Abstract
Spermatozoa contain a number of acrosomal enzymes that are essential for fertilization. Several of these enzymes—for instance, acrosin and hyaluronidase—are biochemically and immunologically unique and are excellent targets for the development of specific, sperm-directed contraceptive agents. Acrosin is a neutral serine proteinase that appears to be required for: (1) the sperm acrosome reaction, (2) sperm binding to the egg, and (3) sperm penetration through the zona pellucida, the innermost of three layers surrounding the egg during fertilization. To date, much of our research has focussed on this enzyme. The present discussion will only deal with a specific type of acrosin inhibitor, although other inhibitory agents directed against acrosin and other sperm enzymes can also function as contraceptive agents (for review, see Reference 1).
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References
Zaneveld, L.J.D. (1982). Sperm enzyme inhibitors for vaginal and other contraception. Res. Front. Fertil. Reg. (PARFR), 2, no. 3
Bhattacharyya, A. K. and Zaneveld, L.J.D. (1982). In Zaneveld, L.J.D. and Chatterton, R. T. (eds.) The Biochemistry of Mammalian Reproduction. ( New York: Wiley )
Zaneveld, L.J.D., Beyler, S. A., Kim, D. S. and Bhattacharyya, A. K. (1979). Biol. Reprod., 20, 1045
Holmberg, K. and Hansen, B. (1979). Acta Chem. Scand. B, 33, 410
Anderson, R. A., Beyler, S. A., Mack, S. R. and Zaneveld, L.J.D. (1981). Biochem. J., 199, 307
Kaminski, J. M. and Diao, X-H. (1984). Biol. Reprod., 30, Suppl. 1, 137
Ganu, V. S. and Shaw, E. (1981). J. Med. Chem., 24, 698
Kitz, R. and Wilson, I. B. (1962). J. Biol. Chem., 237, 3245
Beyler, S. A. and Zaneveld, L. J. D. (1982). Contraception, 26, 137
Van der Ven, H. H., Bhattacharyya, A. K., Kaminski, J., Binor, Z., Bauer, L. and Zaneveld, L. J. D. (1981). Biol. Reprod, 24 (Suppl. 1), 38A
Hall, I. H., Drew, J. H., Sajadi, Z. and Loeler, J. (1979). J. Pharm. Sci., 70, 60
Drew, J. H., Loefffer, L. J. and Hall, I. H. (1981). J. Pharm. Sci., 70, 60
Burck, P. J. and Zimmerman, R. E. (1981). J. Reprod. Fertil., 58, 121
Burck, P. J., Thakkar, A. L. and Zimmerman, R. E. (1982). J. Reprod. Fertil, 66, 109
Zimmerman, R. E., Nevin, R. S., Allen, D. J., Jones, C. D., Goetel, M. E. and Burck, P. J. (1983). J. Reprod. Fertil., 68, 257
Burck, P. J. and Zimmerman, R. E. (1984). Fertil. Steril., 41, 314
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Zaneveld, L.J.D., Kaminski, J.M., Waller, D.P., Anderson, R.A., Bauer, L. (1985). Chemistry, contraceptive activity and toxicology of aryl guanidinobenzoates: inhibitors of sperm acrosin. In: Runnebaum, B., Rabe, T., Kiesel, L. (eds) Future Aspects in Contraception. Springer, Dordrecht. https://doi.org/10.1007/978-94-009-4916-4_3
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DOI: https://doi.org/10.1007/978-94-009-4916-4_3
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