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Concept
Selective androgen receptor modulator
Summary
Selective Androgen Receptor Modulators or SARMs are a class of androgen receptor ligands that were developed with the intention of maintaining some of the desirable effects of androgens, such as preventing osteoporosis and muscle loss while reducing risks of undesirable conditions such as prostate cancer. In the late 1990s, the first nonsteroidal SARM, an analog of bicalutamide, was discovered at Imperial Chemical Industries. Although bicalutamide itself is an antiandrogen, its discovery encouraged a search for non-steroidal agonists of androgen receptors, as it was well-known, that small structural changes can transform a receptor antagonist into an agonist (see "Lock and key" model). It was expected, that non-steroidal androgens could provide similar positive effects as anabolic-androgenic steroids, but with fewer side effects.
Although some work on SARMs was done as early as 1940s, it was not until the late 1990s, when researchers at Ligand Pharmaceuticals and the University of Tennessee discovered a new class of cyclic, nonsteroidal quinolinones, with a high anabolic activity in skeletal muscles, and variable selectivy in other tissues.
At present, there are no SARMs which have been approved for therapeutic use by the U.S. Food and Drug Administration.
The binding of ligands to the androgen receptor (AR) results in a conformational change, this consequentially alters surface topology which will lead to tissue-specific gene regulation. This tissue-specific regulation then allows for the selective stimulation or inhibition of the AR; this requires androgen response elements, co-regulators, and transcription factors. Although the exact mechanisms still remain unclear, tissue specificity and complexity of the pathway is known to dictate the transcriptional and cellular response.
There have been experiments using a SARMs C-6 and S-23 on male mice as a contraceptive agent. Treatment of osteoporosis has been explored as SARMs have been found to have trophic effects on bone density and mineralization.
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Anabolic steroid
Anabolic steroids, also known as anabolic-androgenic steroids (AAS), are synthetic substances that mimic the effects of testosterone, the male sex hormone. They are used to increase muscle size, strength, and performance and are commonly associated with athletic performance enhancement and bodybuilding. Anabolic steroids are classified as Schedule III controlled substances in many countries due to their potential for abuse and adverse health effects. Health risks can be produced by long-term use or excessive doses of AAS.
Selective receptor modulator
In the field of pharmacology, a selective receptor modulator or SRM is a type of drug that has different effects in different tissues. A SRM may behave as an agonist in some tissues while as an antagonist in others. Hence selective receptor modulators are sometimes referred to as tissue selective drugs or mixed agonists / antagonists. This tissue selective behavior is in contrast to many other drugs that behave either as agonists or antagonists regardless of the tissue in question.
Nuclear receptor
In the field of molecular biology, nuclear receptors are a class of proteins responsible for sensing steroids, thyroid hormones, vitamins, and certain other molecules. These intracellular receptors work with other proteins to regulate the expression of specific genes thereby controlling the development, homeostasis, and metabolism of the organism. Nuclear receptors bind directly to DNA regulating the expression of adjacent genes; hence these receptors are classified as transcription factors.