BIOL 2P03 Lecture Notes - Lecture 7: Guanine Nucleotide Exchange Factor, Bacterial Effector Protein, G Protein–Coupled Receptor
17 Apr 2017
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Document Summary
Importance of gpcrs: gpcrs represent the largest and most diverse class of plasma membrane receptors. In humans alone, there are approximately 1,000 different gpcrs. Between 1/3 to 1/2 of all pharmaceutical drugs act on gpcrs: gpcrs regulate almost every physiological function in the human body, dr. alfred gilman and dr. martin rodbell were jointly awarded the nobel prize in. Physiology or medicine in 1994 for their discovery of gpcrs. Signal detection by gpcrs: gpcrs can detect many different physical and chemical signals, including: Small organic molecules such as odorants, tastants, neurotransmitters. Structure of gpcrs: gpcrs share a common architecture. Extracellular region of receptor helps form ligand binding site and is responsible for modulating ligand access to the binding site. Transmembrane region helps form ligand binding site and undergoes conformational changes necessary to induce intracellular signaling. Intracellular region associates with cytosolic signaling molecules, such as heterotrimeric g-proteins. Subunit and / subunits are bound to the inner leaflet of the plasma membrane.
