HORMONE
ACTION
INTRODUCTION
Hormones:
Chemical substances synthesized by one
type of cells & transported through blood
to act on another type of cells.
Endocrine
Paracrine
Autocrine
Insulin
GIT hormones
Prostaglandins
Functions
Homeostatic control.
PTH- Ca, ADH- Water
Regulation of production,
use , storage of energy.
Insulin, Glucagon
Classificatio
n
Steroid hormones
Cortisol, Androgen, Estrogen
Hydrophobic, circulate with transport proteins,
half life (30-90 mins)
bind with intracellular receptor
Steroid hormones
Thyroid hormones
Solubility
Transport
proteins
Plasma half
life
Group I
Lipophilic
Yes
Group II
Hydrophilic
No
Long
Short (minutes)
( hours to
days)
Receptor
Intracellular
Plasma
membrane
Mediator
Hormone
receptor
complex
cAMP, cGMP,
Ca2+, IP3, DAG,
Protein kinase
Examples.
Steroids,
Polypeptides,
HORMONE RECEPTORS
Hormone regulation molecules
Hormones mediates biological effect
by binding to specific receptors
Hormones receptors are proteins
Functional Domains of hormone
receptors
Recognition domain
Signal transduction domain
INSULIN RECEPTORS
Insulin receptors hetero tetra dimers (22)
Dimer is linked by multiple disulfide bonds
The extra-membrane -subunit binds with
insulin
The membrane spanning -subunit through
the tyrosine residue transduces the signal
STEROID HORMONE
RECEPTORS
Functional domains
GROUP I HORMONES
Mechanism of action:
Through intracellular receptors gene
expression
Hormones lipophilic
Passive diffusion
In the cytoplasm binds with receptors
forming HRC
GROUP II HORMONES
Mechanism of action:
Through intracellular receptors gene
expression
Hormones lipophilic
Passive diffusion
In the cytoplasm binds with receptors
forming HRC
Glucagon
, 2 Adrenergic Catecholamines
ACTH
TSH
LH
FSH
PTH
ADH
HCG
CRH
Calcitonin
MSH
Somatostatin
GTP
cGMP
Several compounds (eg., Nitric oxide, ANP )
activate guanylyl cyclase which in turn
increase cGMP
cGMP as second messenger, avtivates
protein kinases & phosphorylates certain
enzymes
Phosphorylated enzymes causes smooth
muscle relaxation & vasodilation
cGMP also involved in rhodopsin visual cycle
1-Adrenergic catecholamines
Acetylcholine (muscarinic)
Angiotensin II
Cholecystokinin
Gastrin
Gonadotropin-releasing hormone
Oxytocin
Platelet-derived growth factor (PDGF)
Substance P
Thyrotropin-releasing hormone
(TRH)
Insulin
Growth hormone (GH)
Prolactin
Insulin-like growth factors I and II
Chorionic somatomammotropin
Epidermal growth factor
Erythropoietin
Fibroblast growth factor (FGF)
Leptin
Nerve growth factor (NGF)
Platelet-derived growth factor
Adiponectin
Class
Mediator
Examples
Group I
Cytosolic
receptor
Hormone
receptor
complex
Corticoids,
Androgen
,Estrogen
Nuclear
receptor
Hormone
receptor
complex
Thyroid
hormones
Vitamin D
cAMP
Glucagon,Cate
cholamines,TS
H,ACTH,LH,FS
H,PTH
Group II
Cell
membrane
receptor
cGMP
Ca2+, IP3,
NO, ANP
TRH,
Protein Kinases
Protein kinases
phosphorylate
proteins i.e. they
add one or more
phosphates
The change in
charge at that site
makes major
changes in the
conformation,
affects activity
cAMP is inactivated
by
phosphodiesterases
, which quickly act
to downregulate its
activity
cAMP
Cyclic AMP is most common second messenger.
Hormones bind receptors and membrane-bound adenylyl
cyclase is activated via the G protein
Adenylyl cyclase catalyzes the conversion of ATP to cAMP
cAMP activates protein kinases
Protein kinases catalyze the phosphorylation of a specific
protein, which triggers a chain of reactions leading to the
particular metabolic effect of the hormone
Protein kinases are very specific in action
cAMP is rapidly inactivated and converted to AMP
1.
2.
3.
4.
5.
6.
7.
Steroid is secreted
Passes into cell
Into nucleus
Binds receptor, DNA
Activates or represses transcription
Controls translation
Peptide alters cellular activity