UPSC MainsZOOLOGY-PAPER-II201510 Marks
Q19.

Describe with suitable diagrams the role of G-protein in the synthesis of C-AMP. Demonstrate how C-AMP activate protein kinase.

How to Approach

This question requires a detailed understanding of signal transduction pathways, specifically the role of G-proteins and cAMP in cellular signaling. The answer should begin by defining G-proteins and cAMP, then meticulously describe the process of cAMP synthesis triggered by G-protein activation. Crucially, it must then explain how cAMP activates protein kinase A (PKA). Diagrams are essential for clarity. The answer should be structured logically, moving from the initial signal reception to the final enzymatic activation.

Model Answer

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Introduction

Cellular communication is fundamental to all biological processes. Hormones and neurotransmitters often exert their effects by binding to cell surface receptors, initiating a cascade of intracellular events. A crucial component of this signaling is the G-protein coupled receptor (GPCR) pathway, which utilizes G-proteins and the second messenger cyclic adenosine monophosphate (cAMP) to amplify and transmit signals. This pathway is involved in a wide range of physiological processes, including vision, olfaction, and hormone responses. Understanding the precise mechanism of cAMP synthesis and its activation of protein kinase is vital for comprehending cellular regulation.

G-Proteins and cAMP: An Overview

G-proteins are a family of proteins that act as molecular switches, transducing signals from cell surface receptors to downstream effector molecules. They are heterotrimeric, consisting of α, β, and γ subunits. The α subunit binds guanine nucleotides (GDP or GTP) and is responsible for the protein’s activity. cAMP (cyclic adenosine monophosphate) is a crucial second messenger involved in many signaling pathways. It is derived from ATP and activates protein kinases, leading to cellular responses.

The Role of G-Protein in cAMP Synthesis

The process begins with a ligand (e.g., hormone) binding to a GPCR. This binding induces a conformational change in the receptor, activating the associated G-protein. Here's a step-by-step breakdown:

  1. Activation of G-protein: The activated receptor promotes the exchange of GDP for GTP on the α subunit of the G-protein.
  2. Dissociation of Subunits: GTP binding causes the G-protein to dissociate into α-GTP and βγ subunits.
  3. Activation of Adenylyl Cyclase: The α-GTP subunit (or in some cases, the βγ subunit) binds to and activates the enzyme adenylyl cyclase.
  4. cAMP Synthesis: Activated adenylyl cyclase catalyzes the conversion of ATP to cAMP.
G-protein coupled receptor pathway

(Diagram illustrating the G-protein coupled receptor pathway, showing ligand binding, G-protein activation, adenylyl cyclase activation, and cAMP synthesis. Source: Wikimedia Commons)

Activation of Protein Kinase by cAMP

cAMP, being a small, diffusible molecule, acts as a potent activator of Protein Kinase A (PKA). The activation process is as follows:

  1. cAMP Binding: cAMP binds to the regulatory subunits of PKA. PKA exists as a tetramer consisting of two regulatory (R) and two catalytic (C) subunits.
  2. Dissociation of Subunits: cAMP binding causes the regulatory subunits to dissociate from the catalytic subunits.
  3. Activation of Catalytic Subunits: The released catalytic subunits are now active and can phosphorylate specific target proteins.
  4. Phosphorylation and Cellular Response: PKA phosphorylates a variety of intracellular proteins, altering their activity and leading to a specific cellular response. These target proteins can include enzymes, ion channels, and transcription factors.
Protein Kinase A activation

(Diagram illustrating the activation of Protein Kinase A by cAMP. Source: Wikimedia Commons)

Types of G-proteins and their effects

G-protein Type Effect on Adenylyl Cyclase Second Messenger
Gs Stimulates cAMP
Gi Inhibits cAMP
Gq Activates Phospholipase C IP3 and DAG

Conclusion

In conclusion, the G-protein pathway is a critical signaling cascade that utilizes G-proteins to activate adenylyl cyclase, leading to the production of cAMP. cAMP, in turn, activates PKA, initiating a cascade of phosphorylation events that ultimately regulate cellular function. This pathway is remarkably versatile and plays a central role in numerous physiological processes. Further research continues to unravel the complexities of GPCR signaling and its implications for disease treatment and prevention.

Answer Length

This is a comprehensive model answer for learning purposes and may exceed the word limit. In the exam, always adhere to the prescribed word count.

Additional Resources

Key Definitions

Second Messenger
A second messenger is an intracellular signaling molecule released by cells in response to the detection of an extracellular signal. They amplify the initial signal and trigger a cellular response.
Phosphorylation
Phosphorylation is the addition of a phosphate group to a molecule. In cellular signaling, it is often used to activate or deactivate proteins, altering their function.

Key Statistics

Approximately 34% of all approved drugs target G protein-coupled receptors (GPCRs).

Source: Pharmacological Reviews, 2015

GPCRs are estimated to be involved in approximately 30-40% of all marketed drugs.

Source: Nature Reviews Drug Discovery, 2007 (Knowledge cutoff)

Examples

Epinephrine and cAMP

Epinephrine (adrenaline) binding to β-adrenergic receptors in heart muscle cells activates a G<sub>s</sub> protein, leading to increased cAMP levels and subsequent activation of PKA. This results in increased heart rate and contractility, preparing the body for "fight or flight".

Frequently Asked Questions

What happens if the G-protein is mutated?

Mutations in G-proteins can disrupt signal transduction, leading to various diseases. For example, mutations in G<sub>s</sub>α are associated with endocrine disorders like McCune-Albright syndrome, characterized by precocious puberty and bone abnormalities.

Topics Covered

BiologyBiochemistrySignal TransductionG-ProteincAMP