Pharmaceutical Biochemistry

Dr. Gul Shahnaz

Hormones, Receptors and Target Cells
Hormones are chemical messengers secreted into blood or extracellular fluid by one cell
that affect the functioning of other cells
The endocrine and nervous systems function to achieve and maintain homeostasis

When the two systems work together, referred to as the neuroendocrine system, they
perform the same general functions: communication, integration, and control

IIn the
h endocrine
d i system, secreting i cellsll sendd hormone
h molecules
l l by b the
h blood
bl d to specific
ifi
target cells contained in target tissues or target organs

Endocrine action: the hormone is distributed in blood and binds to distant target cells.
Paracrine action: the hormone acts locally by diffusing from its source to target cells in the
neighborhood.
Autocrine action: the hormone acts on the same cell that produced it.
How hormones work
General principles of hormone action
Hormones signal a cell by binding to the target cell’s specific receptors in a“lock
and key
key” mechanism
Different hormone receptor interactions produce different regulatory changes
within the target cell through chemical reactions
 Hormone structure
• Based on their chemical structure hormones
are classified into three general classes
(groups) of hormones.
– 1) Amino acid derivatives hormones e.g. epinephrine
• Structurally similar to amino acids
– 2) Peptide hormones e.g. insulin
• Chains of amino acids
– 3) Lipid derivatives hormones e.g. eicosanoids and
steroid
t id h hormones ((prostaglandin
t l di iis an example
l off a
steroid hormone)
A Structural Classification of
Hormones
 Hormones Transportation

• Hormones can be
– Freely circulating
• Rapidly removed from bloodstream
– Bound to transport proteins e.g. albumin or
globulin
 Mechanisms of hormone action
• Each hormone’s shape is specific and can
be recognized by the corresponding target
cells

The binding sites on the target cells are called

hormone receptors
receptors.
– Receptors for peptide hormones, are located on
the surface of cell membranes because they can
not cross the membrane to enter the cell
– Thyroid and steroid hormones can cross the
membrane and bind to receptors in the
cytoplasm or nucleus
 G Proteins and Hormone
Hormones that
can not cross the
•
Activity
membrane (e.g.
Peptide
h
hormones) ) bind
bi d
to the receptor on
the surface of the
cell
Binding g of •
hormones to the
receptor activate
secondary
messenger (in
this figure
binding of
hormone
activates G
protein, and
activated G
protein
i activates
i
adenylcyclase
or activate PDE
or activates PLC
 Hormone Effects on Gene Activity
Hormones that •
can cross the
membrane (e.g.
steroid
hormones) bind
to the receptor
inside the cell, at
the cytoplasm, or
they will enter the
nucleus and bind
to the receptor at
the nucleus and
initiate
transcription)
 Diabetes

• Type I – Insulin dependent diabetes

– Caused by autoimmune destruction of beta cells
• Type II – non insulin dependent diabetes
– Caused by body resisting the effects of insulin at
its receptor.
• Symptoms: Polyuria (inreased frequency of
urination), polydipsia (increased thirst)
The Regulation of Blood
Glucose Concentrations
 Control of endocrine activity
• Hypothalamus regulates the activity of the
e ous and
nervous a d endocrine
e doc e systems
sys e s
– Hypothalamus secrets regulatory hormones
((releasingg hormones and inhibiting g hormones))
that control the activity of the pituitary gland
– Releasing/inhibiting
g g hormones secreted by y the
hypothalamus either stimulate or inhibit activity
of pituitary gland
Three Methods of Hypothalamic
Control over the Endocrine
System