The Largest family of integral membrane protein involved in many biological process and pathologies. 50% of all modern drugs and 25% of the top 200 best selling drugs are estimated to target GPCRs. Transduce the signals mediated by diverse signaling molecules, such as ions, peptides, lipids and photons, to induce different intracellular function. Bind their ligand and toa activate different G proteins.

1. G Protein Coupled Receptors- An
Introduction
by
Arindam Sain
PHYSIOLOGY NEWS

2. PHYSIOLOGY NEWS
 The Largest family of integral membrane protein involved in many
biological process and pathologies
 50% of all modern drugs and 25% of the top 200 best selling drugs
are estimated to target GPCRs
 Transduce the signals mediated by diverse signaling molecules, such
as ions, peptides, lipids and photons, to induce different intracellular
function
 Bind their ligand and toa activate different G proteins

3. PHYSIOLOGY NEWS
G- Protein Cycling
https://doi.org/10.1152/physrev.00015.2014

4. In unstimulated cells, the state of G
alpha is defined by its interaction with
GDP, G beta-gamma, and a GPCR.
Upon receptor stimulation by a ligand,
G alpha dissociates from the receptor
and G beta-gamma, and GTP is
exchanged for the bound GDP, which
leads to G alpha activation. G alpha
then goes on to activate other molecules
in the cell. These effects include
activating the MAPK and PI3K
pathways, as well as inhibition of the
Na+/H+ exchanger in the plasma
membrane, and the lowering of
intracellular Ca2+ levels.
PHYSIOLOGY NEWSSchneider et al., 2018

5. • Subclasses of GPCR pathway, -Gα, Gαs, Gαi, Gαq and Gα12
• downstream signaling molecules, such as adenylyl cyclase, protein kinase A (PKA),
phospholipase Cβ (PLCβ), protein kinase C (PKC) and Rho GTPase
• Change of cellular physiology and the progression of diseases.
• The dissociated Gβγ subunit is related to desensitization and apoptosis.
Experimental & Molecular Medicine volume 48, pagee207(2016)

6. PHYSIOLOGY NEWSLappano et al., 2011

7. Most human GPCRs can be grouped into five main families
• Glutamate,
• Rhodopsin,
• Adhesion,
• Frizzled/Taste2,
• Secretin,
forming the GRAFS classification system.
PHYSIOLOGY NEWS
•Schneider et al., 2018

8. Biomolecules & Therapeutics 2018; 26(2): 101-108.
PHYSIOLOGY NEWS

9. www.ptglab.comPHYSIOLOGY NEWS

10. PHYSIOLOGY NEWS

11. Selected G protein-coupled receptors that are
involved in cancer
PHYSIOLOGY NEWSLappano et al., 2011

12. Selected transduction pathways involved in GPCR-
mediated cancer signaling.
Lappano et al., 2011 PHYSIOLOGY NEWS

13. GPCR-induced transactivation of EGFR and cell proliferation
PHYSIOLOGY NEWS

14. Engineering therapeutic antibodies targeting G-protein–coupled
receptors
PHYSIOLOGY NEWShttps://www.nature.com/articles/emm2015105

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