP, Martin SR, Huang Y, Nagashima KA, Cayanan C, Maddon PJ, Koup RA, Moore JP, Paxton WA. (1996). HIV-1 entry into CD4(+) cells is mediated by the chemokine receptor CC-CKR-5. Nature. 381: 667-673.
70. Dupont R, Jeanson L, Mouscadet J-F, Cotelle P. (2001). Synthesis and HIV-1 integrase inhibitory activities of catechol and biscatechol derivatives. Bioorganic & Medicinal Chemistry Letters. 11: 3175-3178.
71. Dyda F, Hickman AB, Jenkins T, Engelman A, Craigie R, Davies D. (1994). Crystal structure of the catalytic domain of HIV-1 integrase: similarity to other polynucleotidyl transferases. Science. 266: 1981-1986.
72. Eich E, Pertz H, Kaloga M, Schulz J, Fesen MR, Mazumder A, Pommier Y. (1996). (-)-Arctigenin as a lead structure for inhibitors of human immunodeficiency virus type-1 integrase. Journal of Medicinal Chemistry. 39: 86-95.
73. Eijkelenboom A, Sprangers R, Hard K, Lutzke R, Plasterk RH, Boelens R, Kaptein R. (1999). Refined solution structure of the C-terminal DNA-binding domain of human immunovirus-1 integrase. Proteins: Structure, Function, and Genetics. 36: 556-564.
74. Eijkelenboom AP, van den Ent FM, Vos A, Doreleijers JF, Hard K, Tullius TD, Plasterk RH, Kaptein R, Boelens R. (1997). The solution structure of the amino-terminal HHCC domain of HIV-2 integrase: a three-helix bundle stabilized by zinc. Current Biology. 7: 739-746.
75. Ellison V, Gerton J, Vincent KA, Brown PO. (1995). An essential interaction between distinct domains of HIV-1 integrase mediates assembly of the active multimer. The Journal of Biological Chemistry. 270: 3320-3326.
76. Ellison VO, Brown P. (1994). A stable complex between integrase and viral-DNA ends mediates human-immunodeficiency-virus integration in vitro. Proceedings of the National Academy of Sciences United States of America. 91: 7316-7320.
77. Emiliani S, Mousnier A, Busschots K, Maroun M, Maele BV, TempéD, Vandekerckhove L, Moisant F, Ben-Slama L, Witvrouw M, Christ F, Rain J-C, Dargemont C, Debyser Z, Benarous R. (2005). Integrase mutants defective for interaction with LEDGF/p75 are impaired in chromosome tethering and HIV-1 replication. The Journal of Biological Chemistry. 280: 25517-25523.
78. Engelman A, Craigie R. (1992). Identification of conserved amino-acid residues critical for human-immunodeficiency-virus type-1 integrase function in vitro. Journal of Virology. 66: 6361-6369.
79. Engelman A, Bushman FD, Craigie R. (1993). Identification of discrete functional domains of HIV-1 integrase and their organization within an active multimeric complex. The EMBO Journal. 12: 3269-3275.
80. Engelman A, Hickman AB, Craigie R. (1994). The core and carboxyl-terminal domains of the integrase protein of human immunodeficiency-virus type-1 each contribute to nonspecific DNA-binding. Journal of Virology. 68: 5911-5917.
81. Engelman A, Englund G, Orenstein JM, Martin MA, Craigie R. (1995). Multiple effects of mutations in human-immunodeficiency-virus type-1 integrase on viral replication. Journal of Virology. 69: 2729-2736.
82. Engelman A, Liu Y, Chen H, Farzan M, Dyda F. (1997). Structure-based mutagenesis of the catalytic domain of human immunodeficiency virus type 1 integrase. Journal of Virology. 71: 3507-3514.
83. Espeseth AS, Felock P, Wolfe A, Witmer M, Grobler J, Anthony N, Egbertson M, Melamed JY, Young S, Hamill T, Cole JL, Hazuda DJ. (2000). HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase. Proceedings of the National Academy of Sciences United States of America. 97: 11244-11249.
84. Esposito D, Craigie R. (1998). Sequence specificity of viral end DNA binding by HIV-1 integrase reveals critical regions for protein-DNA interaction. The EMBO Journal. 17: 5832-5843.
85. Esté AJ, Cabrera C, Schols D, Cherepanov P, Gutierez A, Witvrouw M, Pannecouque C, Debyser Z, Rando R, Clotet B, Desmyter J, De Clercq E. (1998). Human immunodeficiency virus glycoprotein gp120 as the primary target for the antiviral action of AR177 (Zintevir). Molecular Pharmacology. 53: 340-345.
86. Ezzell C. (1987). AIDS drug gets green light. Nature. 329: 751-751.
87. Farnet CM, Haseltine WA. (1990). Integration of human-immunodeficiency-virus type-1 DNA in vitro. Proceedings of the National Academy of Sciences United States of America. 87: 4164-4168.
88. Farnet CM, Haseltine WA. (1991). Determination of viral-proteins present in the human-immunodeficiency-virus type-1 preintegration complex. Journal of Virology. 65: 1910-1915.
89. Farnet CM, Wang B, Lipford JR, Bushman F. (1996). Differential inhibition of HIV-1 preintegration complexes and purified integrase protein by small molecules. Proceedings of the National Academy of Sciences United States of America. 93: 9742-9747.
90. Farnet CM, Bushman FD. (1997). HIV-1 cDNA integration: Requirement of HMG I(Y) protein for function of preintegration complexes in vitro. Cell. 88: 483-492.
91. Farnet CM, Wang B, Hansen M, Lipford JR, Zalkow L, Robinson WE, Siegel J, Bushman F. (1998). Human immunodeficiency virus type 1 cDNA integration: New aromatic hydroxylated inhibitors and studies of the inhibition mechanism. Antimicrobial Agents and Chemotherapy. 42: 2245-2253.
92. Fauci AS. (2003). HIV and AIDS: 20 years of science. Nature Medicine. 9: 839-843.
93. Faure A, Calmels C, Desjobert C, Castroviejo M, Caumont-Sacros A, Tarrago-Litvak L, Litvak S, Parissi V. (2005). HIV-1 integrase crosslinked oligomers are active in vitro. Nucleic Acids Research. 33: 977-986.
94. Fesen MR, Kohn KW, Leteurtre F, Pommier Y. (1993). Inhibitors of human-immunodeficiency-virus integrase. Proceedings of the National Academy of Sciences United States of America. 90: 2399-2403.
95. Fesen MR, Pommier Y, Leteurtre F, Hiroguchi S, Yung J, Kohn KW. (1994). Inhibition of HIV-1 integrase by flavones, caffeic acid phenethyl ester (CAPE) and related-compounds. Biochemical Pharmacology. 48: 595-608.
96. Fikkert V, Cherepanov P, Van Laethem K, Hantson A, Van Remoortei B, Pannecouque C, De Clercq E, Debyser Z, Vandamme A-M, Witvrouw M. (2002). env chimeric virus technology for evaluating human immunodeficiency virus susceptibility to entry inhibitors. Antimicrobial Agents and Chemotherapy. 46: 3954-3962.
97. Fikkert V, Maele BV, Vercammen J, Hantson A, Remoortel BV, Michiels M, Gurnari C, Pannecouque C, Maeyer MD, Engelborghs Y, Clercq ED, Debyser Z, Witvrouw M. (2003). Development of resistance against Diketo derivatives of human immunodeficiency virus type 1 by progressive accumulation of integrase mutations. Journal of Virology. 77: 11459-11470.
98. Fikkert V, Hombrouck A, Remoortel BV, Maeyer MD, Pannecouque C, Clercq ED, Debyser Z, Witvrouw M. (2004). Multiple mutations in human immunodeficiency virus-1 integrase confer resistance to the clinical trial drug S-1360. AIDS. 18: 2019-2028.
99. Finzi D, Hermankova M, Pierson T, Carruth LM, Buck C, Chaisson RE, Quinn TC, Chadwick K, Margolick J, Brookmeyer R, Gallant J, Markowitz M, Ho DD, Richman DD, Siliciano RF. (1997). Identification of a reservoir for HIV-1 in patients on highly active antiretroviral therapy. Science. 278: 1295-1300.
100. Fitzgerald PM, Springer JP. (1991). Structure and function of retroviral proteases. Annual Review of Biophysics and Biophysical Chemistry. 20: 299-320.
101. Fletcher TMI, Scares MA, McPhearson S, Hui H, Wiskerchen M, Muesing MA, Shaw GM, Leavitt AD, Boeke JD, Hahn BH. (1997). Complementation of integrase function in HIV-1 virions. The EMBO Journal. 16: 5123-5138.
102. Gallay P, Stitt V, Mundy C, Oettinger M, Trono D. (1996). Role of the karyopherin pathway in human immunodeficiency virus type 1 nuclear import. Journal of Virology. 70: 1027-1032.
103. Gallo RC. (2002). HISTORICAL ESSAY: The Early years of HIV/AIDS. Science. 298: 1728-1730.
104. Gao K, Butler SL, Bushman F. (2001). Human immunodeficiency virus type 1 integrase: arrangement of protein domains in active cDNA complexes. The EMBO Journal. 20: 3565-3576.
105. Gerton JL, Brown PO. (1997). The core domain of HIV-1 integrase recognizes key features of its DNA substrates. The Journal of Biological Chemistry. 272: 25809-25815.
106. Gerton JL, Ohgi S, Olsen M, DeRisi J, Brown PO. (1998). Effects of mutations in residues near the active site of human immunodeficiency virus type 1 integrase on specific enzyme-substrate interactions. Journal of Virology. 72: 5046-5055.
107. Gerton JL, Herschlag D, Brown PO. (1999). Stereospecificity of reactions catalyzed by HIV-1 integrase. The Journal of Biological Chemistry. 274: 33480-33487.
108. Goldgur Y, Dyda F, Hickman AB, Jenkins TM, Craigie R, Davis DR. (1998). Three new structures of the core domain of HIV-1 integrase: An active site that binds magnesium. Proceedings of the National Academy of Sciences United States of America. 95: 9150-9154.
109. Goldgur Y, Craigie R, Cohen GH, Fujiwara T, Yoshinaga T, Fujishita T, Sugimoto H, Endo T, Murai H, Davies DR. (1999). Structure of the HIV-1 integrase catalytic domain complexed with an inhibitor: A platform for antiviral drug design. Proceedings of the National Academy of Sciences United States of America. 96: 13040-13043.
110. Goto T, Nakai M, Ikuta K. (1998). The life-cycle of human immunodeficiency virus type 1. Micron. 29: 123-138.
111. Greenwald J, Le V, Butler SL, Bushman FD, Choe S. (1999). The mobility of an HIV-1 integrase active site loop is correlated with catalytic activity. Biochemistry. 38: 8892-8898.
112. Grobler JA, Stillmock K, Hu B, Witmer M, Felock P, Espeseth AS, Wolfe A, Egbertson M, Bourgeois M, Melamed J, Wai JS, Young S, Vacca J, Hazuda DJ. (2002). Diketo acid inhibitor mechanism and HIV-1 integrase: Implications for metal binding in the active site of phosphotransferase enzymes. Proceedings of the National Academy of Sciences United States of America. 99: 6661-6666.
113. Hansen M, Bushman FD. (1997). Human immunodeficiency virus type 2 preintegration complexes: Activities in vitro and response to inhibitors. Journal of Virology. 71: 3351-3356.
114. Hansen M, Smith GJ, Kafri T, Molteni V, Siegel JS, Bushman FD. (1999). Integration complexes derived from HIV vectors for rapid assays in vitro. Nature Biotechnology. 17: 578-582.
115. Hartley O, Gaertner H, Wilken J, Thompson D, Fish R, Ramos A, Pastore C, Dufour B, Cerini F, Melotti A, Heveker N, Picard L, Alizon M, Mosier D, Kent S, Offord R. (2004). Medicinal chemistry applied to a synthetic protein: Development of highly potent HIV entry inhibitors. Proceedings of the National Academy of Sciences United States of America. 101: 16460-16465.
116. Hazuda DJ, Hastings JC, Wolfe AL, Emini EA. (1994). A novel assay for the DNA strand-transfer reaction of HIV-1 integrase. Nucleic Acids Research. 22: 1121-1122.
117. Hazuda DJ, Felock P, Witmer M, Wolfe A, Stillmock K, Grobler JA, Espeseth A, Gabryelski L, Schleif W, Blau C, Miller MD. (2000). Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells. Science. 287: 646-650.
118. Hazuda DJ, Anthony NJ, Gomez RP, Jolly SM, Wai JS, Zhuang L, Fisher TE, Embrey M, Jr. Guare JP, Egbertson MS, Vacca JP, Huff JR, Felock PJW, M. V., Stillmock KA, Danovich R, Grobler J, Miller MD, Espeseth AS, Jin L, Chen I-W, Lin JH, Kassahun K, Ellis JD, Wong BK, Xu W, Pearson PGS, W. A., Cortese R, Emini E, Summa V, Holloway MK, Young SD. (2004). A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase. Proceedings of the National Academy of Sciences United States of America. 101: 11233-11238.
119. Hazuda DJ, Young SD, Guare JP, Anthony NJ, Gomez RP, Wai JS, Vacca JP, Handt L, Motzel SL, Klein HJ, Dornadula G, Danovich RM, Witmer MV, Wilson KAA, Tussey L, Schleif WA, Gabryelski LS, Jin L, Miller MD, Casimiro DR, Emini EA, Shiver JW. (2004). Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaques. Science. 305: 528-532.
120. Hehl EA, Joshi P, Kalpana GV, Prasad VR. (2004). Interaction between human immunodeficiency virus type I reverse transcriptase and integrase proteins. Journal of Virology. 78: 5056-5067.
121. Heinzinger NK, Bukinsky MI, Haggerty SA, Ragland AM, Kewalramani V, Lee MA, Gendelman HE, Ratner L, Stevenson M, Emerman M. (1994). The vpr protein of human-immunodeficiency-virus type-1 influences nuclear-localization of viral nucleic-acids in nondiving host-cells. Proceedings of the National Academy of Sciences United States of America. 91: 7311-7315.
122. Henderson A, Bunce M, Siddon N, Reeves R, Tremethick DJ. (2000). High-mobility-group protein I can modulate binding of transcription factors to the U5 region of the human immunodeficiency virus type 1 proviral promoter. Journal of Virology. 74: 10523-10534.
123. Heuer TS, Brown PO. (1997). Mapping features of HIV-1 integrase near selected sites on viral and target DNA molecules in an active enzyme-DNA complex by photo-cross-linking. Biochemistry. 36: 10655-10665.
124. Heuer TS, Brown PO. (1998). Photo-cross-linking studies suggest a model for the architecture of an active human immunodeficiency virus type 1 integrase-DNA complex. Biochemistry. 37: 6667-6678.
125. Hindmarsh P, Ridky T, Reeves R, Andrake M, Skalka AM, Leis J. (1999). HMG protein family members stimulate human immunodeficiency virus type 1 and avian sarcoma virus concerted DNA integration in vitro. Journal of Virology. 73: 2994-3003.
126. Hwang DJ, Kim SN, Choi JH, Lee YS. (2001). Dicaffeoyl- or digalloyl pyrrolidine and furan derivatives as HIV integrase inhibitors. Bioorganic & Medicinal Chemistry. 9: 1429-1437.
127. Hwang Y, Rhodes D, Bushman F. (2000). Rapid microtiter assays for poxvirus topoisomerase, mammalian type IB topoisomerase and HIV-1 integrase: application to inhibitor isolation. Nucleic Acids Research. 28: 4884-4892.
128. Jaganatharaja J, Gowthaman R. (2006). Computational screening of inhibitors for HIV-1 integrase using a receptor based pharmacophore model. Bioinformation. 1: 112-117.
129. Jenkins TM, Hickman AB, Dyda F, Ghirlando R, Davies DR, Craigie R. (1995). Catalytic domain of human-immunodeficiency-virus type-1 integrase - identification of a soluble mutant by systematic replacement of hydrophobic residues. Proceedings of the National Academy of Sciences United States of America. 92: 6057-6061.
130. Jenkins TM, Engelman A, Ghirlando R, Craigie R. (1996). A soluble active mutant of HIV-1 integrase - Involvement of both the core and carboxyl-terminal domains in multimerization. The Journal of Biological Chemistry. 271: 7712-7718.
131. Jenkins TM, Esposito D, Engelman A, Craigie R. (1997). Critical contacts between HIV-1 integrase and viral DNA identified by structure-based analysis and photo-crosslinking. The EMBO Journal. 16: 6849-6859.
132. Jenkins Y, McEntee M, Weis K, Greene WC. (1998). Characterization of HIV-1 Vpr nuclear import: Analysis of signals and pathways. Journal of Cell Biology. 143: 875-885.
133. Jing N, Marchand C, Liu J, Mitra R, Hogan ME, Pommier Y. (2000). Mechanism of inhibition of HIV-1 integrase by G-tetrad-forming oligonucleotides in vitro. The Journal of Biological Chemistry. 275: 21460-21467.
134. John S, III Fletcher TM, Jonsson CBJ. (2005). Development and application of a high-throughput screening assay for HIV-1 integrase enzyme activities. Journal of Biomolecular Screening. 10: 606-614.
135. Johnson AA, Marchand C, Pommier Y. (2004). HIV-1 integrase inhibitors: A decade of research and two drugs in clinical trial. Current Topics in Medicinal Chemistry. 4: 1059-1077.
136. Johnson MS, McClure MA, Feng DF, Gray J, Doolittle RF. (1986). Computer-analysis of retroviral pol genes-assignment of enzymatic functions to specific sequences and homologies with nonviral enzymes. Proceedings of the National Academy of Sciences United States of America. 83: 7648-7652.
137. Jones KS, Coleman J, Merkel GW, Laue TM, Skalka AM. (1992). Retroviral integrase functions as a multimer and can turn over catalytically. The Journal of Biological Chemistry. 267: 16037-16040.
138. Jorgensen WL. (2004). The many roles of computation in drug discovery. Science. 303: 1813-1818.
139. Kalpana GV, Marmon S, Wang W, Crabtree GR, Goff SP. (1994). Binding and stimulation of HIV-1 integrase by a human homolog of yeast transcription factor SNF5. Science. 266: 2002-2006.
140. Katzman M, Mack JP, Skalka AM, Leis J. (1991). A covalent complex between retroviral integrase and nicked substrate DNA. Proceedings of the National Academy of Sciences United States of America. 88: 4695-4699.
141. Katzman M, Sudol M. (1995). Mapping domains of retroviral integrase responsible for viral-DNA specificity and target site selection by analysis of chimeras between human-immunodeficiency-virus type-1 and visna virus integrases. Journal of Virology. 69: 5687-5696.
142. Katzman M, Sudol M. (1996). Nonspecific alcoholysis, a novel endonuclease activity of human immunodeficiency virus type 1 and other retroviral integrases. Journal of Virology. 70: 2598-2604.
143. Kay J, Dunn BM. (1990). Viral proteinases - weakness in strength. Biochimica et Biophysica Acta. 1048: 1-18.
144. KeserûGM, Kolossvary I. (2001). Fully flexible low-mode docking: Application to induced fit in HIV integrase. Journal of the American Chemical Society. 123: 12708-12709.
145. Khan E, Mack JP, Katz RA, Kulkosky J, Skalka AM. (1991). Retroviral
146. King P, Ma G, Miao W, Jia Q, McDougall B, Reinecke M, Cornell C, Kuan J, Kim T, Jr. Robinson E. (1999). Structure-activity relationships: Analogues of the dicaffeoylquinic and dicaffeoyltartaric acids as potent inhibitors of human immunodeficiency virus type 1 integrase and replication. Journal of Medicinal Chemistry. 42: 497-509.
147. King PJ, Robinson WE. (1998). Resistance to the anti-human immunodeficiency virus type 1 compound L-chicoric acid results from a single mutation at amino acid 140 of integrase. Journal of Virology. 72: 8420-8424.
148. Komano J, Futahashi Y, Urano E, Miyauchi K, Murakami T, Matsuda Z, Yamamoto N. (2005). The interaction of HIV-1 with the host factors. Japanese Journal Of Infectious Diseases. 58: 125-130.
149. Krajewski K, Marchand C, Long YQ, Pommier Y, Roller PP. (2004). Synthesis and HIV-1 integrase inhibitory activity of dimeric and tetrameric analogs of indolicidin. Bioorganic & Medicinal Chemistry Letters. 14: 5595-5598.
150. Krovat EM, Steindl T, Langer T. (2005). Recent Advances in Docking and Scoring. Current Computer-Aided Drug Design. 1: 93-102.
151. Kulkosky J, Jones KS, Katz RA, Mack JP, Skalka AM. (1992). Residues critical for retroviral integrative recombination in a region that is highly conserved among retroviral retrotrasposon integrases and bacterial insertion-sequence transposases. Molecular and Cellular Biology. 12: 2331-2338.
152. Kulkosky J, Katz RA, Merkel G, Skalka AM. (1995). Activities and substrate-specificity of the evolutionarily conserved central domain of retroviral integrase. Virology. 206: 448-456.
153. Kuo C, Assefa H, Kamath S, Brzozowski Z, Slawinski J, Saczewski F, Buolamwini J, Neamati N. (2004). Application of CoMFA and CoMSIA 3D-QSAR and docking studies in optimization of mercaptobenzenesulfonamides as HIV-1 integrase inhibitors. Journal of Medicinal Chemistry. 47: 385-399.
154. Kwong PD, Wyatt R, Robinson J, Sweet RW, Sodroski J, Hendrickson WA. (1998). Structure of an HIV gp120 envelope glycoprotein in complex with the CD4 receptor and a neutralizing human antibody. Nature. 393: 648-659.
155. LaFemina RL, Graham PL, LeGrow K, Hastings JC, Wolfe A, Young SD, Emini EA, Hazuda DJ. (1995). Inhibition of human-immunodeficiency-virus integrase by bis-catechols. Antimicrobial Agents and Chemotherapy. 39: 320-324.
156. Lalezari JP, Henry K, Heran MO, Montaner JSG, Piliero PJ, Trottier B, Walmsley S, Cohen C, Kuritzkes DR, Eron JJJ, Chung J, DeMasi R, Donatacci L, Drobnes C, Delehanty J, Salgo M. (2003). Enfuvirtide, an HIV-1 fusion inhibitor, for drug-resistant HIV infection in North and South America. The New England Journal of Medicine. 348: 2175-2185.
157. Laspia MF, Rice AP, Mathews MB. (1989). HIV-1 tat protein increases transcriptional initiation and stabilizes elongation. Cell. 59: 283-292.
158. Lataillade M, Kozal MJ. (2006). The hunt for HIV-1 integrase inhibitors. AIDS patient care and STDs. 20: 489-501.
159. Leavitt AD, Shiue L, Vaarmus HE. (1993). Site-directed mutagenesis of HIV-1 integrase demonstrates differential effects on integrase functions in vitro. The Journal of Biological Chemistry. 268: 2113-2119.
160. Lee-Huang S, Huang PL, Huang PL, Bourinbaiar AS, Chen H-C, Kung H-F. (1995). Inhibition of the integrase of human-immunodeficiency-virus (HIV) type-1 by anti-HIV plant-proteins MAP30 and GAP31. Proceedings of the National Academy of Sciences United States of America. 92: 8818-8822.
161. Lee MS, Craigie R. (1998). A previously unidentified host protein protects retroviral DNA from autointegration. Proceedings of the National Academy of Sciences United States of America. 95: 1528-1533.
162. Lee SP, Han MK. (1996). Zinc stimulates Mg2+-dependent 3′-processing activity of human immunodeficiency virus type 1 integrase in vitro. Biochemistry. 35: 3837-3844.
163. Lee SP, Xiao J, Knutson JR, Lewis MS, Han MK. (1997). Zn2+ promotes the self-association of human immunodeficiency virus type-1 integrase in vitro. Biochemistry. 36: 173-180.
164. Levy JA, Hoffman AD, Kramer SM, Landis JA, Shimabukuro JM. (1984). Isolation of lymphocytopathic retroviruses from San Francisco patients with AIDS. Science. 225: 840-842.
165. Li L, Yoder K, Hansen MST, Olvera J, Miller MD, Bushman FD. (2000). Retroviral cDNA integration: Stimulation by HMG I family proteins. Journal of Virology. 74: 10965-10974.
166. Lin C-W, Engelman A. (2003). The barrier-to-autointegration factor is a component of functional human immunodeficiency virus type 1 preintegration complexes. Journal of Virology. 77: 5030-5036.
167. Lin Z, Neamati N, Zhao H, Kirsu Y, Turpin JA, Aberham C, Strbel K, Kohn K, Witvrouw M, Pannecouque C, Debyser Z, De Clercq E, Rice WG, Pommier Y, Jr. Burke TR. (1999). Chicoric acid analogues as HIV-1 integrase inhibitors. Journal of Medicinal Chemistry. 42: 1401-1414.
168. Lins RD, Briggs JM, Straatsma TP, Carlson HA, Greenwald J, Choe S, McCammon JA. (1999). Molecular dynamics studies on the HIV-1 integrase catalytic domain. Biophysical Journal. 76: 2999-3011.
169. Llano M, Delgado S, Vanegas M, Poeschla EM. (2004). Lens epithelium-derived growth factor/p75 prevents proteasomal degradation of HIV-1 integrase. The Journal of Biological Chemistry. 279: 55570-55577.
170. Llano M, Vanegas M, Fregoso O, Saenz D, Chung S, Peretz M, Poeschia EM. (2004). LEDGF/p75 determines cellular trafficking of diverse lentiviral but not murine oncoretroviral integrase proteins and is a component of functional lentiviral preintegration complexes. Journal of Virology. 78: 9524-9537.
171. Lodi PJ, Ernst JA, Kuszewski J, Hickman AB, Engelman A, Craigie R, Clore GM, Gronenborn AM. (1995). Solution structure of the DNA-binding domain of HIV-1 integrase. Biochemistry. 34: 9826-9833.
172. Long Y-Q, Jiang X-H, Dayam R, Sanchez T, Shoemaker R, Sei S, Neamati N. (2004). Rational design and synthesis of novel dimeric diketoacid-containing inhibitors of HIV-1 integrase: Implication for binding to two metal ions on the active site of integrase. Journal of Medicinal Chemistry. 47: 2561-2573.
173. Lutzke R.A, Vink C, Plasterk RH. (1994). Characterization of the minimal DNA-binding domain of the HIV integrase protein. Nucleic Acids Research. 22: 4125-4131.
174. Lutzke RA, Plasterk RA. (1998). Structure-based mutational analysis of the C-terminal DNA-Binding domain of human immunodeficiency virus type 1 integrase: Critical residues for protein oligomerization and DNA binding. Journal of Virology. 72: 4841-4848.
175. Lutzke RAP, Eppenas NA, Weber PA, Houghten RA, Plasterk RHA. (1995). Identification of a hexapeptide inhibitor of the human-immunodeficiency-virus integrase protein by using a combinatorial chemical library. Proceedings of the National Academy of Sciences United States of America. 92: 11456-11460.
176. Lyne PD. (2002). Structure-based virtual screening: an overview. Drug Discovery Today. 7: 1047-1055.
177. Maertens G, Cherepanov P, Pluymers W, Busschots K, De Clercq E, Debyser Z, Engelborghs Y. (2003). LEDGF/p75 is essential for nuclear and chromosomal targeting of HIV-1 integrase in human cells. The Journal of Biological Chemistry. 278: 33528-33539.
178. Maignan S, Guilloteau JP, Liu QZ, Mella CC, Mikol V. (1998). Crystal structures of the catalytic domain of HIV-1 integrase free and complexed with its metal cofactor: High level of similarity of the active site with other viral integrases. Journal of Molecular Biology. 282: 359-368.
179. Makhija MT, Kulkarni VM. (2001). Eigen Value Analysis of HIV-1. Integrase Inhibitors. Journal of Chemical Information and Computer Sciences. 41: 1569-1577.
180. Makhija MT, Kulkarni VM. (2001). Molecular electrostatic potentials as input for the alignment of HIV-1 integrase inhibitors in 3D QSAR. Journal of Computer-Aided Molecular Design. 15: 961-978.
181. Makhija MT, Kasliwal RT,Kulkarni VM, Neamati N.(2004). De novo design and synthesis of HIV-1 integrase inhibitors. Bioorganic & Medicinal Chemistry. 12: 2317-2333.
182. Makhija MT. (2006). Designing HIV integrase inhibitors - shooting the last arrow. Current Medicinal Chemistry. 13: 2429-2441.
183. Marchand C, Zhang X, Pais GCG, Cowansage K, Neamati N, Jr. Burke TR, Pommier Y. (2002). Structural determinants for HIV-1 integrase inhibition by beta-diketo acids. The Journal of Biological Chemistry. 277: 12596-12603.
184. Marchand C, Johnson AA, Karki RG, Pais GCG, Zhang X, Cowan-sage K, Patel TA, Nicklaus MC, Burke TRJ, Pommier Y. (2003). Metal-dependent inhibition of HIV-1 integrase by beta-diketo acids and resistance of the soluble double-mutant (F185K/C280S). Molecular Pharmacology. 64: 600-609.
185. Marchand C, Johnson AA, Semenova E, Pommier Y. (2006). Mechanisms and inhibition of HIV integration. Drug Discovery Today: Disease Mechanisms. 3: 253-260.
186. Marciniak RA, Calnan BJ, Frankel AD, Sharp PA. (1990). HIV-1 tat protein trans-activates transcription in vitro. Cell. 63: 791-802.
187. Maroun RG, Krebs D, Roshani M, Porumb H, Auclair C, Toralen F, Fermandjian S. (1999). Conformational aspects of HIV-1 integrase inhibition by a peptide derived from the enzyme central domain and by antibodies raised against this peptide. European Journal of Biochemistry. 260: 145-155.
188. Maroun RG, Gayet S, Benleulmi MS, Porumb H, Zargarian L, Merad H, Leh H, Mouscadet J-F, Troalen F, Fermandjian S. (2001). Peptide inhibitors of HIV-1 integrase dissociate the enzyme oligomers. Biochemistry. 40: 13840-13848.
189. Mason JS, Good AC, Martin EJ. (2001). 3-D Pharmacophores in drug discovery. Current Pharmaceutical Design. 7: 567-597.
190. Mazumder A, Raghavan K, Weinstein J, Kohn KW, Pommier Y. (1995). Inhibition of human-immunodeficiency-virus type-1 integrase by curcumin. Biochemical Pharmacology. 49: 1165-1170.
191. Mazumder A, Neamati N, Ojwang JO, Sunder S, Rando RF, Pommier Y. (1996). Inhibition of the human immunodeficiency virus type I integrase by guanosine quartet structures. Biochemistry. 35: 13762-13771.
192. Mazumder A, Neamati N, Pilon AA, Sunder S, Pommier Y. (1996). Chemical trapping of ternary complexes of human immunodeficiency virus type I integrase, divalent metal, and DNA substrates containing an abasic site - Implications for the role of lysine 136 in DNA binding. The Journal of Biological Chemistry. 271: 27330-27338.
193. Mazumder A, Neamati N, Sommadossi J-P, Gosselin G, Schinazi R, Imbach JL, Pommier Y. (1996). Effects of nucleotide analogues on human immunodeficiency virus type I integrase. Molecular Pharmacology. 49: 621-628.
194. Mazumder A, Wang S, Neamati N, Nicklaus M, Sunder S, Chen J, Milne GWA, Rice WG, Jr. Burke TR, Pommier Y. (1996). Antiretroviral agents as inhibitors of both human immunodeficiency virus type 1 integrase and protease. Journal of Medicinal Chemistry. 39: 2472-2481.
195. McDougall KP, Wu BW, Hostomsky Z, Reineke M, Robinsons WE. (1998). Dicaffeoylquinic and dicaffeoyltartaric acids are selective inhibitors of human immunodeficiency virus type 1 integrase. Antimicrobial Agents and Chemotherapy. 42: 140-146.
196. Meadows CD, Gervay-Hague J. (2006). Current developments in HIV chemotherapy. Chemmedchem. 1: 16-29.
197. Mekouar K, Mouscadet JF, Desmaele D, Subra F, Leh F, Savoure D, Auclair C, D'Angelo J. (1998). Styrylquinoline derivatives: A new class of potent HIV-1 integrase inhibitors that block HIV-1 replication in CEM cells. Journal of Medicinal Chemistry. 41: 2846-2857.
198. Mewshaw JP, Myrick FT, Wakefield DA, Hooper BJ, Harris JL, McCreedy B, Borroto-Esoda K. (2002). Dioxolane guanosine, the active form of the prodrug diaminopurine dioxolane, is a potent inhibitor of drug-resistant HIV-1 isolates from patients for whom standard nucleoside therapy fails. Journal of Acquired Immune Deficiency Syndromes. 29: 11-20.
199. Mighell AJ, Markham AF, Robinson PA. (1997). Alu sequences. FEBS Letters. 417: 1-5.
200. Miller MD, Farnet CM, Bushman FD. (1997). Human immunodeficiency virus type 1 preintegration complexes: Studies of organization and composition. Journal of Virology. 71: 5382-5390.
201. Miller MD, Hazuda DJ. (2004). HIV resistance to the fusion inhibitor enfuvirtide: mechanisms and clinical implications. Drug Resistance Updates. 7: 89-95.
202. Mocroft A, Vella S, Benfield TL, Chiesi A, Miller V, Gargalianos P, Monforte AdA, Yust I, Bruun JN, Phillips AN, Lundgren JD. (1998). Changing patterns of mortality across Europe in patients infected with HIV-1. Lancet. 352: 1725-1730.
203. Molteni V, Rhodes D, Rubins K, Hansen M, Bushman FD, Siegel JS. (2000). A new class of HIV-1 integrase inhibitors: The 3,3,3′,3′-tetramethyl-l, l′-spirobi(indan)-5,5′,6,6′-tetrol family. Journal of Medicinal Chemistry. 43: 2031-2039.
204. Montagnier L. (2002). Historical essay - A history of HIV discovery. Science. 298: 1727-1728.
205. Morris GM, Goodsell DS, Halliday RS, Huey R, Hart WE, Belew RK, Olson AJ. (1998). Automated docking using a Lamarckian genetic algorithm and an empirical binding free energy function. Journal of Computational Chemistry. 19: 1639-1662.
206. Mousnier A, Leh H, Mouscadet JF, Dargemont C. (2004). Nuclear import of HIV-1 integrase is inhibited in vitro by styrylquinoline derivatives. Molecular Pharmacology. 66: 783-788.
207. Mulder LCF, Muesing MA. (2000). Degradation of HIV-1 integrase by the N-end rule pathway. The Journal of Biological Chemistry. 275: 29749-29753.
208. Mulder LCF, Chakrabarti LA, Muesing MA. (2002). Interaction of HIV-1 integrase with DNA repair protein hRad18. The Journal of Biological Chemistry. 277: 27489-27493.
209. Muller G. (2003). Medicinal chemistry of target family-directed masterkeys. Drug Discovery Today. 8: 681-691.
210. Mustata GI, Brigo A, Briggs JM.(2004). HIV-1 integrase pharmacophore model derived from diverse classes of inhibitors. Bioorganic & Medicinal Chemistry Letters. 14: 1447-1454.
211. Neamati N, Hong H, Mazumder A, Wang S, Sunder S, Nicklaus MC, Milne GW, Proksa B, Pommier Y. (1997). Depsides and depsidones as inhibitors of HIV-1 integrase: Discovery of novel inhibitors through 3D database searching. Journal of Medicinal Chemistry. 40: 942-951.
212. Neamati N, Hong H, Sunder S, Milne GWA, Pommier Y. (1997). Potent inhibitors of human immunodeficiency virus type 1 integrase: Identification of a novel four-point pharmacophore and tetracyclines as novel inhibitors. Molecular Pharmacology. 52: 1041-1055.
213. Neamati N, Mazumder A, Sunder S, Owen JM, Schulz RJ, Pommier Y. (1997). 2-mercaptobenzenesulphonamides as novel inhibitors of human immunodeficiency virus type 1 integrase and replication. Antiviral Chemistry & Chemotherapy. 8: 485-495.
214. Neamati N, Mazumder A, Zhao H, Sunder S, Burke TR, Schultz RJ, Pommier Y. (1997). Diarylsulfones, a novel class of human immunodeficiency virus type 1 integrase inhibitors. Antimicrobial Agents and Chemotherapy. 41: 385-393.
215. Neamati N, Hong H, Owen JM, Sunder S, Winslow HE, Christensen JL, Zhao H, Jr. Burke TR, Milne GWA, Pommier Y. (1998). Salicylhydrazine-containing inhibitors of HIV-1 integrase: Implication for a selective chelation in the integrase active site. Journal of Medicinal Chemistry. 41: 3202-3209.
216. Neamati N, Mazumder A, Sunder S, Owen JM, Tandon M, Lown JW, Pommier Y. (1998). Highly potent synthetic polyamides, bisdistamycins, and lexitropsins as inhibitors of human immunodeficiency virus type 1 integrase. Molecular Pharmacology. 54: 280-290.
217. Neamati N, Turpin JA, Winslow HE, Christensen JL, Williamson K, Orr A, Rice WG, Pommier Y, Garofalo A, Brizzi A, Campiani G, Fiorini I, Nacci V. (1999). Thiazolothiazepine inhibitors of HIV-1 integrase. Journal of Medicinal Chemistry. 42:3334-3341.
218. Neamati N. (2001). Structure-based HIV-1 integrase inhibitor design: a future perspective. Expert Opinion in Investigational Drugs. 10: 281-296.
219. Neamati N, Lin Z, Karki RG, Orr A, Cowansage K, Strumberg D, Pais GCG, Voight JH, Nicklaus MC, Winslow HE, Zhao H, Turpin JA, Yi J, Skalka AM, Jr. Burke TR, Pommier Y. (2002). Metal-dependent inhibition of HIV-1 integrase. Journal of Medicinal Chemistry. 45: 5661-5670.
220. Ni H, Sotriffer CA, McCammon JA. (2001). Ordered water and ligand mobility in the HIV-1 integrase-5CITEP complex: A molecular dynamics study. Journal of Medicinal Chemistry. 44: 3043-3047.
221. Nicklaus MC, Neamati N, Hong H, Mazumder A, Sunder A, Chen J, Milne GWA, Pommier Y. (1997). HIV-1 integrase pharmacophore: Discovery of inhibitors through three-dimensional database searching. Journal of Medicinal Chemistry. 40: 920-929.
222. Nikitin S, Zaitseva N, Demina O, Solovieva V, Mazin E, Mikhalev S, Smolov M, Rubinov A, Vlasov P, Lepikhin D, Khachko D, Fokin V, Queen C, Zosimov V. (2005). A very large diversity space of synthetically accessible compounds for use with drug design programs. Journal of Computer-Aided Molecular Design. 19: 47-63.
223. Nunnari G, Argyris E, Fang J, Mehlman KE, Pomerantz RJ, Daniel R. (2005). Inhibition of HIV-1 replication by caffeine and caffeine-related methylxanthines. Virology. 335: 177-184.
224. O'Doherty U, Swiggard WJ, Jeyakumar D, McGain D, Malim MH. (2002). A sensitive, quantitative assay for human immunodeficiency virus type 1 integration. Journal of Virology. 76: 10942-10950.
225. O'Hara BM, Olson WC. (2002). HIV entry inhibitors in clinical development. Current Opinion in Pharmacology. 2: 523-528.
226. Ojwang JO, Buckheit RW, Pommier Y, Mazumder A, De Vreese K, EstéJ A, Reymen D, Pallansch LA, Lackman-Smith C, Wallace TL, De Clrecq E, McGrath MS, Rando RF. (1995). T30177, an oligonucleotide stabilized by an intramolecular guanosine octet, is a potent inhibitor of laboratory strains and clinical isolates of human-immunodeficiency-virus type. Antimicrobial Agents and Chemotherapy. 39: 2426-2435.
227. Ooms F. (2000). Molecular modeling and computer aided drug design. Examples of their applications in medicinal chemistry. Current Medicinal Chemistry. 7: 141-158.
228. Otto MJ. (2004). New nucleoside reverse transcriptase inhibitors for the treatment of HIV infections. Current Opinion in Pharmacology. 4: 431-436.
229. Pais GCG, Zhang X, Marchand C, Neamati N, Cowasange K, Svarovskaia ES, Pathak V, Tang Y, Nicklaus M, Pommier Y, Jr. Burke TR. (2002). Structure activity of 3-aryl-1,3-diketo-containing compounds as HIV-1 integrase inhibitors. Journal of Medicinal Chemistry. 45: 3184-3194.
230. Pani A, Marongiu ME. (2000). Anti-HIV-1 integrase drugs: How far from the shelf? Current Pharmaceutical Design. 6: 569-584.
231. Pannecouque C, Pluymers W, Van Maele B, Tetz V, Cherepanov P, De Clercq E, Witvrouw M, Debyser Z. (2002). New class of HIV integrase inhibitors that block viral replication in cell culture. Current Biology. 12: 1169-1177.
232. Parissi V, Calmels C, Soultrait VRD, Caumont A, Fournier M, Chaignepain S, Litvak S. (2001). Functional interactions of human immunodeficiency virus type 1 integrase with human and yeast HSP60. Journal of Virology. 75: 11344-11353.
233. Pemberton IK, Buckle M, Buc H. (1996). The metal ion-induced cooperative binding of HIV-1 integrase to DNA exhibits a marked preference for Mn(II) rather than Mg(II). The Journal of Biological Chemistry. 271: 1498-1506.
234. Piller SC, Caly L, Jans DA. (2003). Nuclear import of the pre-integration complex (PIC): The Achilles heel of HIV? Current Drug Targets. 4: 409-429.
235. Pluymers W, Neamati N, Pannecouque C, Fikkert V, Marchand C, Jr. Burke TR, Pommier Y, Schols D, De Clercq E, Debyser Z, Witvrouw M. (2000). Viral entry as the primary target for the anti-HIV activity of chicoric acid and its tetra-acetyl esters. Molecular Pharmacology. 58: 641-648.
236. Pluymers W, Pais G, Van Maele B, Pannecouque C, Fikkert V, Jr. Burke TR, De Clercq E, Witvrouw M, Neamati N, Debyser Z. (2002). Inhibition of human immunodeficiency virus type 1 integration by diketo derivatives. Antimicrobial Agents and Chemotherapy. 46: 3292-3297.
237. Podtelezhnikov AA, Gao K, Bushman FD, McCammon JA. (2003). Modeling HIV-1 integrase complexes based on their hydrodynamic properties. Biopolymers. 68: 110-120.
238. Pomerantz R, Horn DL. (2003). Twenty years of therapy for HIV-1 infection. Nature Medicine. 9: 867-873.
239. Pommier Y, Marchand C, Neamati N. (2000). Retroviral integrase inhibitors year 2000: update and perspectives. Antiviral Research. 47: 139-148.
240. Pommier Y, Johnson AA, Marchand C. (2005). Integrase inhibitors to treat HIV/AIDS. Nature Reviews Drug Discovery. 4: 236-248.
241. Popovic M, Read E, Gallo RC. (1984). Detection, isolation, and continuous production of cytopathic retroviruses (HTLV-III) from patients with AIDS and pre-AIDS. Science. 224: 497-500.
242. Pruss D, Bushman FD, Wolffe AP. (1994). Human-immunodeficiency-virus integrase directs integration to sites of severe DNA distortion within the nucleosome core. Proceedings of the National Academy of Sciences United States of America. 91: 5913-5917.
243. Raghavan K, Buolamwini JK, Fesen MR, Pommier Y, Kohn KW, Weintein JN. (1995). 3-Dimensional quantitative structure-activity relationship (QSAR) of HIV integrase inhibitors - A comparative molecular-field analysis (COMFA) study. Journal of Medicinal Chemistry. 38: 890-897.
244. Ramratnam B, Mittler JE, Zhang L, Boden D, Hurley A, Fang F, Macken CA, Perelson AS, Markowitz M, Ho DD. (2000). The decay of the latent reservoir of replication-competent HIV-1 is inversely correlated with the extent of residual viral replication during prolonged anti-retroviral therapy. Nature Medicine. 6: 82-85.
245. Rando RF, Ojwang J, Elbaggari A, Reyes GR, Tinder R, McGrath MS, Hogan ME. (1995). Suppression of human-immunodeficiency-virus type-1 activity in vitro by oligonucleotides which form intramolecular tetrads. The Journal of Biological Chemistry. 270: 1754-1760.
246. Reinke R, Lee DJ, Jr. Robinson WE. (2002). Inhibition of human immunodeficiency virus type 1 isolates by the integrase inhibitor L-731,988, a diketo acid. Antimicrobial Agents and Chemotherapy. 46: 3301-3303.
247. Rice P, Craigie R, Davies DR. (1996). Retroviral integrases and their cousins. Current Opinion in Structural Biology. 6: 76-83.
248. Richon AB, Young SS. An Introduction to QSAR Methodology Network Science Corporation, http://www.netsci.org/Science/Compchem/feature19.html, October 1997.
249. Rijck JD, Vandekerckhove L, Gijsbers R, Hombrouck A, Hendrix J, Vercammen J, Engelborghs Y, Christ F, Debyser Z. (2006). Overexpression of the lens epithelium-derived growth factor/p75 integrase binding domain inhibits human immunodeficiency virus replication. Journal of Virology. 80: 11498-11509.
250. Rizzuto CD, Wyatt R, Hernádez-Ramos N, Sun Y, Kwong PD, Hendrickson WA, Sodroski J. (1998). A conserved HIV gp120 glycoprotein structure involved in chemokine receptor binding. Science. 280: 1949-1953.
251. Robinson WE, Cordeiro M, Abdel-Malek S, Jia Q, Chow SA, Reinecke MG, Mitchell WM. (1996). Dicaffeoylquinic acid inhibitors of human immunodeficiency virus integrase: Inhibition of the core catalytic domain of human immunodeficiency virus integrase. Molecular Pharmacology. 50: 846-855.
252. Robinson WE, Reinecke MG, Abdel-Malek S, Jia Q, Chow SA. (1996). Inhibitors of HIV-1 replication that inhibit HPV integrase. Proceedings of the National Academy of Sciences United States of America. 93: 6326-6331.
253. Roe L, Chow SA, Brown PO. (1997). 3′-end processing and kinetics of 5′-end joining during retroviral integration in vivo. Journal of Virology. 71: 1334-1340.
254. Rowley D, Hansen M, Rhodes D, Sotriffer C, Ni H, McCammon J, Bushman F, Fenical W. (2002). Thalassiolins A-C: New marine-derived inhibitors of HIV cDNA integrase. Bioorganic & Medicinal Chemistry. 10: 3619-3625.
255. Saiz-Urra L, Gonzalez MP, Fall Y, Gomez G. (2006). Quantitative structure activity relationship studies of HIV-1 integrase inhibition. 1. GETAWAY descriptors. European Journal of Medicinal Chemistry. 1-7.
256. Sato M, Motomura T, Aramaki H, Matsuda T, Yamashita M, Ito Y, Kawakami H, Matsuzaki Y, Watanabe W, Yamataka K, Ikeda S, Kodama E, Matsuoka M, Shinkai H. (2006). Novel HIV-1 integrase inhibitors derived from quinolone antibiotics. Journal of Medicinal Chemistry. 49: 1506-1508.
257. Schames J, Henchman RH, Siegel JS, Sotriffer CA, Ni H, McCammon JA. (2004). Discovery of a novel binding trench in HIV integrase. Journal of Medicinal Chemistry. 47: 1879-1881.
258. Schneider G, Fechner U. (2005). Computer-based de novo design of drug-like molecules. Nature Reviews Drug Discovery. 4: 649-663.
259. Schrder ARW, Shinn P, Chen C, Berry C, Ecker JR, Bushman F. (2002). HIV-1 integration in the human genome favors active genes and local hotspots. Cell. 110: 521-529.
260. Sherman PA, Fyfe JA. (1990). Human Immunodeficiency Virus integration protein expressed in Escherichia coli possesses selective DNA cleaving activity. Proceedings of National Academy of Sciences United States of America. 87: 5119-5123.
261. Sherman PA, Fyfe JA. (1990). Human-immunodeficiency-virus integration protein expressed in Escherichia coli possesses selective DNA cleaving activity. Proceedings of the National Academy of Sciences United States of America. 87: 5119-5123.
262. Shibagaki Y, Chow SA. (1997). Central core domain of retroviral integrase is responsible for target site selection. The Journal of Biological Chemistry. 272: 8361-8369.
263. Siliciano JD, Kajdas J, Finzi D, Quinn TC, Chadwick K, Margolick JB, Kovacs C, Gange SJ, Siliciano RF. (2003). Long-term follow-up studies confirm the stability of the latent reservoir for HIV-1 in resting CD4(+) T cells. Nature Medicine. 9: 727-728.
264. Singh SB, Jayasuriya H, Salituro GM, Zink DL, Shafiee A, Heimbuch B, Silverman KC, Lingham RB, Genilloud O, Teran A, Vilella D, Felock P, Hazuda D. (2001). The complestatins as HIV-1 integrase inhibitors. Efficient isolation, structure elucidation, and inhibitory activities of isocomplestatin, chloropeptin I, new complestatins, A and B, and acid-hydrolysis products of chloropeptin I. Journal of Natural Products. 64: 874-882.
265. Singh SB, Herath K, Guan Z, Zink DL, Dombrowski AW, Polishook JD, Silverman KC, Lingham RB, Felock PJ, Hazuda DJ. (2002). Integramides A and B, two novel non-ribosomal linear peptides containing nine C-alpha-methyl amino acids produced by fungal fermentations that are inhibitors of HIV-1 integrase. Organic Letters. 4: 1431-1434.
266. Singh SB, Zink DL, Bills GF, Pelaez F, Teran A, Collado J, Silverman KC, Lingman RB, Felock P, Hazuda DJ. (2002). Discovery, structure and HIV-1 integrase inhibitory activities of integracins, novel dimeric alkyl aromatics from Cytonaema sp. Tetrahedron Letters. 43: 1617-1620.
267. Singh SB, Zink DL, Heimbach B, Genilloud O, Teran A, Silverman KC, Lingham RB, Felock P, Hazuda DJ. (2002). Structure, stereochemistry, and biological activity of integramycin, a novel hexacyclic natural product produced by Actinoplanes sp that inhibits HIV-1 integrase. Organic Letters. 4: 1123-1126.
268. Singh SB, Zink DL, Quamina DS, Pelaez F, Teran A, Felock P, Hazuda DJ. (2002). Integrastatins: structure and HIV-1 integrase inhibitory activities of two novel racemic tetracyclic aromatic heterocycles produced by two fungal species. Tetrahedron Letters. 43: 2351-2354.
269. Singh SB, Zink DL, Bills GF, Teran A, Silverman KC, Lingham RB, Felock P, Hazuda DJ. (2003). Four novel bis-(naphtho-gamma-pyrones) isolated from Fusarium species as inhibitors of HIV-1 integrase. Bioorganic & Medicinal Chemistry Letters. 13: 713-717.
270. Sotriffer CA, Ni H, McCammon JA. (2000). HIV-1 integrase inhibitor interactions at the active site: Prediction of binding modes unaffected by crystal packing. Journal of the American Chemical Society. 122: 6136-6137.
271. Sotriffer CA, Ni H, McCammon JA. (2000). Active site binding modes of HIV-1 integrase inhibitors. Journal of Medicinal Chemistry. 43: 4109-4117.
272. Sourgen F, Maroun RG, Frere V, Bouziane M, Auclair C, Troalen F, Fermandjian S. (1996). A synthetic peptide from the human immunodeficiency virus type-1 integrase exhibits coiled-coil properties and interferes with the in vitro integration activity of the enzyme - Correlated biochemical and spectroscopic results. European Journal of Biochemistry. 240: 765-773.
273. Stahl M, Rarey M. (2001). Detailed analysis of scoring functions for virtual screening. Journal of Medicinal Chemistry. 44: 1035-1042.
274. Stanwell C, Ye B, Yuspa SH, Burke TR. (1996). Cell protein cross-linking by Erbstatin and related compounds. Biochemical Pharmacology. 52: 475-480.
275. Steitz TA. (1998). Structural biology - A mechanism for all polymerases. Nature. 391: 231-232.
276. Steitz TA. (1999). DNA polymerases: Structural diversity and common mechanisms. The Journal of Biological Chemistry. 274: 17395-17398.
277. Svarovskaia ES, Barr R, Zhang X, Pais GCG, Marchand C, Pommier Y, Jr. Burke TR, Pathak VK. (2004). Azido-containing diketo acid derivatives inhibit human immunodeficiency virus type 1 integrase in vivo and influence the frequency of deletions at two-long-terminal-repeat-circle junctions. Journal of Virology. 78: 3210-3222.
278. Taktakishvili M, Neamati N, Pommier Y, Nair V. (2001). Discovery of a nuclease-resistant, non-natural dinucleotide that inhibits HIV-1 integrase. Bioorganic & Medicinal Chemistry Letters. 11: 1433-1435.
279. Taktakishvili M, Neamati N, Pommier Y, Pal S, Nair V. (2000). Recognition and inhibition of HIV integrase by novel dinucleotides. Journal of the American Chemical Society. 122: 5671-5677.
280. Tasara TMG, Hottiger MO, Hüscher U. (2000). HIV-1 reverse transcriptase and integrase enzymes physically interact and inhibit each other. FEBS Letters. 507: 39-44.
281. Trkola A, Dragic T, Arthos J, Binley JM, Olson WC, Allaway GP, Cheng-Mayer C, Robinson J, Maddon PJ, Moore JP. (1996). CD4-dependent, antibody-sensitive interactions between HIV-1 and its co-receptor CCR-5. Nature. 384: 184-187.
282. Turlure F, Devroe E, Silver PA, Engelman A. (2004). Human cell proteins and human immunodeficiency virus DNA integration. Frontiers in Bioscience. 9: 3187-3208.
283. van den Ent FMI, Vos A, Plasterk RHA. (1999). Dissecting the role of the N-terminal domain of human immunodeficiency virus integrase by trans-complementation analysis. Journal of Virology. 73: 3176-3183.
284. van Gent DC, Elgersma Y, Bolk MWJ, Vink C, Plasterk RHA. (1991). DNA-binding properties of the integrase proteins of human immunodeficiency viruses type-1 and type-2. Nucleic Acids Research. 19: 3821-3827.
285. van Gent DC, Groeneger AA, Plasterk RH. (1992). Mutational analysis of the integrase protein of human-immunodeficiency-virus type-2. Proceedings of the National Academy of Sciences United States of America. 89: 9598-9602.
286. van Gent DC, Vink C, Groeneger AA, Plasterk RH. (1993). Complementation between HIV integrase proteins mutated in different domains. The EMBO Journal. 12: 3261-3267.
287. Van Maele B, Busschots K, Vandekerckhove L, Christ F, Debyser Z. (2006). Cellular co-factors of HIV-1 integration. Trends in Biochemical Sciences. 31: 98-105.
288. Vandegraaff N, Kumar R, Burrell CJ, Li P. (2001). Kinetics of human immunodeficiency virus type 1 (HIV) DNA integration in acutely infected cells as determined using a novel assay for detection of integrated HIV DNA. Journal of Virology. 75: 11253-11260.
289. Vandegraaff N, Kumar R, Hocking H, Burke TRJ, Mills J, Rhodes D, Burrell CJ, Li P. (2001). Specific inhibition of human immunodeficiency virus type 1 (HIV-1) integration in cell culture: Putative inhibitors of HIV-1 integrase. Antimicrobial Agents and Chemotherapy. 45: 2510-2516.
290. Vandekerckhove L, Christ F, Maele BV, Rijck JD, Gijsbers R, Haute CVd, Witvrouw M, Debyser Z. (2006). Transient and stable knockdown of the integrase cofactor LEDGF/p75 reveals its role in the replication cycle of human immunodeficiency virus. Journal of Virology. 80: 1886-1896.
291. Vercanimen J, Maertens G, Gerard M, Clercq ED, Debyser Z, Engelborghs Y. (2002). DNA-induced polymerization of HIV-1 integrase analyzed with fluorescence fluctuation spectroscopy. The Journal of Biological Chemistry. 277: 38045-38052.
292. Vincent KA, Ellison V, Chow SA, Brown PO. (1993). Characterization of human-immunodeficiency-virus type-1 integrase expressed in escherichia-coli and analysis of variants with amino-terminal mutations. Journal of Virology. 67: 425-437.
293. Vink C, Yeheskiely E, van der Marel GA, van Boom JH, Plasterk RH. (1991). Site-specific hydrolysis and alcoholysis of human-immunodeficiency-virus DNA termini mediated by the viral integrase protein. Nucleic Acids Research. 19: 6691-6698.
294. Vink C, Oude Groeneger AAM, Plasterk RHA. (1993). Identification of the catalytic and DNA-binding region of the human-immunodeficiency-virus type-1 integrase protein. Nucleic Acids Research. 21: 1419-1425.
295. Violot S, findauthors. (2003). The human Polycomb group EED protein interacts with the integrase of human immunodeficiency virus type 1. Journal of Virology. 77: 12507-12522.
296. Vittinghoff E, Scheer S, O'Malley P, Colfax G, Holmberg SD, Buchbinder SP. (1999). Combination antiretroviral therapy and recent declines in AIDS incidence and mortality. Journal of Infectious Diseases. 179: 717-720.
297. Wai JS, Egbertson MS, Payne LS, Fisher TE, Embrey MW, Tran LO, Melamed JY, Langford HM, Guare JPJ, Zhuang L, Grey VE, Vacca JP, Holloway MK, Naylor-Olsen AM, Hazuda DJ, Felock PJ, Wolfe AL, Stillmock KA, Schleif WA, Gabryelski LJ, Young SY. (2000). 4-aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells. Journal of Medicinal Chemistry. 43: 4923-4926.
298. Wallace TL, Gamba-Vitalo C, Loveday KS, Cossum PA. (2000). Acute, multiple-dose, and genetic toxicology of AR177, an anti-HIV oligonucleotide. Toxicological Sciences. 53: 63-70.
299. Wang J-Y, Ling H, Yang W, Craigie R. (2001). Structure of a two-domain fragment of HIV-1 integrase: implications for domain organization in the intact protein. The EMBO Journal. 20: 7333-7343.
300. Wang LD, Liu C-L, Chen W-Z, Wang C-X. (2005). Constructing HIV-1 integrase tetramer and exploring influences of metal ions on forming integrase-DNA complex. Biochemical and Biophysical Research Communications. 337: 313-319.
301. Westby M, Nakayama GR, Butler SL, Blair WS. (2005). Cell-based and biochemical screening approaches for the discovery of novel HIV-1 inhibitors. Antiviral Research. 67: 121-140.
302. Witvrouw M, Van Maele B, Vercammen J, Hantson A, Engelborghs Y, De Clercq E, Pannecouque C, Debyser Z. (2004). Novel inhibitors of HIV-1 integration. Current Drug Metabolism. 5: 291-304.
303. Witvrouw M, Fikkert V, Vercammen J, Van Maele B, Engelborghs Y, Debyser Z. (2005). Identification of Authentic Inhibitors of HIV-1 Integration. Current Medicinal Chemistry: Anti-Infective Agents. 4: 153-165.
304. Wong JK, Hezareh M, Güthard HF, Havlir DV, Ignacio CC, Spina CA, Richman DD. (1997). Recovery of replication-competent HIV despite prolonged suppression of plasma viremia. Science. 278: 1291-1295.
305. Wu L, Gerard NP, Wyatt R, Choe H, Parolin C, Ruffing N, Borsetti A, Cardoso AA, Desjardin E, Newman W, Gerard C, Sodroski J. (1996). CD4-induced interaction of primary HIV-1 gp120 glycoproteins with the chemokine receptor CCR-5. Nature. 384: 179-183.
306. Yang W, Steitz TA. (1995). Recombining the structures of HIV integrase, RuvC and RNase-H. Structure. 3: 131-134.
307. Yang ZN, Mueser TC, Bushman FD, Hyde CC. (2000). Crystal structure of an active two-domain derivative of Rous sarcoma virus integrase. Journal of Molecular Biology. 296: 535-548.
308. Yi J, Arthur JW, Dunbrack RLJ, Skalka AM. (2000). An inhibitory monoclonal antibody binds at the turn of the helix-turn-helix motif in the N-terminal domain of HIV-1 integrase. The Journal of Biological Chemistry. 275: 38739-38748.
309. Yi J, Cheng H, Andrake MD, Dunbrack RLJ, Roder H, Skalka AM. (2002). Mapping the epitope of an inhibitory monoclonal antibody to the C-terminal DNA-binding domain of HIV-1 integrase. The Journal of Biological Chemistry. 277: 12164-12174.
310. Yoder KE, Bushman FD. (2000). Repair of gaps in retroviral DNA integration intermediates. Journal of Virology. 74: 11191-11200.
311. Yung E, Sorin M, Pal A, Craig E, Morozov A, Delattre O, Kappes J, Ott D, Kalpana GV. (2001). Inhibition of HIV-1 virion production by a transdominant mutant of integrase interactor 1. Nature Medicine. 7: 920-926.
312. Yung E, Sorin M, Wang E-J, Perumal S, Ott D, Kalpana GV. (2004). Specificity of interaction of INI1/hSNF5 with retroviral integrases and its functional significance. Journal of Virology. 78: 2222-2231.
313. Zhang X, Pais GCG, Svarovskaia ES, Marchand C, Johnson AA, Karki RG, Nicklaus MC, Pathak VK, Pommier Y, Burke TRJ. (2003). Azido-containing aryl beta-diketo acid HIV-1 integrase inhibitors. Bioorganic & Medicinal Chemistry Letters. 13: 1215-1219.
314. Zhang X, Marchand C, Pommier Y, Burke TRJ. (2004). Design and synthesis of photoactivatable aryl diketo acid-containing HIV-1 integrase inhibitors as potential affinity probes. Bioorganic & Medicinal Chemistry Letters. 14: 1205-1207.
315. Zhao H, Neamati N, Hong H, Mazumder A, Wang S, Sunder S, Milne GWA, Pommier Y, Burke RB. (1997). Coumarin-based inhibitors of HIV integrase. Journal of Medicinal Chemistry. 40: 242-249.
316. Zhao H, Neamati N, Mazumder A, Sunder S, Pommier Y, Burke TR. (1997). Arylamide inhibitors of HIV-1 integrase. Journal of Medicinal Chemistry. 40: 1186-1194.
317. Zhao L, O'Reilly MK, Shultz MD, Chmielewski. (2003). Interfacial peptide inhibitors of HIV-1 integrase activity and dimerization. Bioorganic & Medicinal Chemistry Letters. 13: 1175-1177.
318. Zheng R, Jenkins TM, Craigie R. (1996). Zinc folds the N-terminal domain of HIV-1 integrase, promotes multimerization, and enhances catalytic activity. Proceedings of the National Academy of Sciences United States of America. 93: 13659-13664.
319. Zhu K, Dobard C, Chow SA. (2004). Requirement for integrase during reverse transcription of human immunodeficiency virus type 1 and the effect of cysteine mutations of integrase on its interactions with reverse transcriptase. Journal of Virology. 78: 5045-5055.
320. Zhu T, Muthui D, Holte S, Nickle D, Feng F, Brodie S, Hwangboo Y, Mullins JI, Corey L. (2002). Evidence for human immunodeficiency virus type 1 replication in vivo in CD14(+) monocytes and its potential role as a source of virus in patients on highly active antiretroviral therapy. Journal of Virology. 76: 707-716.
321. Zhuang L, Wai JS, Embrey MW, Fisher TE, Egbertson MS, Payne LS, Guare JPJ, Vacca JP, Hazuda DJ, Felock PJ, Wolfe AL, Stillmock KA, Witmer MV, Moyer G, Schleif WA, Gabryelski LJ, Leonard YM, Lynch JJJ, Michelson SR, Young SD. (2003). Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells. Journal of Medicinal Chemistry. 46: 453-456.
322. Zouhiri F, Mouscadet JF, Mekouar K, Desmaele D, Savoure D, Leh H, Subra F, Le Bret M, Auclair C, D'Angelo J. (2000). Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture. Journal of Medicinal Chemistry. 43: 1533-1540.