Hormones. Mechanism of
regulatory effects
prof. Davydov V.V.
Department of biochemistry and molecular biology
Hormones refers to biologically active substances
which are synthesized in endocrine glands, secreted into
the bloodstream and have a regulatory effect on the
metabolism and function of certain visceral organs.
Role of hormones:
- take part in the integration of metabolism in the
various tissues in the human body;
- take part in the adaptation of metabolism to effect of
adverse factors
Classification of hormones
• hypothalamic hormones (liberins, statins);
• anterior pituitary hormones (adrenocorticotropic hormone –
ACTH, growth hormone, follicle stimulating hormone, luteinizing
hormone, luteotropic hormone, thyroid stimulating hormone);
• posterior pituitary hormone (vasopressin, oxytocin);
• thyroid hormones (thyroxine, triiodothyronine, calcitonin);
• parathyroid hormone (PTH);
• pancreatic hormones (insulin, glucagon);
• hormones of adrenal cortex (glucocorticoids, mineralocorticoids)
and adrenal medulla (epinephrine);
• sex hormones (testosterone, estradiol);
Membrane receptor
Cytoplasm receptor
Mechanism regulatory effects of hormones which
bind with intracellular (cytoplasmic) receptors
Mechanism regulatory effects of hormones which
bind with membrane receptors
Classification of hormones which bind with
membrane receptors
№ hormone effector
protein
second
massager
1 ACTH, ТТH,
calcitonin,
glucagon,
epinephrine, FSH,
LH, MSH
adenylate
cyclase
cAMP
2 atrial nairiuretic
peptide
guanylate
cyclase
cGMP
3 Vasopressin (V1),
gastrin, tyroliberin,
gonadoliberin
phospholipase
С
1,2-diacylglycerol,
inositol 1,4,5-
triphosphate, Са2+
4 insulin,
oxytocin
- -
Mechanism of regulatory effect of hormones
which effect are mediated by activation of
adenylate cyclase
Structure of β2–adrenergic receptor
(serpentine receptor)
Mechanism of regulatory effect of hormones
which effect are mediated by activation of
adenylate cyclase
Scheme of G-protein transformations
Mechanism of regulatory effect of hormones
which effect are mediated by activation of
adenylate cyclase
cАMP
N
NN
N
NH2
O
OH
CH2O
O
P
OH
O
Mechanism of activation of protein kinase A by cAMP
Protein phosphorylation by protein kinase A
Enzymes which are regulated by cAMP-dependent
phosphorylation
Enzyme Pathway
Glycogen synthase
Kinase phosphorylase
Pyruvate kinase
Phosphofructokinase
Pyruvate dehydrogenase
complex
Hormone sensitive lipase
Fructose 1,6-bisphospha-
tase
CREB (cAMP response
element-binding protein)
– factor of transcription
Glycogen synthesis
Glycogenolysis
Glycolysis
Glycolysis
Oxidative decarboxylation of
pyruvate
Lipolysis
Gluconeogenesis
CRE of DNA – take part in
the regulation of gene
expression
Mechanism of regulatory effect of hormones
which effect are mediated by activation of
adenylate cyclase
Classification of adrenoreceptors
Effect of cholera toxin
Effect of pertussis toxins
дифтерия
Classification of hormones which interact with
membrane receptors
№ hormone effector
protein
second
massager
1 ACTH, ТТH,
calcitonin, glucagon,
epinephrine, FSH,
LH, MSH
adenylate
cyclase
cAMP
2 atrial nairiuretic
peptide
guanylate
cyclase
cGMP
3 vasopressin,
gastrin, thyroliberin,
gonadoliberin
phospholipase
С
1,2-diacylglycerol,
inositol 1,4,5-
triphosphate, Са2+
4 insulin,
oxytocin
- -
Mechanism formation of the cellular response to
the vasopressin
Reaction, which are catalyzed by phospholipase C
CH2O-CO-R
CHO-CO-R1
CH2
O
POH O
O
OHOH
OH OPO3H
2
OPO3H
2
CH2O-CO-R
CHO-CO-R1
CH2
OH
OPO3H
2
OHOH
OH OPO3H
2
OPO3H
2
H2O+
PL C+
phosphatidyl inositol
4,5-bisphosphate
1,2-diacylglycerol
(DAG) inositol
1,4,5-triphosphate
(IP3)
Mechanism formation of the cellular response to
the vasopressin
Complex calcium-calmodulin
Some intracellular proteins regulated by calcium-
calmodulin complex
Adenylate cyclase
Glutamate decarboxylase
Myosin light chain kinase
Nitric oxide synthase
Ca-ATPase (Ca2+-pump
of membranes)
Mechanism formation of the cellular response to
the vasopressin
Classification of hormones which interact with
membrane receptors
№ hormone effector
protein
second
massager
1 ACTH, ТТH,
calcitonin, glucagon,
epinephrine, FSH,
LH, MSH
adenylate
cyclase
cAMP
2 atrial nairiuretic
peptide
guanylate
cyclase
cGMP
3 vasopressin,
gastrin, thyroliberin,
gonadoliberin
phospholipase
С
1,2-diacylglycerol,
inositol 1,4,5-
triphosphate, Са2+
4 insulin,
oxytocin
- -
Receptor to ANP
Guanylate cyclase reaction
O
N
N
N
N
OH
OH
CH2O
O
P O
OH
NH2
cGMP
GTP + H2O cGMP + H4P2O7
Tyrosine kinase mechanism
effect of hormones
1. Activation of receptor
2.Phosphorylation proteins
3. Activation of MAP kinases
or STAT kinases
4. Activation of genes
expression in nucleus
Thanks for your listening!
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