Hormone

Sry Suryani Widjaja

Biochemistry Department
• SIGNAL GENERATION
– The Ligand-Receptor Complex Is the Signal for
Group I Hormones
• GROUP II PEPTIDE & CATECHOLAMINE
HORMONESHAVE MEMBRANE RECEPTORS &
USE INTRACELLULAR MESSENGERS
• Intracellular signalling and signal
transduction
– Cell-surface and intracellular receptors
• Cell-surface receptors : integral
transmembrane proteins that span the plasma
membrane of a cell, with both an extracellular
and an intracellular domain
• Transmembrane receptors include G-protein-
coupled receptors, receptor tyrosine kinases,
integrins, pattern-recognition receptors and
ligand-activated ion channels.
• G-protein-coupled receptors, guanine
nucleotide-binding proteins, are a family of
proteins involved in second messenger cascades;
they alternate between an inactive guanosine
diphosphate (GDP) and active guanosine
triphosphate (GTP) bound state, ultimately
regulating downstream cell processes.
• G-proteins belong to a large group of enzymes
called GTPases
• G-proteins can refer to two distinct families of
proteins:
– Heterotrimeric G-proteins, sometimes referred to
as the ‘large’ G-proteins, which are activated by G-
protein-coupled receptors and made u p of alpha
(α), beta (β) and gamma (γ ) subunits.
• Small’ G-proteins (20–25 kDa), which belong
to the Ras superfamily of small GTPases.
– homologous to the alpha (α) subunit found in
heterotrimers, and are in fact monomeric.

– However, they also bind GTP and GDP and are

involved in signal transduction.
• Adenyl cyclase, a transmembrane protein is a
lyase enzyme,(in biochemistry, a lyase is an
enzyme that catalyses the breaking of various
chemical bonds by means other than
hydrolysis and oxidation, often forming a new
double bond or a new ring structure.
• Located in cytoplasm
• Lyases differ from other enzymes in that they
only require one substrate for the reaction in
one direction, but two substrates for the
reverse reaction).
• There are 10 known adenyl cyclases in
mammals, ADCY1 through ADCY10
• Adenyl cyclase catalyses the conversion of
ATP to 3,5-cAMP and pyrophosphate.
• Adenyl cyclase can be activated or inhibited
by G-proteins, which are coupled to
membrane receptors and thus can respond to
hormonal or other stimuli.

• Receptor tyrosine kinases. These are

transmembrane receptor proteins with an
intracellular kinase domain and an
extracellular domain that binds the ligand.
• Integrins : play a role in the attachment of a cell to the
extracellular matrix, as well as to other cells.

• Pattern recognition receptors. These are proteins

expressed by cells of the immune system that identify
molecules associated with microbial pathogens or cellular
stress. They include the so-called Toll-like receptors.

• Ligand-activated ion channels. These recognise a specific

ligand and then undergo a structural change that opens a
gap (channel) in the plasma membrane through which ions
can pass. These ions will then relay the signal.
 Intracellular receptor
• Intracellular receptors include both nuclear
receptors and cytoplasmic receptors, soluble
proteins that are localised within the
nucleoplasm and the cytoplasm.
• Typical ligands include the steroid hormones
(e.g. testosterone, progesterone, cortisol) and
derivatives of vitamins A and D, which freely
diffuse through the plasma membrane
• Nuclear receptors are ligand-activated
transcription activators.
• The glucocorticoid receptor protein
• Retinoid X receptor (RXR) and orphan
receptors
• NOD-like receptors
– belong to the pattern recognition receptors group
and are involved in the regulation of inflammatory
and apoptotic processes
• Several Hormones Act Through Calcium or
Phosphatidylinositols.
• Ionized calcium, Ca2+, is an important
regulator of a variety of cellular processes,
including muscle contraction, stimulus
secretion coupling, blood clotting cascade,
enzyme activity, and membrane excitability.
• Ca2+ is also an intracellular messenger
• of hormone action
• Phosphatidylinositide Metabolism Affects
Ca2+-Dependent Hormone Action.
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