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A bifunctional colchicinoid that binds to the androgen receptor

Nima Sharifi1, Ernest Hamel, Markus A Lill

  • 1Room 21-81, Cancer Stem Cell Section, Laboratory of Cancer Prevention, National Cancer Institute at Frederick, Building 560, Frederick, MD 21702, USA. nima.sharifi@nih.gov

Molecular Cancer Therapeutics
|August 19, 2007
PubMed

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Many cellular signals are hydrophilic and cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind intracellular receptors that reside within the cell cytoplasm or nucleus. Many mammalian steroid hormones and nitric oxide (NO) gas use this cell signaling mechanism.
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Transducer Mechanism: Nuclear Receptors

Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
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The Two-State Receptor Model

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