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Description: A potent androgenic steroid and major product secreted by the leydig cells of the testis. Its production is stimulated by luteinizing hormone from the pituitary gland. In turn, testosterone exerts feedback control of the pituitary LH and FSH secretion. Depending on the tissues, testosterone can be further converted to dihydrotestosterone or estradiol. [PubChem]
Drug Type: Small Molecule; Approved; Investigational
Pharmacology: Testosterone is a steroid hormone from the androgen group. Testosterone is primarily secreted in the testes of males and the ovaries of females although small amounts are secreted by the adrenal glands. It is the principal male sex hormone and an anabolic steroid. In both males and females, it plays key roles in health and well-being. Examples include enhanced libido, energy, immune function, and protection against osteoporosis. On average, the adult male body produces about twenty times the amount of testosterone than an adult female's body does.
Mechanism of Action: The effects of testosterone in humans and other vertebrates occur by way of two main mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of certain estrogen receptors. Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5α-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5α-reductase. DHT binds to the same androgen receptor even more strongly than T, so that its androgenic potency is about 2.5 times that of T. The T-receptor or DHT-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing the androgen effects.
Indication: For replacement therapy in males for conditions associated with a deficiency or absence of endogenous testosterone.
Half Life: 10-100 minutes
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Individual Studies
  • LNCaP treatment of cells with DHT and a sequence-specific DNA binding polyamide

    Homo sapiens Homo sapiens | RNA Expression   RNA Expression

    Androgen Receptor (AR) is essential for the growth and progression of prostate cancer in both hormone-sensitive and hormone-refractory disease. We have designed a sequence-specific DNA binding polyamide (1) that targets the consensus androgen response element (ARE). This polyamide binds the PSA prom…

    Authors: Dervan PB, Nickols NG

    Organization: California Institute of Technology 1200 …

  • Expression data from LNCaP cell line

    Homo sapiens Homo sapiens | RNA Expression   RNA Expression

    Androgen receptor (AR) is a ligand-dependent transcription factor that plays a key role in the onset and progression of prostate cancer. Surprisingly little is known of AR binding sites and collaborating transcription factors in the human genome. Here we have identified the DNA sequence motifs that …

    Authors: Wang Qianben, Li Wei

    Organization: Dana Farber Cancer Institute 44 Binney S…

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Thought leaders and organizations working on research involving testosterone.

  • Claudia Mattern
  • Guido van Wingen
  • Nick F Ramsey
  • Jack van Honk
  • Jan Buitelaar
  • Acrux DDS Pty Ltd
  • Boston University
  • National Institute on Aging (NIA)
  • National Institute of Diabetes and Digestive and Kidney Diseases (NIDD…
  • Solvay Pharmaceuticals
  • Monash University
  • Radboud University of Nijmegen
  • University of Bristol
  • Utrecht University
  • University of Zurich

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