techniques for searching conformational space (chapter 1). In addition, peptidomimetic
chemistry techniques using bioisosteric substitutions can be used to design peptide
mimics which are bioactive yet “less peptidic” in molecular structure (chapter 3).
Finally, if the hormone receptor has been isolated, high throughput screening in con-
junction with a combinatorial library may lead to the identification of a nonpeptidic
organic molecule lead compound to be optimized as a potential drug. By exploiting this
multipronged strategy, drug design that targets hormones and hormonal receptors
persists as a viable and useful medicinal chemistry pursuit.
Selected References
Steroid Hormones
R. Alonso, I. Lopez-Coviella (1998). Gonadal steroids and neuronal function. Neurochemical
Research 23: 675–688.
J. L. Arriza, C. Weinberger, G. Cerelli, T. M. Glaser, B. L. Handelin, D. E. Housman, R. E. Evans
(1987). Cloning of human mineralocorticoid receptor c-DNA: structural and functional
kinship with the glucocorticoid receptor. Science 227: 268–275.
C. Bai, A. Schmidt, L. P. Freedman (2003). Steroid hormone receptors and drug discovery:
therapeutic opportunities and assay designs. Assay Drug Dev. Technol. 1: 843–852.
S. Barker (2003). Anti-estrogens in the treatment of breast cancer: current status and future direc-
tions.Curr. Opin. Invest. Drugs (Thomson Curr. Drugs) 4: 652–657.
M. R. Bell, F. H. Batzold, R. C. Winneker (1986). Chemical control of fertility. Annu. Rep. Med.
Chem. 21: 169–177.
S. Bhasin (1993). Androgen treatment of hypogonadal men. J. Clin. Endocrinol. Metab.
81 : 757.
M. S. Brown, J. L. Goldstein (1984). How LDL receptors influence cholesterol and atheroscle-
rosis. Sci. Am. 255: 58–66.
M. J. Coghlan, S. W. Elmore, P. R. Kym, M. E. Kort (2002). Selective glucocorticoid receptor
modulators.Ann. Rep. Med. Chem. 37: 167.
H. Danielson, J. Sjövall (Eds.) (1985). Sterols and Bile Acids.New Comprehensive Biochemistry,
vol. 12. Amsterdam: Elsevier.
J. Gorski (1986). The nature and development of steroid hormone receptors. Experientia 42:
744–750.
A. B. Grey, J. P. Stapleton, M. C. Evans, I. R. Reid (1995). The effect of anti-estrogen tamoxifen
on cardiovascular risk factors in normal post-menopausal women. J. Clin. Endocrinol.
Metab. 80: 8192.
O. Jenne, C. W. Bardin (1984). Androgen and antiandrogen receptor binding. Annu. Rev. Physiol.
46 : 107–118.
V. C. Jordan (1984). Biochemical pharmacology of antiestrogen action. Pharmacol. Rev. 36:
245–276.
R. S. Newton, B. R. Krause (1986). Approaches to drug intervention in atherosclerotic disease.
Annu. Rep. Med. Chem. 21: 189–200.
G. H. Rasmussen (1986). Chemical control of androgen action. Annu. Rep. Med. Chem. 21:
179–188.
D. R. Rowley, D. J. Tindall (1986). Androgen receptor protein: purification and molecular prop-
erties. In: G. Litwack, (Ed.) Biochemical ActionofHormonesvol. 13. New York: Academic
Press, pp. 305–324.
382 MEDICINAL CHEMISTRY