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Cellular singling and different
types of receptors:
Dr: AYUB ABDULKADIR SHEIKH ABDI
Course outline
1) Signaling Through Ion Channels.
2) Signaling Through Enzyme And Enzyme
Coupled Receptors.
3) Signaling Through G Protein Coupled
Receptors.
4) Signaling Through Intracellular Receptors.
5) Signaling Through Receptors That Undergo
Cleavage
1- Signaling Through Ion Channel
Receptors:
• An ion channel receptor is a type of plasma
membrane receptor that contains both a messenger-
binding site and an ion channel.
2 a- Signaling Through Enzyme
Receptors:
• An enzyme receptor is a type of plasma
membrane receptor that contains a messenger-
binding site, a transmembrane segment, and a
site that functions as an enzyme.
• There are two major categories of enzyme
receptors:
1. Receptor tyrosine kinases.
2. Receptor guanylyl cyclases.
A) Receptor Tyrosine Kinases:
B) Receptor Guanylyl Cyclases:
2b- Signaling Through Enzyme-
Coupled Receptors:
• An enzyme-coupled receptor is a type of plasma
membrane receptor that contains a messenger-
binding site, a transmembrane segment, and a site
coupled to a separate enzyme.
• The enzyme coupled receptors has different types of
proteins compared to the other enzyme receptors
mention above.
• For many enzyme-coupled receptors, the enzyme
that is linked to the receptor is a janus kinase ( JAK), a
type of tyrosine kinase.
Signal transducers and
activators of transcription
(STATs)
3- Signaling Through G Protein-
Coupled Receptors:
• A G protein-coupled receptor is a type of plasma
membrane receptor that contains a messenger-
binding site, a transmembrane segment, and a
site coupled to a G protein.
• A G protein is a membrane protein that is so-
named because it binds guanosine nucleotides,
either guanosine diphosphate (GDP) or guanosine
triphosphate (GTP).
• Three subunits comprise a G protein: alpha (α),
beta (β), and gamma (γ).
These components of the G protein function in the following way:
• When the α subunit is bound to GDP, the G protein is inactive.
• Once a messenger activates a G protein-coupled receptor, the
receptor undergoes a conformational change that triggers the
α subunit of the G protein to release GDP in exchange for GTP.
The binding of GTP to the α subunit causes the G protein to
undergo a conformational change and become activated.
• Upon activation, the α subunit typically separates from the β
and γ subunits, which remain together as a βγ complex. Then
either the α subunit or βγ complex moves along the cytosolic
surface of the plasma membrane to alter the activity of a target
protein that is involved in the next step of the signal
transduction pathway.
A) G Protein Signaling Pathways That Use
Cyclic AMP as a Second Messenger:
cyclic AMP
Gs (s = stimulatory).
G protein inhibatory that innactivates
the Adenylyl cyclase:
B) G Protein Signaling Pathways That Use IP3,
DAG, and Calcium as Second Messengers:
Phosphatidylinositol bisphosphate (PIP2).
Diacylglycerol (DAG).
Inositol trisphosphate (IP3).
C) G Protein Signaling Pathways That
Use phosphodiesterase
Lipoxins
D) G Protein Signaling Pathways That
Use phospholipase A2
Cellular signaling
E) G Protein Regulation of Ion Channels:
• G protein regulating of ion channels either opens
or close ion channels.
• Many neurotransmitters activate G protein
signaling pathways that either:
• Directly (the G protein directly opens the ion
channel by binding to it)
• Indirectly regulate ion channels.
o Direct regulation of an ion channel
by a G protein:
o Indirect regulation of an ion channel
by a G protein:
• These proteins, located in the cytosol or
nucleus, are ligand-activated transcription
factors.
• These receptors link extracellular signals to
gene transcription.
4- Signaling Through Intracellular
Receptors
A) Signaling pathway used by
nitric oxide:
MLCK = myosin light chain kinase.
B) Signaling pathway used by
Thyroid hormones:
C) Signaling pathway used by
Steroids:
Glucocorticoid
Heat shock protein
Glucocorticoid response element
• In response to ligand binding, some transmembrane
proteins undergo regulated intramembranous
proteolysis (RI), which liberates one or more fragments of
their cytosolic domain that signal a cellular response by
entering the nucleus to modulate gene expression.
5- Signaling through Receptors that
undergo cleavage:

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Cellular signaling

  • 1. Cellular singling and different types of receptors: Dr: AYUB ABDULKADIR SHEIKH ABDI
  • 2. Course outline 1) Signaling Through Ion Channels. 2) Signaling Through Enzyme And Enzyme Coupled Receptors. 3) Signaling Through G Protein Coupled Receptors. 4) Signaling Through Intracellular Receptors. 5) Signaling Through Receptors That Undergo Cleavage
  • 3. 1- Signaling Through Ion Channel Receptors: • An ion channel receptor is a type of plasma membrane receptor that contains both a messenger- binding site and an ion channel.
  • 4. 2 a- Signaling Through Enzyme Receptors: • An enzyme receptor is a type of plasma membrane receptor that contains a messenger- binding site, a transmembrane segment, and a site that functions as an enzyme. • There are two major categories of enzyme receptors: 1. Receptor tyrosine kinases. 2. Receptor guanylyl cyclases.
  • 7. 2b- Signaling Through Enzyme- Coupled Receptors: • An enzyme-coupled receptor is a type of plasma membrane receptor that contains a messenger- binding site, a transmembrane segment, and a site coupled to a separate enzyme. • The enzyme coupled receptors has different types of proteins compared to the other enzyme receptors mention above. • For many enzyme-coupled receptors, the enzyme that is linked to the receptor is a janus kinase ( JAK), a type of tyrosine kinase.
  • 8. Signal transducers and activators of transcription (STATs)
  • 9. 3- Signaling Through G Protein- Coupled Receptors: • A G protein-coupled receptor is a type of plasma membrane receptor that contains a messenger- binding site, a transmembrane segment, and a site coupled to a G protein. • A G protein is a membrane protein that is so- named because it binds guanosine nucleotides, either guanosine diphosphate (GDP) or guanosine triphosphate (GTP). • Three subunits comprise a G protein: alpha (α), beta (β), and gamma (γ).
  • 10. These components of the G protein function in the following way: • When the α subunit is bound to GDP, the G protein is inactive. • Once a messenger activates a G protein-coupled receptor, the receptor undergoes a conformational change that triggers the α subunit of the G protein to release GDP in exchange for GTP. The binding of GTP to the α subunit causes the G protein to undergo a conformational change and become activated. • Upon activation, the α subunit typically separates from the β and γ subunits, which remain together as a βγ complex. Then either the α subunit or βγ complex moves along the cytosolic surface of the plasma membrane to alter the activity of a target protein that is involved in the next step of the signal transduction pathway.
  • 11. A) G Protein Signaling Pathways That Use Cyclic AMP as a Second Messenger: cyclic AMP Gs (s = stimulatory).
  • 12. G protein inhibatory that innactivates the Adenylyl cyclase:
  • 13. B) G Protein Signaling Pathways That Use IP3, DAG, and Calcium as Second Messengers: Phosphatidylinositol bisphosphate (PIP2). Diacylglycerol (DAG). Inositol trisphosphate (IP3).
  • 14. C) G Protein Signaling Pathways That Use phosphodiesterase
  • 15. Lipoxins D) G Protein Signaling Pathways That Use phospholipase A2
  • 17. E) G Protein Regulation of Ion Channels: • G protein regulating of ion channels either opens or close ion channels. • Many neurotransmitters activate G protein signaling pathways that either: • Directly (the G protein directly opens the ion channel by binding to it) • Indirectly regulate ion channels.
  • 18. o Direct regulation of an ion channel by a G protein:
  • 19. o Indirect regulation of an ion channel by a G protein:
  • 20. • These proteins, located in the cytosol or nucleus, are ligand-activated transcription factors. • These receptors link extracellular signals to gene transcription. 4- Signaling Through Intracellular Receptors
  • 21. A) Signaling pathway used by nitric oxide: MLCK = myosin light chain kinase.
  • 22. B) Signaling pathway used by Thyroid hormones:
  • 23. C) Signaling pathway used by Steroids: Glucocorticoid Heat shock protein Glucocorticoid response element
  • 24. • In response to ligand binding, some transmembrane proteins undergo regulated intramembranous proteolysis (RI), which liberates one or more fragments of their cytosolic domain that signal a cellular response by entering the nucleus to modulate gene expression. 5- Signaling through Receptors that undergo cleavage: