Biology 2382B Lecture Notes - Lecture 8: Membrane Protein, Photon, Dissociation Constant

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Section 8: g-protein coupled receptors all about signalling (major drug target) Has extracellular and cytosolic domains one binds ligand and one signals. Has a transmembrane domain made of 7 a-helices. Ligand binding activates g-protein alpha subunit (gtpase enzyme) binds gtp and hydrolyzes it with help from other enzymes activates an effector generates 2nd messengers. G-alpha classes: s = stimulatory, i = inhibitory, t = transducent. Small amount of ligand generates strong response (signal amplification) Response is immediate (proteins already there; waiting to be activated) Ligands are diverse (photon, lipids, neurotransmitters, mostly odours) ~800 genes code for different gpcr"s they"re everywhere. Atp/gtp cleavage by g alpha subunit cyclization (by an effector) camp and cgmp (cyclic nucleotides serve as intracellular 2nd messengers ) They activate protein kinase a (pka) and protein kinase g (pkg) respectively. Use fret fast way to test drugs. Add yellow fluorescent protein to beta/gamma subunit. Add cyan fluorescent protein to alpha subunit.

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