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MCAT Content / Endocrine System Mechanisms Of

Hormone Action / Cellular Mechanisms Of
Hormone Action

Cellular
mechanisms of
hormone action
Topic:
Endocrine System Mechanisms Of Hormone Action

Hormones mediate changes in target

cells by binding to specific hormone
receptors. In this way, even though
hormones circulate throughout the body
and come into contact with many
different cell types, they only affect cells
that possess the necessary receptors.
Receptors for a specific hormone may be
found on many different cells or may be
limited to a small number of specialized
cells.

The hormone binds to the receptor

protein, resulting in the activation of a
signal transduction mechanism that
ultimately leads to cell type-specific
responses. Receptor binding alters
cellular activity, resulting in an increase
or decrease in normal body processes.
Depending on the location of the protein
receptor on the target cell and the
chemical structure of the hormone,
hormones can mediate changes directly
by binding to intracellular hormone
receptors and modulating gene
transcription, or indirectly by binding to
cell surface receptors and stimulating
signaling pathways.

Lipid-soluble hormones such as steroid

hormones diffuse across the lipid bilayer
membranes of the endocrine cell. Once
outside the cell, they bind to transport
proteins that keep them soluble in the
bloodstream. At the target cell, the
hormones are released from the carrier
protein and diffuse across the lipid
bilayer of the plasma membrane of the
target cells. They then adhere to
intracellular receptors residing in the
cytoplasm or in the nucleus. The cell
signaling pathways induced by the
steroid hormones regulate specific genes
within the cell’s DNA. The hormones and
receptor complex act as transcription
regulators by increasing or decreasing
the synthesis of mRNA molecules from
particular genes. This, in turn, determines
the amount of corresponding protein that
is synthesized from this RNA; this is
known as altering gene expression. This
protein can be used either to change the
structure of the cell or to produce
enzymes that catalyze chemical
reactions. In this way, the steroid
hormone regulates specific cell
processes. 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 in the
same way that steroid hormones do.

Amino acid-derived hormones and

polypeptide hormones are not lipid-
derived (lipid-soluble or fat-soluble);
therefore, they 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. When a hormone
binds to its membrane receptor, a G
protein that is associated with the
receptor is activated. G proteins are
proteins separate from receptors that are
found in the cell membrane. The
activated G protein, in turn, activates a
membrane-bound enzyme called
adenylyl cyclase. Adenylyl cyclase
catalyzes the conversion of ATP to cAMP.
cAMP, in turn, enables a group of
proteins called protein kinases, which
transfer a phosphate group from ATP to a
substrate molecule in a process called
phosphorylation. The phosphorylation
of a substrate molecule changes its
structural orientation, thereby activating
it. These activated molecules can then
mediate changes in cellular processes.
The hormone that initiates the signaling
pathway is called a first messenger,
which enables a second messenger in
the cytoplasm.

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Key Points

• Lipid -soluble hormones are able to

diffuse directly across the membranes of
both the endocrine cell where they are
produced and that of the target cell, as
the cell membranes are made of a lipid
bilayer.

• Amino acid-derived hormones and

polypeptide hormones are not lipid-
derived (lipid-soluble or fat-soluble);
therefore, they cannot diffuse through the
plasma membrane of cells.

• These hormones can bind to receptors

that are located either in the cytoplasm of
the cell or within the nucleus of the cell.

• When these hormones bind to their

receptors, this signals the cell to
synthesize more or less mRNA from a
gene or genes, which then results in
more or less protein being created from
those mRNA molecules.

• The increase or decrease in protein

production can alter the cell structurally
or alter how and when it catalyzes
chemical reactions.

• When a lipid (fat) insoluble hormone

binds to a plasma membrane hormone
receptor, this triggers specific actions
inside the cell that alter the cell’s
activities, such as gene expression.

• Because the first event in this sequence

is the binding of the hormone to the
plasma membrane receptor, the hormone
is called the “first messenger”, while the
molecule that is activated within the cell
and carries out intracellular change is
called the ” second messenger “.

• In many cases, a hormone binding to a

plasma membrane receptor activates a
special kind of protein called a G protein,
which in turn activates an enzyme that
generates cAMP, a second messenger.

• cAMP activates another group of

proteins called protein kinases, which can
change the structure of other molecules
by adding a phosphate group to them;
these activated molecules can then affect
changes within the cell.

Key Terms

gene expression: the transcription and

translation of a gene into messenger
RNA and, thus, into a protein

transcription: the synthesis of RNA

under the direction of DNA

steroid: a class of organic compounds

having a structure of 17 carbon atoms
arranged in four rings; they are lipids and
occur naturally as sterols, bile acids,
adrenal and sex hormones, and some
vitamins

second messenger: any substance used

to transmit a signal within a cell,
especially one which triggers a cascade
of events by activating cellular
components

cyclic adenosine monophosphate:

cAMP, a second messenger derived from
ATP that is involved in the activation of
protein kinases and regulates the effects
of adrenaline

G protein: any of a class of proteins,

found in cell membranes, that pass
signals between hormone receptors and
effector enzymes

water-soluble hormone: A lipophobic

hormone that binds to a receptor on, or
within, the plasma membrane, to initiate
an intracellular signaling cascade

lipid-soluble hormone: A lipophilic

hormone that passes through the plasma
membrane of a cell, binds to an
intracellular receptor and changes gene
expression

intracellular: inside the cell

adenylyl cyclase: an enzyme which

catalyzes the cyclization of adenosine
triphosphate (ATP) into cyclic adenosine
monophosphate (cAMP)

protein kinases: are enzymes that

regulate the biological activity of proteins
by phosphorylation of amino acids

phosphorylation: a biochemical process

that involves the addition of phosphate

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