1. Woster, P.M., Black, A.Y., Duff, K.J., Coward, J.K. and Pegg, A.E.: Synthesis and Biological Evaluation of S-Adenosyl-1,12-diamino-3-thio-9-azadodecane, a Multisubstrate Adduct Inhibitor of Spermine Synthase. J. Med. Chem. 31, 1300-1307 (1989)
  2. Pegg, A.E., Wechter, R., Poulin, R., Woster, P.M. and Coward, J.K.: Effect of S-Adenosyl-1,12-diamino-3-thio-9-azadodecane, a Multisubstrate Adduct Inhibitor of Spermine Synthase, on Polyamine Metabolism in Mammalian Cells. Biochemistry 28, 8446-8453 (1989).
  3. Woster, P.M.: S-Adenosylmethionine Decarboxylase and Spermidine/Spermine-N1-Acetyltransferase - Emerging Targets for Rational Inhibitor Design, In "Polyamines: Regulation and Molecular Interaction", R.A. Casero, Jr., Ph.D., editor, R.G. Landes Co., Austin, TX, 1995, pp 171-204.
  4. Saab, N.H., West, E.E., Bieszk, N.C., Preuss, C.V., Mank, A.R., Casero, R.A. and Woster, P.M.: Synthesis and Evaluation of Unsymmetrically Substituted Polyamine Analogues as Inhibitors of Spermidine/Spermine-N1-Acetyltransferase (SSAT) and as Potential Antitumor Agents. J. Med. Chem. 36, 2998-3004 (1993).
  5. Woster, P.M.: Spermidine/Spermine-N1-Acetyltransferase - An Emerging Target for the Design of Antitumor Agents. Curr. Opin. Invest. Drugs 2, 1291-1299 (1993).
  6. Woster, P.M.: S-Adenosylmethionine Decarboxylase and Spermidine/Spermine-N1-Acetyltransferase - Emerging Targets for Rational Inhibitor Design, In "Polyamines: Regulation and Molecular Interaction", R.A. Casero, Jr., Ph.D., editor, R.G. Landes Co., Austin, TX, 1995, pp 171-204.
  7. Wu, R., Saab, N.H., Huang, H., Wiest, L, Pegg, A.E., Casero, Jr., R.A. and Woster, P.M.: Synthesis and Evaluation of Polyamine Phosphinates and Phosphonamidates as Transition State Analogue Inhibitors of Spermidine/Spermine-N1-Acetyltransferase. Bioorg. Med. Chem. 4, 825-836 (1996).
  8. Ha, H.C., Sirisoma, N.S., Kuppusamy, P., Zweier, J.L., Woster, P.M. and Casero, R.A.: The Natural Polyamine Spermine Functions Directly as a Free Radical Scavenger. Proc. Nat. Acad. Sci. U.S.A. , 95, 11140-11143 (1998).
  9. Hibasami, H., Borchardt, R.T., Chen, S.-Y., Coward, J.K. and Pegg, A.E. Studies of inhibition of rat spermidine synthase and spermine synthase. Biochem. J. 187 (1980) 419-428. [Medline UI: 80241809]
  10. Pajula, R.-L., Raina, A. and Eloranta, T. Polyamine synthesis in mammalian tissues. Isolation and characterization of spermine synthase from bovine brain. Eur. J. Biochem. 101 (1979) 619-626. [Medline UI: 80091579]
  11. .Hannonen, P., Janne, J. and Raina, A. Partial purification and characterization of spermine synthase from rat brain. Biochim. Biophys. Acta 289 (1972) 225-231. [Medline UI: 73043235]
  12. Pegg, A.E., Shuttleworth, K. and Hibasami, H. Specificity of mammalian spermidine synthase and spermine synthase. Biochem. J. 197 (1981) 315-320. [Medline UI: 82113021]
  13. Tabor, C.W. Propylamine transferase (spermidine synthesis). Methods Enzymol. 5 (1962) 761-765.
  14. Tabor, H. and Tabor, C.W. Biosynthesis and metabolism of 1,4-diaminobutane, spermidine, spermine, and related amines. Adv. Enzymol. Relat. Areas Mol. Biol. 36 (1972) 203-268. [Medline UI: 73033389]
  15. Tait, G.H. The formation of homospermidine by an enzyme from Rhodopseudomonas viridis. Biochem. Soc. Trans. 7 (1979) 199-200. [Medline UI: 79170251]
  16. Böttcher, F., Ober, D., Hartmann, T. Biosynthesis of pyrrolizidine alkaloids: putrescine and spermidine are essential substrates of enzymatic homospermidine formation. Can. J. Chem. 72 (1994) 80-85.
  17. Yamamoto, S., Nagata, S., Kusaba, K. Purification and characterization of homospermidine synthase in Acinetobacter tartarogens ATCC 31105. J. Biochem. 114 (1993) 45-49. [Medline UI: 94012579]
  18. Srivenugopal, K.S., Adiga, P.R. Enzymatic synthesis of sym-homospermidine in Lathyrus sativus T (grass pea) seedlings. Biochem. J. 190 (1980) 461-464. [Medline UI: 81133501]
  19. "Synthesis of N4-Acylated N1,N8-Bis(acyl)Spermidines: An Approach to the Synthesis of Siderophores." R. J. Bergeron, K. A. McGovern, M. A. Channing, and P. S. Burton, J. Org. Chem., 45,1589-1592 (1980).
  20. "Synthesis, Absorption and Toxicity of N1,N8-Bis(2,3-dihydroxybenzoyl)Spermidine, a Potent Iron Chelator." R. J. Bergeron, P. S. Burton, K. A. McGovern, E. J. St. Onge, and R. R. Streiff, J. Med. Chem., 23, 1130-1133 (1980).
  21. "Reagents for the Selective Acylation of Spermidine, Homospermidine and Bis-[3-amino- propylamine." R. J. Bergeron, P. S. Burton, K. A. McGovern, and S. J. Kline, Synthesis, 732-733 (1981).
  22. Biological Properties of N4-Spermidine Derivatives and their Potential in Anticancer Chemotherapy." C. W. Porter, R. J. Bergeron, and N. J. Stolowich, Cancer Res., 42, 4072- 4078 (1982).

  23. "Spermidine Requirement for Cell Proliferation in Eukaryotic Cells: Structural Specificity and Quantitation." C. W. Porter and R. J. Bergeron, Science, 219, 1083-1085 (1983).
  24. “Reagents for the Stepwise Functionalization of Spermidine, Homospermidine and Bis-(3- aminopropyl)amine.” R. J. Bergeron, J. R. Garlich, and N. J. Stolowich, J. Org. Chem., 49, 2997-3001 (1984).
  25. “Treatment With alpha-Difluoromethylornithine Plus a Spermidine Analogue Leads to Spermine Depletion and Growth Inhibition in Cultured L1210 Leukemia Cells.” R. Casero, R. J. Bergeron, and C. W. Porter, J. Cell. Physiol., 121, 476-482 (1984).

25. "Antineoplastic and Antiherpetic Activity of Spermidine Catecholamide Iron Chelators." R. J. Bergeron, P. F. Cavanaugh, Jr., S. J. Kline, R. G. Hughes, Jr., G. T. Elliott, and C. W. Porter, Biochem. Biophys. Res. Comm., 121, 848-854 (1984).

  1. "Biological Properties of N4- and N1, N8-Spermidine Derivatives in Cultured L1210 Leukemia Cells." C. W. Porter, P. F. Cavanaugh, N. J. Stolowich, B. Ganis, E. Kelly, and R. J. Bergeron, Cancer Res., 45, 2050-2057 (1985).

27. "Methods for the Selective Modification of Spermidine and its Homologues." R. J. Bergeron, Accts. Chem. Res., 19, 105-113 (1986).

28. "Hexahydropyrimidines as Masked Spermidine Vectors in Drug Delivery." R. J. Bergeron and H. W. Seligsohn, Bioorg. Chem., 14, 345-355 (1986).

29. "Structural Determinants of Spermidine-DNA Interactions." P. M. Vertino, R. J. Bergeron, P. F. Cavanaugh, Jr., and C. W. Porter, Biopolymers, 26, 691-703 (1987).

30. "Relative Abilities of Bis(ethyl) Derivatives of Putrescine, Spermidine, and Spermine to Regulate Polyamine Biosynthesis and Inhibit L1210 Leukemia Cell Growth." C. W. Porter, J. McManis, R. A. Casero, and R. J. Bergeron, Cancer Res., 47, 2821-2825 (1987).

31. "Regulation of Ornithine Decarboxylase Activity by Spermidine and the Spermidine Analogue N1N8-Bis(ethyl)Spermidine." C. W. Porter, F. G. Berger, A. E. Pegg, B. Ganis, and R. J. Bergeron, Biochem. J., 242, 433-440 (1987).

32. "Selective Regulation of S-Adenosylmethionine Decarboxylase Activity by the Spermine Analogue 6-Spermyne." C. W. Porter, J. S. McManis, D. Lee, and R. J. Bergeron, Biochem. J., 254, 337-342 (1988).

.33. "Regulation of Polyamine Biosynthetic Activity by Spermidine and Spermine Analogues- A Novel Antiproliferative Strategy." C. W. Porter and R. J. Bergeron, Adv. Exp. Med. Biol., 250, (Progress in Polyamine Research), V. Zappia and A. E. Pegg, Eds., Plenum Publishing Corp. 677-690 (1988).

34. "Major Increases in Spermidine/Spermine-N1-Acetyltransferase Activity by Spermine Analogues and their Relationship to Polyamine Depletion and Growth Inhibition in L1210 Cells." P. R. Libby, M. Henderson, R. J. Bergeron, and C. W. Porter, Cancer Res., 49, 6226-6231 (1989).

35. "Structure-Function Correlations of Polyamine Analog-Induced Increases in Spermidine/Spermine Acetyltransferase Activity." P. R. Libby, R. J. Bergeron, and C. W. Porter, Biochem. Pharmacol., 38, 1435-1442 (1989).

36. "Characterization of Human Spermidine/Spermine N1-Acetyltransferase Purified from Cultured Melanoma Cells." P. R. Libby, B. Ganis, R. J. Bergeron, and C. W. Porter, Arch. Biochem. Biophys., 284, 238-244 (1991).

37. "Differential Effects of the Spermine Analog, N1,N12 Bis(ethyl) Spermine, on Polyamine Metabolism and Cell Growth in Human Melanoma Cell Lines and Melanocytes." N. W. Shappell, J. T. Miller, R. J. Bergeron and C. W. Porter, Anticancer Res., 12, 1083-1090 (1992).

38. "Antitumor Activity of N, N'-Bis(ethyl)Spermine Homologues Against Human MALME-3 Melanoma Xenografts." R. J. Bernacki, R. J. Bergeron, and C. W. Porter, Cancer Res., 52, 2424-2430 (1992).

39. "Radiopotentiation of Human Brain Tumor Cells by the Spermine Analog N1,N14- Bis(ethyl)Homospermine." C.-Z. Chen, L. J. Hu, R. J. Bergeron, L. J. Marton, and D. F. Deen, Int. J. Radiat. Oncol. Biol. Phys., 29, 1041-1047 (1994).

40. Fogel-Petrovic, M., Kramer, D.L., Vujcic, S., Miller, J., McManis, J.S., Bergeron, R.J. and Porter, C.W., Structural basis for differential induction of spermdine/spermine N1-acetyltransferase activity by novel spermine analogs. Molec. Pharm. 52:69-74, 1997.

41. Alhonen, L., Karppinen, A., Uusi-Oukari, M., Vujcic, S., Korhonen, P., Halmekytö, M., Kramer, D. L., Hines, R., Jänne, J., and Porter, C.W. Correlation of polyamine and growth responses to N1`,N11-diethylnorspermine in primary fetal fibroblasts derived from transgenic mice overexpressing spermidine/spermine N1-acetyltransferase. J. Biol. Chem. 273:1964-1969, 1998.

42. Alhonen, L., Pietilä, M., Halmekytö, M., Kramer, D.L., Jänne, J. and Porter, C.W., Transgenic mice with activated polyamine catabolism due to overexpression of spermidine/spermine N1-acetyltransferase show enhanced sensitivity to the polyamine analogue, N1,N11-diethylnorspoermine. Mol. Pharm. 55:693-698, 1999.

43. Bachrach, U.: Metabolism and Function of Spermine and Related Polyamines, in Ann. Rev. Microbiol., 24, (Clifton, C., ed., Ann. Reviews, Inc., Palo Alto, CA), 109 (1970).

44. Tabor, H., and Tabor, C.: Biosynthesis and Metabolism of 1,4-Diaminobutane, Spermidine, Spermine, and Related Amines, in Advances in Enzymology, XXXVI, 203 (1972).

45. Unemoto, T., Ikeda, K., Hayashi, M., and Miyaki, K.: Studies on Polyamines. I. A New Fluorometric Determination of Spermine and Spermidine, Chem. Pharm. Bull., 11, 148 (1963).

46. Tari, L.W. and Secco, A.S. Base-pair opening and spermine binding-B-DNA features displayed in the crystal structure of a gal operon fragment:Implications for protein-DNA recognition Nucleic Acids Res., 23(No. 11), 2065-2073, (1995).

47. Xie, X., S. Rao, P. Walian, V. Hatch, G.N. Phillips Jr., and C. Cohen. 1994. Coiled-coil packing in spermine-induced tropomyosin crystals: A comparative study of three forms. J. Mol. Biol. 236: 1212-1226. [abstract]

48. ¹H MRS of Prostatic Tissue Focased on the Detection of Spermine, a Possible Biomarker of Malignant Behavior in Prostate Cancer. M. van der Graaf, R.G. Schipper, G.O.N. Oosterhof, J.A. Schalken, A.A.J. Verhofstad and A. Heerschap. University Hospital, Nijmegen, The Netherlands.

49. Araneda, R.C., Lan, J.-Y., Zheng, X., Zukin, R.S. and Bennett, M.V.L. Spermine and arcaine block and permeate N-methyl-D-aspartate receptor channels. Biophys. J. 76: 2899-2911, 1999.

50. Borrell, A, Besford, RT, Altabella, T, Masgrau, C, and Tiburcio, AF (1996) Regulation of arginine decarboxylase by spermine in osmotically-stressed oat leaves. Physiologia Plantarum 98: 105-110

51. Evans, CH, Lee, TS and Flugelman, AA: Spermine directed immunosuppression of cervical carcinoma cell sensitivity to a majority of lymphokine activated killer (LAK) lymphocyte cytotoxicity. Natural Immunity 14: 157-163, 1995.

52. Chieko Koike, Debra T. Chao, Karen Hodgens, William Landis, Bruce R. Zetter, "Spermine induction of apoptosis in metastatic prostate carcinoma" (submitted).

53. Cleavage of double-stranded DNA by manganese tris(methylpyridiniumyl)porphyrin linked to 3’-spermine-oligonucleotides.
M. PITIE and B. MEUNIER
J. Biol. Inorg. Chem., 1, 239-246 (1996).

54. Feuerstein, B. G., Pattabiraman, N., Marton, L. J. Theoretical models of spermine/DNA interactions Annals of the New York Academy of Sciences vol. 483:251, 1986.

55. . Feuerstein, B. G., Pattabiraman, N., Marton, L. J. Spermine-DNA interactions: a theoretical study, Proc. Natl. Acad. Sci., USA, 83:5948-5952, 1986.

56. DESIDERIO M.A., Mattei S., Biondi G. e Colombo M.P. Cytosolic and nuclear spermidine acetyltransferases in growing NIH 3T3 fibroblasts stimulated with serum or polyamines: relationship to polyamine-biosynthetic decarboxylases and histone acetyltransferase. Biochem. J. 293, 475-479, 1993.

57. DESIDERIO M.A., BARDELLA L. Expression of spermidine/spermine N1-acetyltransferase in growing Yoshida AH-130 hepatoma cells. Hepatology 19, 728-734, 1994.

58. Jamdar, S.C., L.J. Osborne, G.N. Wells, and G.M. Cohen. 1987. "Effect of Spermine on Translocation of Mg++-dependent Phosphatidate Phosphohydrolase." Biochemica et Biophysica Acta., 917, 381-387.