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Carcinogenesis in the different organs of the reproductive system, particularly, prostate, ovarian, and cervical tissues, involves aberrant expression of various physiological receptors belonging to different superfamilies. This chapter provides insights into the physiological receptors that are associated with the genesis, progression, metastasis, management, as well as the prognosis of the cancers of the male and female reproductive systems. It also highlights the structural and binding characteristics of the highly predominant receptors, namely, androgen, estrogen, progesterone, and gonadotropin-releasing hormone (GnRH) receptors, which are overexpressed in these cancers and discusses various strategies to target them.