HOAT1: Difference between revisions
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:::*Path B: Located between TM5 and TM8. | :::*Path B: Located between TM5 and TM8. | ||
::*This suggests that aromatic | ::*This suggests that aromatic residues located at the top border are important for extracellular anion binding, while residues at the bottom play a role in exporting extracellular anions to the cytoplasmic side. | ||
residues located at the top border are important for extracellular | |||
anion binding, while residues at the bottom play a role in | |||
exporting extracellular anions to the cytoplasmic side. | |||
*'''Conformational State:''' | *'''Conformational State:''' | ||
| Line 102: | Line 99: | ||
'''2. Key Interacting Residues''' | '''2. Key Interacting Residues''' | ||
:*Olmesartan occupies Site 3 of | :*Olmesartan occupies Site 3 of the binding pocket and is located within 5A˚ distance of residues of TM1, TM4, TM5, TM7, TM10, and TM11, namely N35, M207, G227, Y230, W346, Y353, Y354, F438, F442, S462, and R466. | ||
the binding pocket and is located within 5A˚ distance of residues | |||
of TM1, TM4, TM5, TM7, TM10, and TM11, namely N35, M207, | |||
G227, Y230, W346, Y353, Y354, F438, F442, S462, and R466. | |||
:*The | :*The biphenyl group and tetrazole ring of olmesartan rely on interactions with hydrophobic residues close to the bottom gate in the binding pocket. | ||
biphenyl group and tetrazole ring of olmesartan rely on interactions | |||
with hydrophobic residues close to the bottom gate in | |||
the binding pocket. | |||
:*Upon olmesartan binding, the side chain of Y230 undergoes a vertical rotation to accommodate and interact with the substrate. | :*Upon olmesartan binding, the side chain of Y230 undergoes a vertical rotation to accommodate and interact with the substrate. | ||