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Selective Androgen Receptor Degrader
A selective androgen receptor degrader or downregulator (SARD) is a type of pharmaceutical drug, drug which interacts with the androgen receptor (AR) such that it causes the AR to be degraded and thus downregulation and upregulation, downregulated. They are under investigation for the treatment of prostate cancer and other androgen-dependent conditions. As of 2017, dimethylcurcumin (ASC-J9), a SARD, is under development for the treatment of acne vulgaris. See also * Androgen deprivation therapy References Antiandrogens Hormonal antineoplastic drugs Receptor modulators, {{Antineoplastic-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pharmaceutical Drug
A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy (pharmacotherapy) is an important part of the medical field and relies on the science of pharmacology for continual advancement and on pharmacy for appropriate management. Drugs are classified in multiple ways. One of the key divisions is by level of control, which distinguishes prescription drugs (those that a pharmacist dispenses only on the order of a physician, physician assistant, or qualified nurse) from over-the-counter drugs (those that consumers can order for themselves). Another key distinction is between traditional small molecule drugs, usually derived from chemical synthesis, and biopharmaceuticals, which include recombinant proteins, vaccines, blood products used therapeutically (such as IVIG), gene therapy, monoclonal antibodies and cell therapy (for instance, stem cell therapies) ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Androgen Receptor
The androgen receptor (AR), also known as NR3C4 (nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor that is activated by binding any of the androgenic hormones, including testosterone and dihydrotestosterone in the cytoplasm and then translocating into the nucleus. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor. The main function of the androgen receptor is as a DNA-binding transcription factor that regulates gene expression; however, the androgen receptor has other functions as well. Androgen-regulated genes are critical for the development and maintenance of the male sexual phenotype. Function Effect on development In some cell types, testosterone interacts directly with androgen receptors, whereas, in others, testosterone is converted by 5-alpha-reductase to dihydrotestosterone, an even more potent agonist for androgen receptor activation. T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Downregulation And Upregulation
In the biological context of organisms' production of gene products, downregulation is the process by which a cell decreases the quantity of a cellular component, such as RNA or protein, in response to an external stimulus. The complementary process that involves increases of such components is called upregulation. An example of downregulation is the cellular decrease in the expression of a specific receptor in response to its increased activation by a molecule, such as a hormone or neurotransmitter, which reduces the cell's sensitivity to the molecule. This is an example of a locally acting (negative feedback) mechanism. An example of upregulation is the response of liver cells exposed to such xenobiotic molecules as dioxin. In this situation, the cells increase their production of cytochrome P450 enzymes, which in turn increases degradation of these dioxin molecules. Downregulation or upregulation of an RNA or protein may also arise by an epigenetic alteration. Such an epigene ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prostate Cancer
Prostate cancer is cancer of the prostate. Prostate cancer is the second most common cancerous tumor worldwide and is the fifth leading cause of cancer-related mortality among men. The prostate is a gland in the male reproductive system that surrounds the urethra just below the bladder. It is located in the hypogastric region of the abdomen. To give an idea of where it is located, the bladder is superior to the prostate gland as shown in the image The rectum is posterior in perspective to the prostate gland and the ischial tuberosity of the pelvic bone is inferior. Only those who have male reproductive organs are able to get prostate cancer. Most prostate cancers are slow growing. Cancerous cells may spread to other areas of the body, particularly the bones and lymph nodes. It may initially cause no symptoms. In later stages, symptoms include pain or difficulty urinating, blood in the urine, or pain in the pelvis or back. Benign prostatic hyperplasia may produce similar symptoms ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Androgen-dependent Condition
An androgen-dependent condition, disease, disorder, or syndrome, is a medical condition that is, in part or full, dependent on, or is sensitive to, the presence of androgenic activity in the body. Known androgen-dependent conditions include acne, seborrhea, androgenic alopecia, hirsutism, hidradenitis suppurativa, precocious puberty in boys, hypersexuality, paraphilias, benign prostatic hyperplasia (BPH), prostate cancer, and hyperandrogenism in women such as in polycystic ovary syndrome (PCOS), congenital adrenal hyperplasia (CAH), and androgen-secreting tumors (gonadal or adrenal tumor). Such conditions may be treated with drugs with antiandrogen actions, including androgen receptor antagonists such as cyproterone acetate, spironolactone, and bicalutamide, 5α-reductase inhibitors such as finasteride and dutasteride, CYP17A1 inhibitors such as abiraterone acetate, gonadotropin-releasing hormone (GnRH) analogues such as leuprorelin and cetrorelix, and/or other antigonadotropin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dimethylcurcumin
Dimethylcurcumin (development code ASC-J9) is a nonsteroidal antiandrogen and a synthetic curcuminoid which is under development by AndroScience Corporation as a topical medication for the treatment of acne vulgaris. It has also been under investigation for the treatment of male pattern hair loss, spinal muscular atrophy, and wounds, but no development has been reported for these indications. There has been interest in the drug for the potential treatment of prostate cancer as well. As of 2017, it is in phase II clinical trials for acne vulgaris. Dimethylcurcumin is an androgen receptor (AR) inhibitor and shows strong and specific antiandrogenic activity ''in vitro'' (e.g., against LNCaP cell growth) at sufficiently high concentrations. However, its mechanism of action and effects differ from those of conventional antiandrogens; it is not an antagonist of the AR and instead appears to act as a selective degradation enhancer (SARD) of certain subpopulations of the AR, for insta ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acne Vulgaris
Acne, also known as ''acne vulgaris'', is a long-term skin condition that occurs when dead skin cells and oil from the skin clog hair follicles. Typical features of the condition include blackheads or whiteheads, pimples, oily skin, and possible scarring. It primarily affects skin with a relatively high number of oil glands, including the face, upper part of the chest, and back. The resulting appearance can lead to anxiety, reduced self-esteem, and, in extreme cases, depression or thoughts of suicide. Susceptibility to acne is primarily genetic in 80% of cases. The roles of diet and cigarette smoking in the condition are unclear, and neither cleanliness nor exposure to sunlight appear to play a part. In both sexes, hormones called androgens appear to be part of the underlying mechanism, by causing increased production of sebum. Another common factor is the excessive growth of the bacterium ''Cutibacterium acnes'', which is present on the skin. Treatments for acne are ava ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Androgen Deprivation Therapy
Androgen deprivation therapy (ADT), also called androgen suppression therapy, is an antihormone therapy whose main use is in treating prostate cancer. Prostate cancer cells usually require androgen hormones, such as testosterone, to grow. ADT reduces the levels of androgen hormones, with drugs or surgery, to prevent the prostate cancer cells from growing. The pharmaceutical approaches include antiandrogens and chemical castration. Several studies have concluded that ADT has demonstrated benefit in patients with metastatic disease, and as an adjunct to radiation therapy in patients with locally advanced disease, as well as those with unfavorable intermediate-risk or high-risk localized disease. However, in patients with low-risk prostate cancer, ADT has demonstrated no survival advantage, and significant harm, such as impotence, diabetes and bone loss. The therapy can also eliminate cancer cells by inducing androgen deprivation-induced senescence. Lowering androgen levels or sto ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiandrogens
Antiandrogens, also known as androgen antagonists or testosterone blockers, are a class of drugs that prevent androgens like testosterone and dihydrotestosterone (DHT) from mediating their biological effects in the body. They act by blocking the androgen receptor (AR) and/or inhibiting or suppressing androgen production. They can be thought of as the functional opposites of AR agonists, for instance androgens and anabolic steroids (AAS) like testosterone, DHT, and nandrolone and selective androgen receptor modulators (SARMs) like enobosarm. Antiandrogens are one of three types of sex hormone antagonists, the others being antiestrogens and antiprogestogens. Antiandrogens are used to treat an assortment of androgen-dependent conditions. In men, antiandrogens are used in the treatment of prostate cancer, enlarged prostate, scalp hair loss, overly high sex drive, unusual and problematic sexual urges, and early puberty. In women, antiandrogens are used to treat acne, seborrhea, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hormonal Antineoplastic Drugs
A hormone (from the Greek participle , "setting in motion") is a class of signaling molecules in multicellular organisms that are sent to distant organs by complex biological processes to regulate physiology and behavior. Hormones are required for the correct development of animals, plants and fungi. Due to the broad definition of a hormone (as a signaling molecule that exerts its effects far from its site of production), numerous kinds of molecules can be classified as hormones. Among the substances that can be considered hormones, are eicosanoids (e.g. prostaglandins and thromboxanes), steroids (e.g. oestrogen and brassinosteroid), amino acid derivatives (e.g. epinephrine and auxin), protein or peptides (e.g. insulin and CLE peptides), and gases (e.g. ethylene and nitric oxide). Hormones are used to communicate between organs and tissues. In vertebrates, hormones are responsible for regulating a variety of physiological processes and behavioral activities such as dige ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
