Chemistry of

signals and receptors

FAIZA RASHID
(Lecturer health sciences)
Receptors
 Receptors are protein molecules that recognize and respond to the
body’s own (endogenous) chemical messengers, such as hormones or
neurotransmitters.
 Neurotransmitters are chemical messengers in the body. Their job is
to transmit signals from nerve cells to target cells. These target cells
may be in muscles, glands, or other nerves. The brain needs
neurotransmitters to regulate many necessary functions, including:
heart rate.
 Hormones: Chemicals released from cells or glands and which travel
some distance to bind with receptors on target cells throughout the
body
Receptors

 Receptors are a special class of proteins that function

by binding a specific ligand molecule. A molecule that
binds to a receptor is called a ligand, such as a
neurotransmitter, hormone, pharmaceutical-drug,
toxin, or parts of the outside of a virus or microbe.
Receptors
 When a ligand binds to its receptor, the receptor can change
conformation, transmitting a signal into the cell.
 When a ligand binds to its corresponding receptor, it
activates or inhibits the receptor's associated-biochemical
pathway.
 While many receptors sit at the cell membrane, exposing an
outer surface to bind molecules that cannot penetrate the
cell, other receptors are located inside the cell and bind to
hormones that pass through the cell membrane. Receptors
for steroid hormones (e.g., estrogen) are among the latter
group.
The role of the receptor
Receptors can induce
 Cell growth
 Cell division
 Cell death
 Control membrane channels
 Regulate cell binding.
 Receptors also play an important role in signal
transduction, immune therapy and immune responses.
The Role of the receptor
Nerve Nerve
Signal

Messenger
Receptor

Response
Nucleus
Cell Cell
The Binding Site

Messenger Induced fit Messenger

Messenger

Cell
Membrane Receptor Receptor Receptor

Cell Cell Cell

message
Message
The role of the receptor
Receptors contain a binding site (hollow on the receptor surface) that is
recognised by the chemical messenger

Binding of the messenger involves intermolecular bonds

Binding results in an induced fit of the receptor protein

Change in receptor shape results in a ‘domino’ effect

Domino effect is known as signal transduction, leading to a chemical signal being

received inside the cell

Chemical messenger does not enter the cell. It departs the receptor unchanged and
is not permanently bound
 The Binding Site
 A hydrophobic hollow or cleft on the receptor surface - equivalent to the
active site of an enzyme

 Accepts and binds a chemical messenger

 Contains amino acids which bind the messenger

 No reaction or catalysis takes place

Binding site

ENZYME
 The Binding Site

Messenger
M

Induced fit

 Binding site is nearly the correct shape for the messenger

 Binding alters the shape of the receptor (induced fit)
 Altered receptor shape leads to further effects - signal
transduction
How does the Binding
Site Change Shape?

Phe
Phe

H
O
H
O Ser
Ser CO2
CO2 Induced
Asp Fit Asp

 Before –
 Intermolecular bonds not optimum length for maximum binding strength
 After –
 Intermolecular bond lengths optimised
 Induced Fit
 Binding interactions must be strong enough to hold the messenger
sufficiently long for signal transduction to take place
 Interactions must be weak enough to allow the messenger to
depart
 Implies a fine balance

M M

RE RE
R

Signal transduction
 Main Types of Receptors
1. Ion channel receptors

2. G-protein-coupled receptors

3. Kinase-linked receptors

4. Intracellular receptors