Add time:08/30/2019         Source:sciencedirect.com

Chapter 3 discusses cancer chemotherapy related to the hormonal regulation of tumors, starting with the regulation of gene transcription by estrogens and the proposed mechanisms to explain the development of estrogen-dependent tumors. Nonsteroidal antiestrogens, also known as “selective estrogen receptor modulators” (SERMs), are explained at the molecular and atomic levels, and their action is rationalized by using the structures of their complexes with the receptor. The mechanisms of resistance to hormonal therapy are discussed, as well as alternative endocrine treatments. After explaining different mechanisms to rationalize aromatase action, steroidal (type I) and nonsteroidal (type II) aromatase inhibitors are studied, first discussing the advantages of the mechanism-based inhibitors known as aromatase inactivators and then the structure–activity relationships in steroidal aromatase inhibitors, especially how the coordination of azole derivatives to the iron atom of the heme group of the enzyme explains their affinity but also their problematic selectivity. We comment on the role of steroid sulfatase in steroid biosynthesis, the mechanism of action of its inhibitors, and the advantages of dual aromatase–sulfatase inhibitors. The chapter discusses the importance in prostatic cancer of steroidal and nonsteroidal antiandrogens and the resistance associated with the presence of a variant of the androgen receptors, as well as inhibitors of the different enzymes involved in androgen biosynthesis. The mechanisms associated with the anticancer activity of agonists of the gestagen receptor, glucocorticoids, retinoids, and agonists of vitamin D receptors and peroxysome proliferator activating receptors (PPARγ) are also commented.

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