signal transduction 2 - Signal Transduction 2 Bioc 460...

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Unformatted text preview: Signal Transduction 2 Bioc 460 Spring 2010 Please see learning objectives and assignments from part one. G protein-coupled receptors are involved in many biological processes G protein-coupled receptors are involved in many biological processes GCPRs are important drug targets Table from Klabunde, T and Hessler, G ChemBioChem 2002: 928-944 Agonists bind receptors and modulate their function Antagonists bind receptors without affecting the function, instead antagonists block ligand binding The signature feature of all GPCR signaling is the cycling between the GTP-bound, active, conformation and the GDP-bound, inactive, conformation of the heterotrimeric G-protein. Glucagon and epinephrine are metabolically important hormones that bind GCPRs Glucagon (29 amino acid polypeptide) NH 2-His-Ser-Gln-Gly-Thr-Phe- Thr-Ser-Asp-Tyr-Ser-Lys-Tyr- Leu-Asp-Ser- Arg-Arg-Ala-Gln- Asp-Phe-Val-Gln-Trp-Leu- Met- Asn-Thr-COOH Epinephrine is a catecholamine derived from tyrosine Binding of epinephrine to its cognate GPCR initiates a signaling cascade that results in activation of protein kinase A...
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signal transduction 2 - Signal Transduction 2 Bioc 460...

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