Antisense oligonucleotides: Is the glass half full or half empty?

Biochemical Pharmacology

Volumn 55, Issue 1, 1998, Pages 9-19

  Bennett, C F ^a  

^a ISIS PHARMACEUTICALS   (United States)

Author keywords

Antisense oligonucleotides; Nucleic acids; Pharmacokinetics; Pharmacology; Toxicology

Indexed keywords

ANTISENSE OLIGONUCLEOTIDE; OLIGODEOXYNUCLEOTIDE PHOSPHOROTHIOATE;

DRUG BIOAVAILABILITY; DRUG TARGETING; GENE EXPRESSION; HUMAN; NONHUMAN; PRIORITY JOURNAL; REVIEW; RNA HYBRIDIZATION; RNA SYNTHESIS;

EID: 0031912506     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(97)00214-1     Document Type: Note

References (123)

1. S.T. Crooke Therapeutic applications of oligonucleotides Annu Rev Pharmacol Toxicol 32 1992 329 376
2. C.A. Stein Y-C Cheng Antisense oligonucleotides as therapeutic agents-Is the bullet really magical? Science 261 1993 1004 1012
3. S.T. Crooke C.F. Bennett Progress in antisense oligonucleotide therapeutics Annu Rev Pharmacol Toxicol 36 1996 107 129
4. H.W. Sharma R Narayanan The therapeutic potential of antisense oligonucleotides Bioessays 17 1995 1055 1063
5. C.A. Stein A.M. Krieg Problems in interpretation of data derived from in vitro and in vivo use of antisense oligodeoxynucleotides Antisense Res Dev 4 1994 67 69
6. C.A. Stein Does antisense exist? Nature Med 1 1995 1119 1121
7. E De Clercq F Eckstein T.C. Merigan Interferon induction increased through chemical modification of synthetic polyribonucleotide Science 165 1969 1137 1140
8. 1 Biochemistry 11 1972 3507 3512
9. R.L. Letsinger P.S. Miller Protecting groups for nucleosides used in synthesizing oligonucleotides J Am Chem Soc 91 1969 3356 3359
10. P.S. Miller J Yano E Yano C Carroll K Jayaraman P.O.P. Ts'o Nonionic nucleic acid analogues. Synthesis and characterization of dideoxyribonucleoside methylphosphonates Biochemistry 18 1979 5134 5143
11. K Jayaraman K McParland P Miller P.O.P. Ts'o Selective inhibition of Escherichia coli protein synthesis and growth by nonionic oligonucleotides complementary to the 3′ end of 16S rRNA Proc Natl Acad Sci USA 78 1981 1537 1541
12. J-R Bertrand J-L Imbach C Paoletti C Malvy Comparative activity of α- and β-anomeric oligonucleotides on rabbit β globin synthesis: Inhibitory effect of cap targeted α-oligonucleotides Biochem Biophys Res Commun 164 1989 311 318
13. W.S. Marshall M.H. Caruthers Phosphorodithioate DNA as a potential therapeutic drug Science 259 1993 1564 1570
14. A.M. Iribarren B.S. Sproat P Neuner I Sulston U Ryder AI Lamond 2′-O-Alkyl oligoribonucleotides as antisense probes Proc Natl Acad Sci USA 87 1990 7747 7751
15. K-H Altmann N.M. Dean D Fabbro S.M. Freier T Geiger R Haner D Husken P Martin B.P. Monia M Muller F Natt P Nicklin J Phillips U Pieies H Sasmor H.E. Moser Second generation of antisense oligonucleotides: From nuclease resistance to biological efficacy in animals Chimia 50 1996 168 176
16. L.L. Cummins S.R. Owens L.M. Risen E.A. Lesnik S.M. Freier D McGee C.J. Guinosso P.D. Cook Characterization of fully 2′-modified oligoribonucleotide hetero- and homoduplex hybridization and nuclease sensitivity Nucleic Acids Res 23 1995 2019 2024
17. R.A. McKay L.L. Cummins M.J. Grabam E.A. Lesnik S.R. Owens M Winniman N.M. Dean Enhanced activity of an antisense oligonucleotide targeting murine protein kinase C-α by the incorporation of 2′-O-propyl modifications Nucleic Acid Res 24 1996 411 417
18. R Alul G.D. Hoke (2′-5′)-Oligo-3′-deoxynucleotides: Selective binding to single-stranded RNA but not DNA Antisense Res Dev 5 1995 3 11
19. F Debart J-J Vasseur Y.S. Sanghvi P.D. Cook Synthesis and incorporation of methyleneoxyl (methylimino) linked thymidine dimer into antisense oligonucleotides Bioorg Med Chem Lett 2 1992 1479 1482
20. M Matteucci K-Y Lin S Butcher C Moulds Deoxyoligonucleotides bearing neutral analogues of phosphodiester linkages recognize duplex DNA via triple-helix formation J Am Chem Soc 113 1991 7767 7768
21. S.M. Gryaznov D.H. Lloyd J-K Chen R.G. Schultz L.A. DeDionisio L Ratmeyer W.D. Wilson Oligonucleotide N3′ → P5′ phosphoramidates Proc Natl Acad Sci USA 92 1995 5798 5802
22. A De Mesmaeker A Waldner J Lebreton V Fritsch R.M. Wolf Novel backbone replacements for oligonucleotides Carbohydrate Modifications in Antisense Research Y.S. Sanghvi P.D. Cook ACS Symposium Series No. 580 1994 American Chemical Society Washington, DC 24 39
23. P.E. Nielsen M Egholm R.H. Berg O Buchardt Sequence-selective recognition of DNA by strand displacement with a thymine-substituted polyamide Science 254 1991 1497 1500
24. N.M. Dean R McKay T.P. Condon C.F. Bennect Inhibition of protein kinase C-α expression in human A549 cells by antisense oligonucleotides inhibits induction of intercellular adhesion molecule 1 (ICAM-1) mRNA by phorbol esters J Biol Chem 269 1994 16416 16424
25. B.P. Monia J.F. Johnston H Sasmor L.L. Cummins Nuclease resistance and antisense activity of modified oligonucleotides targeted to Ha- ras J Biol Chem 271 1996 1453314540
26. S.T. Crooke M.J. Grabam J.E. Zuckerman D Brooks B.S. Conklin L.L. Cummins M.J. Greig C.J. Guinosso D Kornbrust M Manoharan H.M. Sasmor T Schleich K.L. Tivel R.H. Griffey Pharmacokinetic properties of several novel oligonucleotide analogs in mice J Pharmacol Exp Ther 277 1996 923 937
27. R Zhang R.B. Diasio Z Lu T Liu Z Jiang W.M. Galbraith S Agrawal Pharmacokinetics and tissue distribution in rats of an oligodeoxynucleotide phosphorothioate (GEM 91) developed as a therapeutic agent for human immunodeficiency virus type-1 Biochem Pharmacol 49 1995 929 939
28. 14C-labeled phosphorothioate oligonucleotide ISIS 2105 after intravenous administration to rats J Pharmacol Exp Ther 267 1993 1181 1190
29. R Zhang Z Lu H Zhao X Zhang R.B. Diasio I Habus Z Jiang R.P. Iyer D Yu S Agrawal In vivo stability, disposition and metabolism of a “hybrid” oligonucleotide phosphorothioate in rats Biochem Pharmacol 50 1995 545 556
30. R Zhang R.P. Iyer D Yu W Tan X Zhang Z Lu H Zhao S Agrawal Pharmacokinetics and tissue distribution of a chimeric oligodeoxynucleoside phosphorothioate in rats after intravenous administration J Pharmacol Exp Ther 278 1996 971 979
31. S Agrawal J Temsamani J.Y. Tang Pharmacokinetics, biodistribution, and stability of oligodeoxynucleotide phosphorothioates in mice Proc Natl Acad Sci USA 88 1991 7595 7599
32. 14C-labeled phosphorothioate oligonucleotide, ISIS 2105, after intradermal administration to rats J Pharmacol Exp Ther 269 1994 89 94
33. 3H-labeled oligonucleotides. I. Comparison of a phosphodiester and a phosphorothioate Mol Pharmacol 45 1994 932 943
34. S.K. Srinivasan P Iversen Review of in vivo pharmacokinetics and toxicology of phosphorothioate oligonucleotides J Clin Lab Anal 9 1995 129 137
35. F Plenat N Klein-Monhoven B Marie J-M Vignaud A Duprez Cell and tissue distribution of synthetic oligonucleotides in healthy and tumor-bearing nude mice Am J Pathol 147 1995 124 135
36. A Rifai W Brysch K Fadden J Clark K-H Schlingensiepen Clearance kinetics, biodistribution, and organ saturability of phosphorothioate oligodeoxynucleotides in mice Am J Pathol 149 1996 717 725
37. Butler M, Stecker K and Bennett CF, Histological localization of phosphorothioate oligodeoxynucleotides in normai rodent tissue. Nucleosides Nucleotides , in press.
38. R Oberbauer G.F. Schreiner T.W. Meyer Renal uptake of an 18-mer phosphorothioate oligonucleotide Kidney Int 48 1995 1226 1232
39. Y Shoji S Akhtar A Periasamy B Herman R.L. Juliano Mechanism of cellular uptake of modified oligodeoxynucleotides containing methylphosphonate linkages Nucleic Acids Res 19 1991 5543 5550
40. S.L. Loke C.A. Stein X.H. Zhang K Mori M Nakanishi C Subasinghe J.S. Cohen L.M. Neckers Characterization of oligonucleotide transport into living cells Proc Natl Acad Sci USA 86 1989 3474 3478
41. C.A. Stein J.L. Tonkinson L-M Zhang L Yakubov J Gervasoni R Taub S.A. Rotenberg Dynamics of the internalization of phosphodiester oligodeoxynucleotides in HL60 cells Biochemistry 32 1993 4855 4861
42. C.F. Bennett M-Y Chiang H Chan J.E.E. Shoemaker C.K. Mirabelli Cationic lipids enhance cellular uptake and activity of phosphorothioate antisense oligonucleotides Mol Pharmacol 41 1992 1023 1033
43. S Wu-Pong T.L. Weiss C.A. Hunt Calcium dependent cellular uptake of a c- myc antisense oligonucleotide Cell Mol Biol 40 1994 843 850
44. F.O. Nestle R.S. Mitra C.F. Bennett H Chan B.J. Nickoloff Cationic lipid is not required for uptake and selective inhibitory activity of ICAM-1 phosphorothioate antisense oligonucleotides in keratinocytes J Invest Dermatol 103 1994 569 575
45. S.B. Noonberg M.R. Garovoy C.A. Hunt Characteristics of oligonucleotide uptake in human keratinocyte cultures J Invest Dermatol 101 1993 727 731
46. R.M. Crooke M.J. Graham M.E. Cooke S.T. Crooke In vitro pharmacokinetics of phosphorothioate antisense oligonucleotides J Pharmacol Exp Ther 275 1995 462 473
47. N.M. Dean R McKay Inhibition of protein kinase C-α expression in mice after systemic administration of phosphorothioate antisense oligodeoxynucleotides Proc Natl Acad Sci USA 91 1994 11762 11766
48. T Yazaki S Ahmad A Chahlavi E Zylber-Katz N.M. Dean S.D. Rabkin R.L. Martuza R.I. Glazer Treatment of glioblastoma U-87 by systemic administration of an antisense protein kinase C-α phosphorothioate oligodeoxynucleotide Mol Pharmacol 50 1996 236 242
49. N Dean R McKay L Miraglia R Howard S Cooper J Giddings P Nicklin L Meister R Ziel T Geiger M Muller D Fabbro Inhibition of growth of human tumor cell lines in nude mice by an antisense oligonucleotide inhibitor of protein kinase C-a expression Cancer Res 56 1996 3499 3507
50. B.P. Monia J.F. Johnston T Geiger M Muller D Fabbro Antitumor activity of a phosphorothioate oligodeoxynucleotide targeted against C- raf kinase Nature Med 2 1995 668 675
51. T Kumasaka W.M. Quinlan N.A. Doyle T.P. Condon J Sligh F Takei A.L. Beaudet C.F. Bennett C.M. Doerschuk The role of the intercellular adhesion molecule-1 (ICAM-1) in endotoxin-induced pneumonia evaluated using ICAM-1 antisense oligonucleotides, anti-ICAM-1 monoclonal antibodies, and ICAM-1 mutant mice J Clin Invest 97 1996 2362 2369
52. M Nesterova Y.S. Cho-Chung A single-injection protein kinase A-directed antisense treatment to inhibit tumor growth Nature Med 1 1995 528 533
53. M.F. Neurath S Pettersson K-H Meyerzum Büschenfelde W Strober Local administration of antisense phosphorothioate oligonucleotides to the p65 subunit of NF-KB abrogates established experimental colitis in mice Nature Med 2 1996 998 1004
54. E Noiri T Peresleni F Miller M.S. Goligorsky In vivo targeting of inducible NO synthase with oligodeoxynucleotides protects rat kidney against ischemia J Clin Invest 97 1996 2377 2383
55. M Christofidou-Solomidou S.M. Albelda F.C. Bennett G.F. Murphy Experimental production and modulation of human cytotoxic dermatitis in human-murine chimeras Am J Pathol 150 1997 631 639
56. C.F. Bennett D Kornbrust S Henry K Stecker R Howard S Cooper S Dutson W Hall H.I. Jacoby An ICAM-1 antisense oligonucleotide prevents and reverses dextran sulfate sodiutn-induced colitis in mice J Pharmacol Exp Ther 280 1997 988 1000
57. C Helene J-J Toulme Specific regulation of gene expression by antisense, sense and antigene nucleic acids Biochim Biophys Acta 1049 1990 99 125
58. C.F. Bennett S.T. Crooke Regulation of endothelial cell adhesion molecule expression with antisense oligonucleotides Adv Pharmacol 28 1994 1 43
59. S.T. Crooke Therapeutic Applications of Oligonucleotides 1995 R.G. Landes Co Austin
60. A.J. Stewart Y Canitrot E Baracchini N.M. Dean R.G. Deeley S.P.C. Cole Reduction of expression of the multidrug resistance protein, MRP, in human tumor cells by antisense phosphorothioate oligonucleotides Biochem Pharmacol 51 1996 461 469
61. T.P. Condon C.F. Bennett Altered mRNA splicing and inhibition of human E-selectin expression by an antisense oligonucleotide in human umbilical vein endothelial cells J Biol Chem 271 1996 30398 30403
62. R.V. Giles D.G. Spiller D.M. Tidd Detection of ribonuclease H-generated mRNA fragments in human leukemia cells following reversible membrane permeabilization in the presence of antisense oligodeoxynucleotides Antisense Res Dev 5 1995 23 31
63. M-Y Chiang H Chan M.A. Zounes S.M. Freier W.F. Lima C.F. Bennett Antisense oligonucleotides inhibit intercellular adhesion molecule l expression by two distinct mechanisms J Biol Chem 266 1991 18162 18171
64. B.P. Monia E.A. Lesnik C Gonzalez W.F. Lima D McGee C.J. Guinosso A.M. Kawasaki P.D. Cook S.M. Freier Evaluation of 2′-modified oligonucleotides containing 2′deoxy gaps as antisense inhibitors of gene expression J Biol Chem 268 1993 14514 14522
65. P.F. Torrence R.K. Maitra K Lesiak S Khamnei A Zhou R.H. Silverman Targeting RNA for degradation with a (2′-5′) oligoadenylate-antisense chimera Proc Natl Acad Sci USA 90 1993 1300 1304
66. P Lengyel J.F. Speyer S Ochoa Synthetic polynucleotides and the amino acid code Proc Natl Acad Sci USA 47 1961 1936 1942
67. B.F. Baker S.F. Lot T.P. Condon S Cheng-Flournoy E Lesnik H.M. Sasmor C.F. Bennett 2′-O-(2-Methoxy)ethyl modified anti-ICAM-1 oligonucleotides selectively increase the ICAM-1 mRNA Ievel and inhibit formation of the ICAM-1 translation initiation complex in HUVECs J Biol Chem 272 1997 11994 12000
68. H Sierakowska M.J. Sambade S Agrawal R Kole Repair of thalassemic human β-globin mRNA in mammalian cells by antisense oligonucleotides Proc Natl Acad Sci USA 93 1996 12840 12844
69. D Hodges S.T. Crooke Inhibition of splicing of wild-type and mutated luciferase-adenovirus pre-mRNA by antisense oligonucleotides Mol Pharmacol 48 1995 905 918
70. C.F. Bennett T Condon S Grimm H Chan M-Y Chiang Inhibition of endothelial cell-leukocyte adhesion molecule expression with antisense oligonucleotides J Immunol 152 1994 3530 3540
71. B.P. Monia J.F. Johnston D.J. Ecker M.A. Zounes W.F. Lima S.M. Freier Selective inhibition of mutant Ha- ras mRNA expression by antisense oligonucleotides J Biol Chem 267 1992 19954 19962
72. B.P. Monia J.F. Johnston T Geiger M Muller D Fabbro Antitumor activity of a phosphorothioate antisense oligodeoxynucleotide targeted against C- raf kinase Nature Med 2 1996 668 675
73. B.P. Monia H Sasmor J.F. Johnston S.M. Freier E.A. Lesnik M Muller T Geiger K-H Altmann H Moser D Fabbro Sequence-Specific antitumor activity of a phosphorothioate oligodeoxyribonucleotide targeted to human C- raf kinase supports an antisense mechanism of action in vivo Proc Natl Acad Sci USA 93 1996 15481 15484
74. 1 cells J Biol Chem 268 1993 21875 21882
75. A Colige B.P. Sokolov P Nugent R Baserga D.J. Prockop Use of an antisense oligonucleotide to inhibit expression of a mutated human procollagen gene (COL1A1) in transfected mouse 3T3 cells Biochemistry 32 1993 7 11
76. R.W. Wagner M.D. Matteucci J.G. Lewis A.J. Gutierrez C Moulds B.C. Froehler Antisense gene inhibition by oligonucleotides containing C-5 propyne pyrimidines Science 260 1993 1510 1513
77. S.D. Fenster R.W. Wagner B.C. Froehler D.J. Chin Inhibition of human immunodeficiency virus type-l env expression by C-5 propyne oligonucleotides specific for rev-response element stem-loop V Biochemistry 33 1994 83918398
78. J.L. Duff B.P. Monia B.C. Berk Mitogen-activated protein (MAP) kinase is regulated by the MAP kinase phosphatase (MKP-1) in vascular smooth muscle cells. Effect of actinomycin D and antisense oligonucleotides J Biol Chem 270 1995 7161 7166
79. R.W. Wagner M.D. Matteucci D Grant T Huang B.C. Froehler Potent and selective inhibition of gene expression by an antisense heptanucleotide Nature Biotech 14 1996 840 844
80. M Matteucci Structural modifications toward improved antisense oligonucleotides Perspect Drug Dis Des 4 1996 1 16
81. A.M. Kawasaki M.D. Casper S.M. Freier E.A. Lesnik M.C. Zounes L.L. Cummins C Gonzalez P.D. Cook Uniformly modified 2′-deoxy-2′-fluoro phosphorothioate oligonucleotides as nuclease-resistant antisense compounds with high affinity and specificity for RNA targets J Med Chem 36 1993 831 841
82. B.J. Blencowe B.S. Sproat U Ryder S Barabino A.I. Lamond Antisense probing of the human U4/U6 snRNP with biotinylated 2′-OMe RNA oligonucleotides Cell 59 1989 531 539
83. E.A. Lesnik C.J. Guinosso A.M. Kawasaki H Sasmor M Zounes L.L. Cummins D.J. Ecker P.D. Cook S.M. Freier Oligodeoxynucleotides containing 2′-O-modified adenosine: Synthesis and effects on stability of DNA:RNA duplexes Biochemistry 32 1993 7832 7838
84. Y.S. Sanghvi Heterocyclic base modifications in nucleic acids and their applications in antisense oligonucleotides S.T. Crooke B Lebleu Antisense Research and Applications 1993 CRC Press Boca Raton 273 288
85. K.S. Ramasamy M Zounes C Gonzalez S.M. Freier E.A. Lesnik L.L. Cummins R.H. Griffey B.P. Monia P.D. Cook Remarkable enhancement of binding affinity of heterocyclemodified DNA to DNA and RNA. Synthesis, characterization and biophysical evaluation of N 2-imidazolylpropylguanine and N 2-imidazolylpropyl-2-aminoadenine modified oligonucleotides Tetrahedron Lett 35 1994 215 218
86. I.V. Kutyavin R.L. Rhinehart E.A. Lukhtanov V.V. Gorn R.B. Myer H.B. Gamper Oligonucleotides containing 2-aminoadenine and 2-thiothymine act as selectively binding complementary agents Biochemistry 35 1996 11170 11176
87. R.J. Jones K-Y Lin J.F. Milligan S Wadwani M.D. Matteucci Synthesis and binding properties of pyrimidine oligodeoxynucleoside analogs containing neutral phosphodiester replacements. The formacetal and 3′-thioformacetal internucleoside linkages J Org Chem 58 1993 2983 2991
88. J-J Vasseur F Debart Y.S. Sanghvi P.D. Cook Oligonucleosides: Synthesis of a novel methylhydroxylaminelinked nucleoside dimer and its incorporation into antisense sequences J Am Chem Soc 114 1992 4006 4007
89. A De Mesmaeker A Waldner J Lebreton P Hoffmann V Fritsch R.M. Wolf S.M. Freier Amides as a new type of backbone modification in oligonucleotides Angew Chem Int Ed 33 1994 226 229
90. C Meier J.W. Engels Peptide nucleic acids (PNAs)Unusual properties of nonionic oligonucleotide analogues Angew Chem Int Edn 31 1992 1008 1010
91. M Egholm O Buchardt L Christensen C Behrens S.M. Freier D.A. Driver R.H. Berg S.K. Kim B Norden P.E. Nielsen PNA hybridizes to complementary oligonucleotides obeying the Watson-Crick hydrogen-bonding rules Nature 365 1993 566 568
92. C Helene J-J Toulme Control of gene expression by oligonucleotides covalently linked to intercalating agents and nucleic acid-cleaving reagents J.S. Cohen Oligonucleotides: Antisense Inhibitors of Gene Expression 1989 CRC Press Boca Raton 137 172
93. J Goodchild E Carroll III J.R. Greenberg Inhibition of rabbit β-globin synthesis by complementary oligonucleotides: Identification of mRNA sites sensitive to inhibition Arch Biochem Biophys 263 1988 401 409
94. T.A. Bacon E Wickstrom Walking along human c- myc mRNA with antisense oligodeoxynucleotides: Maximum efficacy at the 5′ cap region Oncogene Res 6 1991 13 19
95. W.F. Lima V Brown-Driver M Fox R Hanecak T.W. Bruice Combinatorial screening and rational optimization for hybridization to folded hepatitis C virus RNA of oligonucleotides with biological antisense activity J Biol Chem 272 1997 626 638
96. W.F. Lima B.P. Monia D.J. Ecker S.M. Freier Implication of RNA structure on antisense oligonucleotide hybridization kinetics Biochemistry 31 1992 12055 12061
97. W-Y Gao F-S Han C Storm W Egan Y-C Cheng Phosphorothioate oligonucleotides are inhibitors of human DNA polymerases and RNase H: Implications for antisense technology Mol Pharmacol 41 1992 223 229
98. J.R. Perez Y Li C.A. Stein S Majumder A Van Oorschot R Narayanan Sequence-independent induction of Sp1 transcription factor activity by phosphorothioate oligodeoxynucleotides Proc Natl Acad Sci USA 91 1994 5957 5961
99. M.A. Guvakova L.A. Yakubov I Vlodavsky J.L. Tonkinson C.A. Stein Phosphorothioate oligodeoxynucleotides bind to basie fibroblast growth factor, inhibit its binding to cell surface receptors, and remove it from low affinity binding sites on extracellular matrix J Biol Chem 270 1995 2620 2627
100. 2 enzyme activity by phosphorothioate oligonucleotides Nucleic Acids Res 22 1994 3202 3209
101. T.L. Burgess E.F. Fisher S.L. Ross J.V. Bready Y Qian L.A. Bayewitch A.M. Cohen C.J. Herrera S.S.-F Hu T.B. Kramer F.D. Lott F.H. Martin G.F. Pierce L Simonet C.L. Farrell The antiproliferative activity of c-myb and c-myc antisense oligonucleotides in smooth muscle cells is caused by a nonantisense mechanism Proc Natl Acad Sci USA 92 1995 4051 4055
102. A.M. Krieg A-K Yi S Matson T.J. Waldschmidt G.A. Bishop R Teasdale G.A. Koretzky D.M. Klinman CpG motifs in bacterial DNA trigger direct B-cell activation Nature 374 1995 546 549
103. L.C. Bock L.C. Griffin J.A. Latham E.H. Vermaas J.J. Toole Selection of single-stranded DNA molecules that bind and inhibit human thrombin Nature 355 1992 564 566
104. A.D. Ellington J.W. Szostak Selection in vitro of singlestranded DNA molecules that fold into specific ligandbinding structures Nature 355 1992 850 852
105. A.D. Ellington Aptamers achieve the desired recognition Curr Biol 4 1994 427 429
106. L Benimetskaya J.L. Tonkinson M Koziolkiewicz B Karwowski P Guga R Zeltser W Stec C.A. Stein Binding of phosphorothioate oligodeoxynucleotides to basie fibroblast growth factor, recombinant soluble CD4, laminin and fibronectin is P-chirality independent Nucleic Acids Res 23 1995 4239 4245
107. C.A. Stein Phosphorothioate antisense oligodeoxynucleotides: Questions of specificity Trends Biotechnol 14 1996 147 149
108. J-Y Maltese H.W. Sharma L Vassilev R Narayanan Sequence context of antisense RelA/NF-κB phosphorothioates determines specificity Nucleic Acids Res 23 1995 1146 1151
109. J.R. Williamson Guanine quartets Curr Opin Struct Biol 3 1993 357 362
110. Z.K. Ballas W.L. Rasmussen A.M. Krieg Induction of NK activity in murine and human cells by CpG motifs in oligodeoxynucleotides and bacterial DNA J Immunol 157 1996 1840 1845
111. D.K. Monteith S.P. Henry R.B. Howard S Flournoy A.A. Levin C.F. Bennett S.T. Crooke Immune stimulation-A class effect of phosphorothioate oligonucleotides in rodents Anticancer Drug Des 12 1997 421 432
112. Levin AA, Monteith DK, Leeds JM, Nicklin PL, Geary RS, Butler M, Templin MV and Henry SP, Toxicity of oligodeoxynucleotide therapeutic agents. In: Antisense Research and Applications (Ed. Crooke ST). Springer, Heidelberg, in press.
113. T Geiser Large-scale economic synthesis of antisense phosphorothioate analogues of DNA for preclinical investigations Ann NY Acad Sci 616 1990 173 183
114. S Agrawal X Zhang Z Lu H Zhao J.M. Tamburin J Yan H Cai R.B. Diasio I Habus Z Jiang R.P. Iyer D Yu R Zhang Absorption, tissue distribution and in vivo stability in rats of a hybrid antisense oligonucleotide following oral administration Biochem Pharmacol 50 1995 571 576
115. R.L. Letsinger G.R. Zhang D.K. Sun T Ikeuchi P.S. Sarin Cholesteryl-conjugated oligonucleotides: Synthesis, properties, and activity as inhibitors of replication of human immunodeficiency virus in cell culture Proc Natl Acad Sci USA 86 1989 6553 6556
116. S.K. Alahari N.M. Dean M.H. Fisher R Delong M Manoharan K.L. Tivel R.L. Juliano Inhibition of expression of the multidrug resistance-associated P-glycoprotein by phosphorothioate and 5′-cholesterol-conjugated phosphorothioate antisense oligonucleotides Mol Pharmacol 50 1996 808 819
117. 3H]labeled phosphorothioate oligonucleotide formulated in the presence and absence of a cationic lipid J Control Rel 41 1996 121 130
118. E.M. Southern DNA fingerprinting by hybridization to oligonucleotide arrays Electrophoresis 16 1995 1539 1542
119. R Geary J Leeds S.P. Henry D.K. Monteith A.A. Levin Antisense oligonucleotide inhibitors for the treatment of cancer: l) Pharmacokinetic properties of phosphorothioate oligodeoxynucleotides Anticancer Drug Des 12 1997 383 393
120. Q Zhao J Temsamani P.L. Iadarola Z Jiang S Agrawal Effect of different chemically modified oligodeoxynucleotides on immune stimulation Biochem Pharmacol 51 1996 173 182
121. Boggs RT, McGraw K, Condon T, Flournoy S, Villiet P, Bennett CF and Monia BP, Characterization and modulation of immune stimulation by modified oligonucleotides. Antisense Nucleic Acid Drug Dev, in press.
122. S Kumar H.K. Tewary P.L. Iversen Characterization of binding sites, extent of binding, and drug interactions of oligonucleotides with albumin Antisense Res Dev 5 1995 131 139
123. W.H. Gmeiner P Sahasrabudhe R.T. Pon J Sonntag S Srinivasan P.L. Iversen Preparation of oligomeric 2′-deoxy5-fluorouridylate of defined length and backbone composition: A novel pro-drug form of the potent anti-cancer drug 2′-deoxy-5-fluorouridylate Nucleosides Nucleotides 14 1995 243 253