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Other lipid-soluble hormones that are not steroid hormones, such as vitamin D and thyroxine, have receptors located in the nucleus. The hormones diffuse across both the plasma membrane and the nuclear envelope, then bind to receptors in the nucleus. The hormone-receptor complex stimulates transcription of specific genes.

Plasma membrane hormone receptors

Amino acid derived hormones and polypeptide hormones are not lipid-derived (lipid-soluble) and therefore cannot diffuse through the plasma membrane of cells. Lipid insoluble hormones bind to receptors on the outer surface of the plasma membrane, via plasma membrane hormone receptors . Unlike steroid hormones, lipid insoluble hormones do not directly affect the target cell because they cannot enter the cell and act directly on DNA. Binding of these hormones to a cell surface receptor results in activation of a signaling pathway; this triggers intracellular activity and carries out the specific effects associated with the hormone. In this way, nothing passes through the cell membrane; the hormone that binds at the surface remains at the surface of the cell while the intracellular product remains inside the cell. The hormone that initiates the signaling pathway is called a first messenger    , which activates a second messenger in the cytoplasm, as illustrated in [link] .

Illustration shows epinephrine bound to the extracellular surface of a beta-adrenergic receptor. A G-protein associated with the intracellular surface of the receptor is activated when the GDP associated with it is replaced with GTP. The G protein activates the enzyme adenylyl cyclase, which converts ATP to cAMP, triggering a cellular response.
The amino acid-derived hormones epinephrine and norepinephrine bind to beta-adrenergic receptors on the plasma membrane of cells. Hormone binding to receptor activates a G-protein, which in turn activates adenylyl cyclase, converting ATP to cAMP. cAMP is a second messenger that mediates a cell-specific response. An enzyme called phosphodiesterase breaks down cAMP, terminating the signal.

The specific response of a cell to a lipid insoluble hormone depends on the type of receptors that are present on the cell membrane and the substrate molecules present in the cell cytoplasm. Cellular responses to hormone binding of a receptor include altering membrane permeability and metabolic pathways, stimulating synthesis of proteins and enzymes, and activating hormone release.

Section summary

Hormones cause cellular changes by binding to receptors on target cells. The number of receptors on a target cell can increase or decrease in response to hormone activity. Hormones can affect cells directly through intracellular hormone receptors or indirectly through plasma membrane hormone receptors.

Lipid-derived (soluble) hormones can enter the cell by diffusing across the plasma membrane and binding to DNA to regulate gene transcription and to change the cell’s activities by inducing production of proteins that affect, in general, the long-term structure and function of the cell. Lipid insoluble hormones bind to receptors on the plasma membrane surface and trigger a signaling pathway to change the cell’s activities by inducing production of various cell products that affect the cell in the short-term. The hormone is called a first messenger and the cellular component is called a second messenger. G-proteins activate the second messenger (cyclic AMP), triggering the cellular response. Response to hormone binding is amplified as the signaling pathway progresses. Cellular responses to hormones include the production of proteins and enzymes and altered membrane permeability.

Art connections

[link] Heat shock proteins (HSP) are so named because they help refold mis-folded proteins. In response to increased temperature (a “heat shock”), heat shock proteins are activated by release from the NR/HSP complex. At the same time, transcription of HSP genes is activated. Why do you think the cell responds to a heat shock by increasing the activity of proteins that help refold misfolded proteins?

[link] Proteins unfold, or denature, at higher temperatures.

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Source:  OpenStax, Bmcc 103 - concepts of biology. OpenStax CNX. Aug 06, 2015 Download for free at https://legacy.cnx.org/content/col11855/1.2
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