Angiotensin receptor
Oxford Dictionary of Biochemistry:
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angiotensin receptor
any of several membrane proteins that bind angiotensin, and mediate its intracellular effects. Two types of receptor, AT1 and AT2, have been identified on the basis of their response to drugs. The AT1 receptor (previously known as AII1 or AIIα) has high affinity for losartan, and lower affinity for CGP42112A; the reverse is true for AT2 receptors. The potency of endogenous ligands is angiotensin II > angiotensin III. In peripheral tissues, AT1 receptors, but not AT2 receptors, interact with G proteins, inhibit adenylate cyclase, and activate phospholipases C and A2. AT2 receptors may stimulate a phosphotyrosine phosphatase leading to inhibition of guanylate cyclase. Sulfhydryl reducing agents inhibit the binding of angiotensin II to AT1 receptors, but enhance its binding to AT. Both types are G protein-coupled 7TM proteins.
| angiotensin converting enzyme inhibitors, angiotensin converting enzyme, angiotensin | |
| angiotensinase, angiotensinogen, angle |
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Angiotensin receptor
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Angiotensin receptor
| angiotensin II receptor, type 1 | |
|---|---|
| Identifiers | |
| Symbol | AGTR1 |
| Alt. symbols | AGTR1B |
| IUPHAR | AT1 |
| Entrez | 185 |
| HUGO | 336 |
| OMIM | 106165 |
| RefSeq | NM_000685 |
| UniProt | P30556 |
| Other data | |
| Locus | Chr. 3 q21-q25 |
| angiotensin II receptor, type 2 | |
|---|---|
| Identifiers | |
| Symbol | AGTR2 |
| IUPHAR | AT2 |
| Entrez | 186 |
| HUGO | 338 |
| OMIM | 300034 |
| RefSeq | NM_000686 |
| UniProt | P50052 |
| Other data | |
| Locus | Chr. X q22-q23 |
The angiotensin receptors are a class of G protein-coupled receptors with angiotensin II as their ligands.[1] They are important in the renin-angiotensin system: they are responsible for the signal transduction of the vasoconstricting stimulus of the main effector hormone, angiotensin II.[2]
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Contents
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Structure
The AT1 and AT2 receptors share a sequence identity of ~30%, but have a similar affinity for angiotensin II, which is their main ligand.
Members
Overview table
| Receptor | Mechanism[3] |
|---|---|
| AT1 | |
| AT2 | |
| AT3 | |
| AT4 |
AT1
Main article: Angiotensin II receptor type 1
The AT1 receptor is the best elucidated angiotensin receptor.
Location within the body
Angiotensin receptors are found (within these organs, or organ structures or objects) within the body. The AT1 subtype is found in the heart, blood vessels, kidney, adrenal cortex, lung and brain and mediates the vasoconstrictor effects. AT2 is probably involved in vascular growth.
Mechanism
The angiotensin receptor is activated by the vasoconstricting peptide angiotensin II. The activated receptor in turn couples to Gq/11 and Gi/o and thus activates phospholipase C and increases the cytosolic Ca2+ concentrations, which in turn triggers cellular responses such as stimulation of protein kinase C. Activated receptor also inhibits adenylate cyclase and activates various tyrosine kinases.[2]
Effects
Effects mediated by the AT1 receptor include vasoconstriction, aldosterone synthesis and secretion, increased vasopressin secretion, cardiac hypertrophy, augmentation of peripheral noradrenergic activity, vascular smooth muscle cells proliferation, decreased renal blood flow, renal renin inhibition, renal tubular sodium reuptake, modulation of central sympathetic nervous system activity, cardiac contractility, central osmocontrol and extracellular matrix formation.[4]
AT2
Main article: Angiotensin II receptor type 2
AT2 receptors are more plentiful in the fetus and neonate. The AT2 receptor remains enigmatic and controversial. Effects mediated by the AT2 receptor are suggested to include inhibition of cell growth, fetal tissue development, modulation of extracellular matrix, neuronal regeneration, apoptosis, cellular differentiation, and maybe vasodilation and left ventricular hypertrophy.[5]
AT3 and AT4
Other poorly characterized subtypes include the AT3 and AT4 receptors. The AT4 receptor is activated by the angiotensin II metabolite angiotensin IV, and may play a role in regulation of the CNS extracellular matrix, as well as modulation of oxytocin release.[6][7][8][9][10][11][12][13]
See also
References
- ^ de Gasparo M, Catt KJ, Inagami T, Wright JW, Unger T (2000). "International union of pharmacology. XXIII. The angiotensin II receptors". Pharmacol. Rev. 52 (3): 415–72. PMID 10977869. http://pharmrev.aspetjournals.org/cgi/content/abstract/52/3/415.
- ^ a b Higuchi S, Ohtsu H, Suzuki H, Shirai H, Frank GD, Eguchi S (2007). "Angiotensin II signal transduction through the AT1 receptor: novel insights into mechanisms and pathophysiology". Clin. Sci. 112 (8): 417–28. doi:10.1042/CS20060342. PMID 17346243.
- ^ Unless else specified in box, then ref is: Senselab
- ^ Catt KJ, Mendelsohn FA, Millan MA, Aguilera G (1984). "The role of angiotensin II receptors in vascular regulation". J. Cardiovasc. Pharmacol. 6 (Suppl 4): S575–86. doi:10.1097/00005344-198406004-00004. PMID 6083400.
- ^ D'Amore A, Black MJ, Thomas WG (December 2005). "The angiotensin II type 2 receptor causes constitutive growth of cardiomyocytes and does not antagonize angiotensin II type 1 receptor-mediated hypertrophy". Hypertension 46 (6): 1347–54. doi:10.1161/01.HYP.0000193504.51489.cf. PMID 16286564.
- ^ Albiston AL, Mustafa T, McDowall SG, Mendelsohn FA, Lee J, Chai SY (March 2003). "AT4 receptor is insulin-regulated membrane aminopeptidase: potential mechanisms of memory enhancement". Trends Endocrinol. Metab. 14 (2): 72–7. doi:10.1016/S1043-2760(02)00037-1. PMID 12591177.
- ^ Chai SY, Fernando R, Peck G, Ye SY, Mendelsohn FA, Jenkins TA, Albiston AL (November 2004). "The angiotensin IV/AT4 receptor". Cell. Mol. Life Sci. 61 (21): 2728–37. doi:10.1007/s00018-004-4246-1. PMID 15549174.
- ^ Davis CJ, Kramár EA, De A, Meighan PC, Simasko SM, Wright JW, Harding JW (2006). "AT4 receptor activation increases intracellular calcium influx and induces a non-N-methyl-D-aspartate dependent form of long-term potentiation". Neuroscience 137 (4): 1369–79. doi:10.1016/j.neuroscience.2005.10.051. PMID 16343778.
- ^ Vanderheyden PM (April 2009). "From angiotensin IV binding site to AT4 receptor". Mol. Cell. Endocrinol. 302 (2): 159–66. doi:10.1016/j.mce.2008.11.015. PMID 19071192.
- ^ Beyer CE, Dwyer JM, Platt BJ, Neal S, Luo B, Ling HP, Lin Q, Mark RJ, Rosenzweig-Lipson S, Schechter LE (May 2010). "Angiotensin IV elevates oxytocin levels in the rat amygdala and produces anxiolytic-like activity through subsequent oxytocin receptor activation". Psychopharmacology (Berl.) 209 (4): 303–11. doi:10.1007/s00213-010-1791-1. PMID 20224888.
- ^ Andersson H (2010). Design and Synthesis of Angiotensin IV Peptidomimetics Targeting the Insulin-Regulated Aminopeptidase (IRAP) (Ph.D. thesis). Uppsala Universitet. http://kth.diva-portal.org/smash/get/diva2:309698/FULLTEXT01. Retrieved 2012-01-08.
- ^ Wright JW, Harding JW (September 2011). "Brain renin-angiotensin—a new look at an old system". Prog. Neurobiol. 95 (1): 49–67. doi:10.1016/j.pneurobio.2011.07.001. PMID 21777652.
- ^ Benoist CC, Wright JW, Zhu M, Appleyard SM, Wayman GA, Harding JW (October 2011). "Facilitation of hippocampal synaptogenesis and spatial memory by C-terminal truncated Nle1-angiotensin IV analogs". J. Pharmacol. Exp. Ther. 339 (1): 35–44. doi:10.1124/jpet.111.182220. PMC 3186286. PMID 21719467. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=3186286.
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