Sandbox Reserved 1095: Difference between revisions
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{{Sandbox_ESBS_2019}}<!-- PLEASE ADD YOUR CONTENT BELOW HERE --> | {{Sandbox_ESBS_2019}}<!-- PLEASE ADD YOUR CONTENT BELOW HERE --> | ||
== Human Angiotensin Receptor == | == Human Angiotensin Receptor == | ||
[https://en.wikipedia.org/wiki/Angiotensin#Angiotensin_II '''Angiotensin receptors'''] of type 1 belong to the [https://en.wikipedia.org/wiki/G_protein-coupled_receptor G protein coupled receptor (GPCR) family]. These transmembrane proteins interact with angiotensin II, their ligand, and play a crucial role in the renin-angiotensin-aldosterone system. AT1 receptors are predominantly expressed in cardiovascular tissues including heart, endothelium, kidney, vascular smooth muscle cells as well as lungs, brain and adrenal cortex. <ref name="Zhang2015"> PMID: 12676163 </ref> They are therefore important for the cardiovascular physiology. | [https://en.wikipedia.org/wiki/Angiotensin#Angiotensin_II '''Angiotensin receptors'''] of type 1 belong to the [https://en.wikipedia.org/wiki/G_protein-coupled_receptor G protein coupled receptor (GPCR) family]. These transmembrane proteins interact with angiotensin II, their ligand, and play a crucial role in the renin-angiotensin-aldosterone system. AT1 receptors are predominantly expressed in cardiovascular tissues including heart, endothelium, kidney, vascular smooth muscle cells as well as lungs, brain and adrenal cortex. <ref name="Zhang2015"> PMID: 12676163 </ref> They are therefore important for the cardiovascular physiology. | ||
< | <Structure load='4zud' size='376' frame='true' caption='Human angiotensin receptor'> | ||
== Functions == | == Functions == | ||
The AT1 receptors participate to the regulation of [https://en.wikipedia.org/wiki/Renin%E2%80%93angiotensin_system the renin-angiotensin-aldosterone system] and therefore to the regulation of the cardiovascular system. It occupies a crucial place in the maintaining of blood pressure, electrolyte homeostasis, water balance, hormone secretion and renal functions. | The AT1 receptors participate to the regulation of [https://en.wikipedia.org/wiki/Renin%E2%80%93angiotensin_system the renin-angiotensin-aldosterone system] and therefore to the regulation of the cardiovascular system. It occupies a crucial place in the maintaining of blood pressure, electrolyte homeostasis, water balance, hormone secretion and renal functions. | ||
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=== Primary and secondary structure === | === Primary and secondary structure === | ||
AT1 receptor consists in a 376 amino acid string <ref> [http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl?pdbcode=4zud&template=main.html Protein Database (PDBsum): 4zud. European Bioinformatics (EBI); 2013.]</ref>. The protein is composed of <scene name='82/829348/Helix_a/1'>18 alpha helix</scene> and <scene name='82/829348/B_sheet/1'>3 beta helix</scene>. Moreover, 7 alpha helix are made of a majority of hydrophobic amino acids. These helix are long enough to cross the membrane and create an <scene name='82/829348/Transmambrane_protein/1'>hydrophobic domain</scene> which is situated into the membrane. The human angiotensin receptor is therefore an alpha helical trans-membrane protein. | AT1 receptor consists in a 376 amino acid string <ref> [http://www.ebi.ac.uk/thornton-srv/databases/cgi-bin/pdbsum/GetPage.pl?pdbcode=4zud&template=main.html Protein Database (PDBsum): 4zud. European Bioinformatics (EBI); 2013.]</ref>. The protein is composed of | ||
<scene name='82/829348/Helix_a/1'>18 alpha helix</scene> | |||
and <scene name='82/829348/B_sheet/1'>3 beta helix</scene>. Moreover, 7 alpha helix are made of a majority of hydrophobic amino acids. These helix are long enough to cross the membrane and create an <scene name='82/829348/Transmambrane_protein/1'>hydrophobic domain</scene> which is situated into the membrane. The human angiotensin receptor is therefore an alpha helical trans-membrane protein. | |||
Since the angiotensin receptor belongs to the GPCRs family, those 7 alpha helix contain 3 extracellular and 3 intracellular loops. | Since the angiotensin receptor belongs to the GPCRs family, those 7 alpha helix contain 3 extracellular and 3 intracellular loops. | ||
The N terminus corresponds to the extracellular domain. The protein is made of three intracellular loops and three extracellular loops. The C terminal domain is located intracellularly. | The N terminus corresponds to the extracellular domain. The protein is made of three intracellular loops and three extracellular loops. The C terminal domain is located intracellularly. | ||
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Many ARBs contain a [https://en.wikipedia.org/wiki/Tetrazole tetrazole] group. Studies showed that tetrazole plays an important role in the binding with AT1R. | Many ARBs contain a [https://en.wikipedia.org/wiki/Tetrazole tetrazole] group. Studies showed that tetrazole plays an important role in the binding with AT1R. | ||
=== Interaction with other GPCRs === | === Interaction with other GPCRs === | ||
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The oligomeric complexes' formation complicate the understanding of AT1R pharmacology. | The oligomeric complexes' formation complicate the understanding of AT1R pharmacology. | ||
== Application in the therapeutic field == | == Application in the therapeutic field == | ||
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[[Image:Sartan_drugs.png]] | [[Image:Sartan_drugs.png]] | ||
</Structure> | |||
</ | |||
== References == | == References == | ||
<references/> | <references/> | ||
