Steroid receptors belong to the nuclear hormone receptor superfamily, which represents one of the important families of drug targets in the pharmaceutical industry. These receptors are generally expressed in a broad range of tissues and play roles in multiple physiological pathways. They represent one of the most complex target classes for drug research as the typical pharmacologically selective, potent, and pure agonist or antagonist may not be sufficient for the development of an optimal compound for therapeutic use. In many cases, the professed compound that is a selective modulator of a steroid hormone receptor that functions as an agonist in one tissue and as an antagonist in another can offer a better therapeutic advantage. In this review, we will selectively summarize members of the steroid hormone receptor subfamily, their therapeutic opportunities, and a glimpse of the methods that can be utilized in the development of drugs that target these receptors.