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Serpentine Receptors

Serpentine Receptors. Presented by Ayush Kishore 04.04.2008 Biochemistry II. Background Information. Integral proteins that have 7 hydrophobic regions that “snake” across the membrane Also known as G Protein Coupled Receptors (GPCR) and 7 Transmembrane Segment Receptors (7TMSR)

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Serpentine Receptors

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  1. Serpentine Receptors Presented by AyushKishore 04.04.2008 Biochemistry II

  2. Background Information • Integral proteins that have 7 hydrophobic regions that “snake” across the membrane • Also known as G Protein Coupled Receptors (GPCR) and 7 Transmembrane Segment Receptors (7TMSR) • Found in in many organ systems • 6 Classes of Serpentine Receptors: differentiated by characteristic motifs

  3. The Basic Mechanism of Serpentine Receptors External Ligand Conformation Change in Receptor G Protein indirectly catalyzes events in the cell G Protein Activated

  4. Mechanism of Transduction in Liver Cell

  5. Activation/Inactivation of Stimulatory G Protein

  6. Stopping the Signal • Signal transduction is regulated by a feed-back mechanism • G protein-coupled receptor kinases phosphorylate the domain • A binding site is created for beta-arrestin at the domain • When beta-arresting binds, the domain can not interact with the stimulatory G protein so that transduction is stopped

  7. Chronic Obstructive Pulmonary Disease • Characterized by limited airflow to airways • Cause by smoking • Salbutamol is an agonist of beta-adrenergic cells in the airway • The effect is airway dilation

  8. Heptahelical Domain

  9. References • Cox, M. M. & Nelson, D. L. The Principles of Biochemistry. Lehninger. 4th edition. 2005 • Gurevich, V.V, Gurevich, E.V. Trends in Pharmacological Sciences, Article in Press

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