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e-Learning Module 1 - Drug Targets I
Structure of a GPCR subunit 7 transmembrane domains. N terminus extracellular. Large loop between TM5 and TM6.
Structure of a ligand gated ion channel subunit (eg: nicotinic acetylcholine receptor)
4 transmembrane domains. N terminus extracellular. large loop between
TM3 and TM4.
TM2 forms lining of channel.
Structure of a voltage gated sodium or calcium channel 24 TM domains, arranged into 4 pseudosubunits. TM4 is the voltage sensor. There is a membrane dipping loop between TM5 and TM6.
N terminus intracellular.
The G protein Gs is coupled to adenylate cyclase (positively).
The G protein Gi is coupled to adenylate cyclase (negatively).
The G protein Gq is coupled to phospholipase C.
IP3 = Inositol tris-phosphate. A second messenger produced in the phospholipase C
pathway (coupled to Gq).
Nuclear hormone receptors are usually present in the cytoplasm.
In Transactivation nuclear hormone receptors must Bind ligand, dissociate from heat shock proteins and dimerize before entering the nucleus.
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