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History of Antisense Oligonucleotides

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Antisense Therapeutics

Part of the book series: Methods in Molecular Medicine ((MIMM,volume 1))

Abstract

Biological science is a rapidly flowing experimental stream, at times encountering a dam that impedes further progress. At such a pomt, a single crack may induce a major breakthrough Discovery of the double helical structure of DNA in 1953 (1) caused such an event, with flooding of new information into the area now known as molecular biology.

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References

  1. Watson, J. D. and Crick, F H C (1953) Molecular structure of nucleic acids a structure for deoxyribonucleic acids. Nature (Lond) 171, 737–738

    Article  CAS  Google Scholar 

  2. Siekevitz, P and Zamecmk, P C (1951) In vitro incorporation of 1-C14-DL-alanine into proteins of rat liver granular fractions Fed Proc 10, 246 (abstract).

    Google Scholar 

  3. Zamecnik, P. C. and Keller, E B. (1954) Relationship between phosphate energy donors and incorporation of labeled amino acids into proteins. J. Biol. Chem 209, 337–354

    PubMed  CAS  Google Scholar 

  4. Zamecmk, P C.(1979) Historical aspects of protein synthesis Ann NY Acad Sci 325, 269–301.

    Article  Google Scholar 

  5. Brachet, J (1950) Chemical Embryology Interscience, New York.

    Google Scholar 

  6. Caspersson, T. O (1950) Growth and Cell Function Norton, New York.

    Google Scholar 

  7. Keller, E. B, Zamecnik, P C, and Loftfield, R B (1954) The role of microsomes in the incorporation of amino acids into proteins. J Histochem Cytochem 2, 378–386

    PubMed  CAS  Google Scholar 

  8. Zamecnik, P C, Hoagland, M B., and Stephenson, M. L. (1957) Synthesis of protein in the cell nucleus, NY Acad Sci V, 273–274.

    Google Scholar 

  9. Zamecnik, P C, Stephenson, M L, Scott, J F, and Hoagland, M B (1957) Incorporation of C14-ATP into soluble RNA isolated from 105,000 x g supernatant of rat liver. Fed Proc 16, 275

    Google Scholar 

  10. Zamecnik, P C, Stephenson, M L and Hecht, L. I (1958) Intermediate reactions in amino acid incorporation Proc Natl Acad Sci USA 44, 73–78

    Article  PubMed  CAS  Google Scholar 

  11. Hoagland, M. B, Stephenson, M L, Scott, J. F., Hecht, L. I, and Zamecnik, P C (1958) A soluble ribonucleic acid intermediate in protein synthesis J Biol Chem 231, 241–256.

    PubMed  CAS  Google Scholar 

  12. Hoagland, M B, Zamecnik, P C, and Stephenson, M. L. (1959) A hypothesis concerning the roles of particulate and soluble ribonucleic acids in protein synthesis, in A Symposium on Molecular Biology (Zu-kle, R E, ed), University of Chicago Press, Chicago, IL, pp 105–114

    Google Scholar 

  13. Nirenberg, M W. and Matthaei, J H (1961) The dependence of cell-free protein synthesis in E. coli upon naturally occurring or synthetic polyribonucleotides Proc. Natl Acad SCi USA 47, 1588–1602.

    PubMed  CAS  Google Scholar 

  14. Nishimura, S., Jones, D S, and Khorana, H G (1965) The in vitro synthesis of a copolypeptide containing two amino acids in alternating sequence dependent upon a DNA-like polymer containing two nucleotides in alternating sequence J Mol Biol. 13, 302–324.

    Article  PubMed  CAS  Google Scholar 

  15. Allen, D W and Zamecnik, P C. (1962) The effect of puromycin on rabbit reticu-locyte ribosome Biochem Biophys Acta. 55, 865–874.

    Article  PubMed  CAS  Google Scholar 

  16. Zamecnik, P C and Stephenson, M L. (1978) Inhibition of Rous sarcoma virus replication and transformation by a specific oligodeoxynucleotide Proc Natl Acad. Sci. USA 75, 280–284.

    Article  PubMed  CAS  Google Scholar 

  17. Helene, C (1993) Control of gene expression by triple-helix-forming oligonucle-otides the antigene strategy, in Antisense Research and Applications (Crooke, S. T. and Lebleu, B., eds.), CRC, Boca Raton, FL, pp. 375–385.

    Google Scholar 

  18. Maher, L. J., Dervan, P. B., and Wold, B. (1992) Analysis of promoter-specific repression by triplehelical DNA complexes in a eukaryotic cell-free transcription system. Biochemistry 31, 70–81.

    Article  PubMed  CAS  Google Scholar 

  19. Temsamani, J, Metelev, V., Levma, A., Agrawal, S, and Zamecnik, P. (1994) Inhibition of in vitro transcription by ohgodeoxynucleotides. Antisense Res Devel. 4, 279–284.

    CAS  Google Scholar 

  20. Stephenson, M L and Zamecnik, P. C. (1978) Inhibition of Rous sarcoma viral RNA translation by a specific ohgodeoxynucleotide Proc Natl Acad Sci USA 75, 285–288

    Article  PubMed  CAS  Google Scholar 

  21. Zamecnik, P C, Goodchild, J, Taguchi, Y, and Sarm, P S (1986) Inhibition of replication and expression of human T-cell lymphotroptc virus type III in cultured cells by exogenous synthetic oligonucleotides complementary to viral RNA Proc Natl Acad Sci USA 83, 4143–4146

    Article  PubMed  CAS  Google Scholar 

  22. Plesner, P., Goodchild, J, Kalckar, H, and Zamecnik, P. C. (1987) Oligonucleotides with rapid turnover of the phosphate groups occur endogenously in eukaryotic cells Proc Natl Acad Sci USA 84, 1936–1939.

    Article  CAS  Google Scholar 

  23. Inouye, M (1988) Antisense RNA. its functions and applications in gene regulation-a review. Gene 72, 25–34

    Article  PubMed  CAS  Google Scholar 

  24. Kimelman, D (1992) Regulation of eukaryotic gene expression by natural antisense transcripts, in Gene Regulations Biology of Antisense RNA and DNA (Erickson, P and Izant, J G, eds), Raven, New York, pp 1–10

    Google Scholar 

  25. Belikova, A M, Zarytova, V F, and Grineva, N. I (1967) Synthesis of ribonucleosides and diribonucleoside phosphates containing 2-chloroethylamme and nitrogen mustard residues. Tetrahedron Lett 37, 3557–3562

    Article  PubMed  CAS  Google Scholar 

  26. Miller, P S., Braiterman, I T, and Tso, P O. P. (1977) Effects of a trinucleotide ethylphosphtriester, Gmp(Et)Gmp(Et)U, on mammalian cells in culture. Biochemistry 16, 1988–1996

    Article  PubMed  CAS  Google Scholar 

  27. Paterson, B. M., Roberts, B E, and Kuff, E. L (1977) Structural gene tdentification and mapping by DNA-mRNA hybrid-arrested cell-free translation Proc Natl Acad Sci USA 74, 4370–4374.

    Article  PubMed  CAS  Google Scholar 

  28. Hastie, N. D. and Held, W. A (1978) Analyses of mRNA populations by cDNA mRNA hybrid-mediated inhibition of cell-free protein synthesis Proc Natl Acad Sci USA 75, 1217–1221.

    Article  PubMed  CAS  Google Scholar 

  29. van der Krol, A. R, Stuitje, A. R., and Mol, J N. M (1991) Modulation of floral pigmentation by antisense technology, in Antisense Nucleic Acids and Proteins (Mol, J M N. and van der Krol, A R, eds), Marcel Dekker, New York, pp 125–140

    Google Scholar 

  30. Zamecnik, P., Aghajanian, J., Zamecnik, M., Goodchild, J., and Witman, G (1994) Electron micrographic studies of transport of oligodeoxynucleotides across eukaryotic cell membranes. Proc Natl Acad Sci USA 91, 3156–3160

    Article  PubMed  CAS  Google Scholar 

  31. Temsamani, J., Kubert, M, Tang, J, Padmapriya, A, and Agrawal, S (1994) Cellular uptake of oligodeoxynucleotides and their analogs Antisense Res Devel 4, 35–42

    CAS  Google Scholar 

  32. Agrawal, S, Temsamani, J, and Tang, J. Y (1991) Pharmacokmetics, bio-distrtbution and stability of oligodeoxynucleotide phosphorothioates in mice Proc Natl Acad Sci USA 88, 7595–7599

    Article  PubMed  CAS  Google Scholar 

  33. Anderson, W F. (1992) Human gene therapy. Science 256, 808–813.

    Article  PubMed  CAS  Google Scholar 

  34. Khorana, H G, Buchi, H., Ghosh, H., Gupta, N, Jacob, T M., Kossel, H., Mor-gan, R., Narang, S. A, Ohtsuka, E, and Wells, R D. (1966) Polynucleotide syn-thesis and the genetic code Cold Spring Harbor Symp Quant Biol 31, 39–49

    PubMed  CAS  Google Scholar 

  35. Holley, K W, Apgar, J, Everett, G A., Madison J T., Marqursee, M, Merrill, S. H, Penswick, J. R., and Zamir, A (1965) Structure of a ribonucleic acid Sczence 147, 1462–1465

    Article  CAS  Google Scholar 

  36. Monier, R, Stephenson, M L., and Zamecnik, P. C (1960) The preparation and some properties of a low molecular weight ribonucleic acid from baker’s yeast Biochem Biophys Acta 43, 1–8.

    Article  PubMed  CAS  Google Scholar 

  37. Zachau, H. G, Dutting, D, Feldmann, H., Melchers, F, and Karan, W. (1966) Serine specific transfer ribonucleic acids XIV. Comparrson of nucleotide sequence and secondary structure models Cold Spring Harbor Symp Quant Biol 31, 417–424

    PubMed  CAS  Google Scholar 

  38. Raj Bhandary, U. L, Stuart, A, Faulkner, R. D., Chang, S H., and Khorana, H. G (1966) Nucleotide sequence studies on yeast phenylalanyl sRNA Cold Spring Harbor Symp Quant Biol 31, 425–434

    CAS  Google Scholar 

  39. Ingram, V. M and Sjoquist, J A. (1963) Studies on the structure of purified alanine and valine transfer RNA from yeast Cold Spring Harbor Quant Biol 28, 133–138

    CAS  Google Scholar 

  40. Temin, H M and Mizutani, S (1970) RNA-dependent DNA polymerase in viri-ons of Rous sarcoma virus Nature 226, 121l–l213

    Article  Google Scholar 

  41. Baltimore, D (1970) Viral RNA-dependent DNA polymerase Nature (Lond) 226, 1209–1210

    Article  CAS  Google Scholar 

  42. Sanger, F and Coulsen, A R. (1975) A rapid method for determining sequences in DNA by primed synthesis with DNA polymerase J Mol Biol 94, 441–448.

    Article  PubMed  CAS  Google Scholar 

  43. Wickstrom, E (1986) Oligodeoxynucleotide stability in subcellular extracts and culture media. J Biochem Biophys Methods 13, 97–102.

    Article  PubMed  CAS  Google Scholar 

  44. Walder, R W and Walder, J A (1988) Role of RNase H in hybrid-arrested translation by antisense oligonucleotides in current commuincations, in Molecular Biology Anttsense RNA and DNA (Melton, D. A, ed.), Cold Spring Harbor Laboratory, Cold Spring Harbor, NY, pp 35–40.

    Google Scholar 

  45. Stephenson, M L., Scott, J F, and Zamecnik, P. C (1973) Evidence that the polyladenylic acid segment of RNA of avian myeloblastosis virus is located at the “35s” 31-OH terminus Btochem Biophys Res Commun 55, 8–16

    Article  CAS  Google Scholar 

  46. Maxam, A M and Gilbert, W. (1977) A new method of sequencing DNA. Proc Natl Acad Sei USA 74, 560–564.

    Article  CAS  Google Scholar 

  47. Haseltine, W. A, Maxam, A. M., and Gilbert, W (1977) Rous sarcoma virus is terminally redundant the 5′ sequence Proc Natl Acad SCI. USA 74, 989–993

    Article  PubMed  CAS  Google Scholar 

  48. Schwartz, D, Zamecnik, P C., and Weith, H. L (1977) Rous sarcoma virus is terminally redundant: the 3′ sequence Proc. Natl. Acad Sci. USA 74, 994–998

    Article  PubMed  CAS  Google Scholar 

  49. Pitha, P., and Pitha, J. (1980) Polynucleotide analogs as inhibitors of DNA and RNA polymerases, in International Encyclopedta of Pharmacology and Therapetics, Section 103 Inhibitors of DNA and RNA Polymeruses (Sarin, P S. and Gallo, R. C, eds.), Pergamon, New York, pp 235–247

    Google Scholar 

  50. Zamecnik, P. C. and Stephenson, M. L. (1969) Nucleotide pyrophosphate compounds related to the first step in protein synthesis, in The Role of Nucleotides for the Function and Conformation of Enzymes Alfred Benzon Symposium I (Kalckar, H. M, Klenow, H, Munch-Petersen, A., Ottesen, M., and Thaysen, J. H., eds), Munksgaard, Copenhagen, pp 276–291.

    Google Scholar 

  51. Sanger, F, Nicklens, S, and Coulsen, A R (1977) DNA sequencing with chamterminating inhibitors Proc Natl Acad. Sci USA 74, 5463–5467.

    Article  PubMed  CAS  Google Scholar 

  52. Letsinger, R L. and Lunsford, W B (1976) Synthesis of thymidine oligonucleotides by phosphate triester intermediates J Am Chem Soc 98, 3655–3661

    Article  PubMed  CAS  Google Scholar 

  53. Caruthers, M H. (1985) Gene synthesis machines: DNA chemistry and its uses Science 230, 281–285

    Article  PubMed  CAS  Google Scholar 

  54. Agrawal, S, Mayrand, S H, Zamecnik, P C, and Pederson T. (1990) Site-specific excision from RNA by RNase H and mixed phosphate backbone oligodeoxynucleotides. Proc Natl Acad Sci USA 87, 1401–1405

    Article  PubMed  CAS  Google Scholar 

  55. Metelev, V, Lisztewicz, J, and Agrawal, S. (1994) Study of antisense oligonucleotide phosphorothioates containing segments of oligodeoxynucleotides and 2−0-methyl oligoribonucleotides. Bioorg Med Chem Lett 4, 2929–2934

    Article  CAS  Google Scholar 

  56. Stein, C A. and Krieg, A. M. (1994) Editorial. Problems in interpretation of data derived from in vitro and in vivo use of antisense oligodeoxynucleotides Antisense Res Devel 4, 67–69

    CAS  Google Scholar 

  57. Tang, J. Y, Temsamam, J, and Agrawal, S. (1993) Self-stabilized antisense oligonucleotide phosphorothioates. properties and anti-HIV activity Nucleic Acids Res 21(11), 2729–2735

    CAS  Google Scholar 

  58. Buckheit, R W., Jr, Roberson, J L, Lackman-Smith, C., Wyatt, J R, Vickers, T A, and Ecker, D J (1994) Potent and specific inhibition of HIV envelope-mediated cell fusion and virus binding by G-quartet-forming oligonucleotide (Isis-5320) AIDS Res Hum Retrovir l0(11), 1497–1506

    Article  Google Scholar 

  59. Kandtmalla, E R. and Agrawal, S (1995) Single strand targeted triplex-formation Destabilization of guanine quadruplex structures by foldback triplex-forming oligonucleotides Nucleic Acids Res 23, 1068–1074.

    Article  Google Scholar 

  60. Zon, G (1993) Hzstory of Antisense Drug Discovery In Antisense Research and Applications (Crooke, S. T and Lebleu, B., eds), CRC, Boca Raton, FL, PP 1–5

    Google Scholar 

  61. Lisziewtcz, J., Sun, D., Metelev, V, Zamecnik, P., Gallo, R. C., and Agrawal, S (1993) Long-term treatment of human immunodeficiency virus-infected cells with antisense oligonucleotide phosphorothioates. Proc Natl Acad Sci USA 90, 3860–3864

    Article  Google Scholar 

  62. Leiter, J M, Agrawal, S, Palese, P., and Zamecnik, P. C. (1990) Inhibition of influenza virus replication by phosphorothtoate oligodeoxynucleotides Proc Natl Acad Sci USA 87, 3430–3434

    Article  PubMed  CAS  Google Scholar 

  63. Zamecnik, P C, Agrawal, S, and Palese, P, unpublished data

    Google Scholar 

  64. Rapaport, E, Misiura, K, Agrawal, S., and Zamecnik, P. C. (1992) Antimalarial activities of oligodeoxynucleotide phosphorothioates in chloroqume-resistant Plasmodrum falciparum Proc Natl Acad Sci USA 89, 8577–8580

    Article  CAS  Google Scholar 

  65. Dluzewski, A R, Mitchell, G H, Fryer, P R., Griffiths, S., Wilson, R J M, and Gratzer, W. B. (1992) Origins of the parasitophorous vacuole membrane of the malaria parasite, Plasmodium falciparum, in human red blood cells. J Cell Sci 102, 527–532

    PubMed  Google Scholar 

  66. Zamecnik, P C, Rapaport, E, Metelev, V, and Barker, R (1996) Inhibition of replication of drug resistant P. fahparum in vitro by specific anttsense phosphorothioate oligodeoxynucleottdes, in Antisense Oligodeoxynucleotides From Technology to Therapy (Schlingenstepen, K H., Schlingensrepen, R, and Brysch, W, eds.), Blackwell International/Blackwell Wissenschaft, Berlin, in press

    Google Scholar 

  67. Barker, R H., Jr., Metelev, V., Rapaport, E., and Zamecnik, P (1996) Inhibition of Plasmodium falciparum malaria using antisense oligodeoxynucleotrdes Proc Natl Acad SCi USA, in press.

    Google Scholar 

  68. Crooke, S. J. (1994) Editorial. Progress in evaluation of the potential of antisense technology. Antisense Res Devel 4, 145–146.

    CAS  Google Scholar 

  69. Hawkins, J W (1995) Editorial Oligonucleotide therapeutics: coming’ round the clubhouse turn Antisense Res Devel. 5, 1

    CAS  Google Scholar 

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© 1996 Humana Press Inc., Totowa, NJ

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Zamecnik, P.C. (1996). History of Antisense Oligonucleotides. In: Agrawal, S. (eds) Antisense Therapeutics. Methods in Molecular Medicine, vol 1. Humana Press. https://doi.org/10.1385/0-89603-305-8:1

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  • DOI: https://doi.org/10.1385/0-89603-305-8:1

  • Publisher Name: Humana Press

  • Print ISBN: 978-0-89603-305-4

  • Online ISBN: 978-1-59259-585-3

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