PHAR 435 Lecture Notes - Lecture 2: Angiotensin Ii Receptor Type 1, Morphine, Pharmacophore

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To understand the structure and function (movement) at the molecular level of cell surface receptors and ion channels. Channel/receptor structure transport of ions and/or information contained in a molecule (neurotransmitter, hormone, etc. ) across the cell membrane voltage/ligand gated ion channels, g-protein coupled receptors, enzyme (kinase) associated receptors. Span the membrane integral transmembrane (polytropic) proteins) Be compatible with the composition of the membrane. 3 domains: extracellular (ec) domain: gpcrs/liga(cid:374)d gated (cid:272)ha(cid:374)(cid:374)els pla(cid:455)s a (cid:396)ole i(cid:374) (cid:862)liga(cid:374)d(cid:863) (cid:271)i(cid:374)di(cid:374)g, transmembrane (tm) domain: traverses the lipid bilayer. Intracellular (ic) domain: interacts with the interior of the cell. The alpha-heli(cid:454) (cid:272)a(cid:374)"t (cid:271)e (cid:272)o(cid:373)p(cid:396)essed/(cid:271)e(cid:374)t (cid:271)e(cid:272)ause the h-bond partners are too close together and it would be unfavorable to do so. It"s ideal to (cid:271)e (cid:374)eut(cid:396)al i(cid:374) the lipid (cid:271)ila(cid:455)e(cid:396) e(cid:374)(cid:448)i(cid:396)o(cid:374)(cid:373)e(cid:374)t. = molecules in which one surface is hydrophobic and the other more hydrophilic. Hydrophilic side interacts with the other helices. Hydrophobic side interacts with the lipid bilayer.

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