GOVT. KAKTIYA P.G.

COLLEGE

MY SEMINAR TOPIC: PLASMA MEMBRANE RECEPTOR

SYNOPSIS
 INTRODUCTION
 TYPE
(1) INTERNAL RECEPTOR
(2) CELL SURFACE RECEPTOR
(A) G-PROTIN COUPLED RECEPTOR
(B) ION CHANNEL LINKED RECEPTOR
(C) ENZYME LINKED RECEPTOR
 G-PROTIN COUPLED RECEPTOR
 STRUCTURE OF GPCR
 ACTIVATION OF GPCR
 FUNCTION
 CONCLUSION
 REFRANCE
INTRODUCTION:
1. Receptors are protein molecules inside the target cell or on its surface that receive a chemical signal chemical
Signals are released by signaling cells in the form of small usually volatile or soluble molecules called ligands.
2. A ligand is a molecule that binds another specific molecule in some cases delivering a signal in the process. 3.
Ligands can thus be thought of us signaling molecues.ligands and receptors exist in several varieties however a
specific ligand will have a specific receptor the typically binds only that ligands.
4.Receptors is embeded within the plasma membrane surface of a cell.
5. receptors work like locks and keys.

Fig: Cell surface and intra cellular receptor

TYPE:
There are two types of receptors:
1.Internal receptor
2.Cell surface receptor

1. INTERNAL RECEPTOR:
1. Internal receptors also known as intra cellular or cytoplasm of the cell and respond to hydrophobic ligand
Molecules That are able to travel across the plasma membrane.
2. Once inside the cell,many of these molecules bind to proteins that
act as regulators of mRNA synthesis.recall that mRNA carries
genetic information from the DNA in a cells nucleus out to the
ribosome, where the protein is assembled.
3.When the ligand binds to the internal receptors a change in shape
is triggered that exposes a DNA-binding site on the receptor
protein.
4.The ligand receptor complexmoves into the nucleus, then binds
to special regions of the DNA and promotes the production of
mRNA from specific genes.
5.Internal receptors can directly influence gene expression without
Fig: Intra cellular receptor
having to pass the signal on to other receptors or messengers.

2. CELL SURFACE RECEPTORS:

1.Cell surface receptor, also known as transmembrane receptors, are
protein that are found attached to the cell membrane. These receptor
bind to external igand molecules.
2. This type of receptors spane the plasma membrane and perform
signal transduction, in which an extracellular signal is converted into an
intracellular signal. Ligands that interact with cell surface receptors do
not have yo enter the cell that they effect.
3. Cell scrface receptor are also called cell-specific proteins or markers
because they are specific to individual cell types.each cell surface
receptor has three main components:an external ligand-binding
domain, and a hydrophobic membrane spanning region, and an
intracellular domain inside the cell. Fig: Cell surface receptor
4. The size and extent of each of these domains vary widely, depending on the type of receptor.

There are three general categories of cell surface receptors:

1. G protein coupled receptors
2. Ion channel linked receptors
3. Enzyme linked receptor

(1)G-PROTIEN COUPLED RECEPTOR:

(1) When a g protein bind to a receptor it makes g protein + receptor complex.
G-protein+ receptor = g protein receptor complex →biological action
(2) G-Protein coupled receptor comprise a large protein family of trans
membrane receptors. They are found only in eukaryotes.
(3) The ligands which bind and activate these receptors include:
Photo sensitive compounds,odors, pheromones,
hormones and neurotransmitters.these very in size from small
molecules to peptides and large proteins.
(4) G-Protein coupled receptors are involved in many diseases,
and thus are the target of many modern medicinal drugs there are
two principal signal transduction pathways involving the
G-protein coupled receptors:the cAMP signaling pathway and
the phosphatidylinositol signaling pathway.
(5) Both are mediated via G-protein activation. The G-protein is a trimeric protein,with three subunits designated as
alpha, beta, and gamma. In response to receptor activation, the alpha subunit releases bound guanosine
diphosphate, which is displaced by guanosine triphosphate, thus activating the alpha subunit, which then
dissociates from the beta and gamma subunits.
(6) The activated alpha subunit can further intracellular signaling proteins or target functional proteins directly.

(2) ION CHANNEL LINKED RECEPTOR

(1) During the signal transduction event in a neuron the neurotransmitter binds to the receptor and alters the
conformation of the protein.This opens the ion channel, allowing extracellular ion into the cell.Ion permeability
of the olasma membrane is altered, and this transform the extracellular chemical signal into an intracellular
electric signal which alter the cell excitability.
(2) Acetylcholine receptor is a receptor linked to a cation channel. The protein consists of 4 subunits: alpha beta
gamma and delta subunits. There are two alpha subunits, with one acetycholine binding site each. This receptor
can exist in three conformations.
(3) The closed and unoccupied state is the native protein conformation. As two molecule of acetycholine both bind
to the binding sites on alpha subunits, the conformation of the receptor is altered and the gate is open, allowing
for the entry of many ions and small molecules However, this open and occupied state only lasts for a minor
duration and than the gate is closed, becoming the closed and occupied state.
(4) The two molecules of acetycholine will soon dissociate from the receptor, returning it to the native closed and
unoccupied state.

Fig: Ion channel

(3)ENZYME LINKED RECEPTOR

(1) Enzyme linked receptors are cell surface receptors with intracellular domain that are associate with an enzyme. In
some cases, the intracellular domain of the receptor itself is an enzyme or the enzyme linked receptor has
intracellular domain that intreracts directly with an enzyme.
(2) The enzyme linked receptor normally have large extracellular and intracellular domains, but the membrane –
spanning region consists of a single alpha-helical region of the peptide strand.
(3) When a ligand binds to the extracellular domain, a signal is transferred through the membrane and activates the
enzyme, which sets off a chain of events within the cell that eventually leads to a response. An example of this type
of enzyme linked receptor is the tyrosine kinase receptor.
(4) The tyrosine kinase receptor transfer phosphate groups
To tyrosine molecules. Signaling molecules bind to the extracellular domain of two nearby tyrosine kinase receptors,
which then dimerize.
(5) Phosphate are than added to tyrosine residues on the intracellular domain of the receptors and can then transmit
the signal to the next messenger within the cytoplasm.

Fig: Enzyme linked receptor

STRUCTURE OF GPCR
(1)The Molecules have 7 trans membrane alpha helical like structure that is embedded within the plasma membrane
surface of a cell.

(2) plasma membrane outer side extracellular region and inner

side cytosol region present.

.(3) There are 6 loops – 3 extra cellular loops and 3 intra cellular
loops.
(4) Amino group present in extra cellular fluid region and
carboxylic group present in cytosol region.
(5) 5th and 6th segment that interact with g protein.
(6) 6th loop is called messenger binding site.

Fig: Structure Of GPCR

Activation of G-protein coupled receptor
1.G proteins act very much like molecular switches, who’s “on” or “off” state depends on whether to GTP (guanosine
triphosphate) or GDP (guanosine diphosphate).There are two distinct classes of G proteins: the large heterotrimeric
G proteins and the small monomeric G proteins.
2.The large heterotrimeric G proteins contain three different subunits, called G alpha, G beta, and G
gamma.Heterotrimeric G proteins mediate signal transduction through G protein-linked receptors.The small
monomeric G proteins include Ras
3.G proteins have the same basic structure and mode of activation. Of the three subunits in the heterotrimer, The
largest, binds to a guanine nucleotide (GDP or GTP). When binds to GTP, it also detaches from the complex.
4.The and subunits, on the other hand, are permanently bound together. Some G proteins, such as Gs , act as
stimulators of signal transduction (hence s, for “stimulatory”); others, such as Gi , act to inhibit signal transduction
(hence i, for “inhibitory”).
5.When a messenger binds to a G protein-linked receptor on the surface of the cell, the change in conformation of the
receptor causes a G protein to associate with the receptor,Which in turn causes the subunit to release its bound
GDP.
6. Then acquires a new, different molecule of GTP and detaches from the complex. Depending on the G protein and
the cell type, either the free GTP- subunit or the complex can then initiate signal transduction events in the cell.
7. Each portion of the G protein exerts its effect by binding to a particular enzyme or other protein in the cell. In
some cases, both the GTP- and subunits simultaneously regulate different processes in the cytosol.
8. The activity of a G protein persists only as long as the subunit is bound to GTP, and the subunits remain separated.
Because the subunit catalyzes GTP hydrolysis, it remains active only until it hydrolyzes its associated GTP to
GDP, at which time it reassociates with. This feature allows the signal transduction pathway to shut down when the
messenger is utilized.
9.Some Ga Gbg Ga Ga Ga Gbg Ga Gbg Ga Gbg Ga Ga proteins are very inefficient at catalyzing GTP hydrolysis;
however, their efficiency is dramatically improved by regulators of G protein signaling (RGS) proteins.
10.When RGS proteins bind , they stimulate GTP hydrolysis. Such gtpase activating proteins (gaps) are important
regulators of G protein function, as we will see later in the case of the Ras protein.
11.The large number of different G proteins provides for a diversity of G protein-mediated signal transduction events,
only a few of which we will consider here.Perhaps the most important and widespread G protein-mediated signal
transduction events are the release or formation of second messengers.

Fig: Activation of G-Protein coupled receptor

FUNCTION
(1) Receptors are specialized integral membrane protein that take part in communication between cell and the
out side world.
(2) Receptors perform signal transduction in which an extra celluler signal is converted into an
inter celluler signal
(3) To intergrate various extra cellular and intra cellular regulatory signals.
(4) To propagate regulatory signals from outside to inside the effector cell when the molecular species carrying the
signal can't itself penetrate the cell membrane.
CONCLUSION
A signal in cell produces is recognized by a target cell by means of a receptor protein. The receptor protein perform
the first step in a series of transduction process by converting the incoming extra cellular signal to an intra cellular
signal that direct the cells behavior.
REFERENCE

BOOK NAME AUTHOR NAME PUBLICATION EDITION YEAR

BACKLESS CELL JEFF HARDINE PARSN 7th 2007

BIOLOGY PUBLICATION