Endotelin

Endotelin 1
Endotelin 1
Identifikatori
Simbol	EDN1
NCBI gen	1906
HGNC	3176
OMIM	131240
RefSeq	NM_001955
UniProt	P05305
Ostali podaci
Lokus	Hrom. 6 p23-p24
Strukture
Pretraga za
Strukture	Swiss-model
Domene	InterPro

Dostupne proteinske strukture:
Pfam	strukture / ECOD
PDB	RCSB PDB; PDBe; PDBj
PDBsum	sažetak strukture

Porodica endotelina
Porodica endotelina
Identifikatori
Simbol	EDN
Pfam	PF00322
InterPro	IPR001928
PROSITE	PDOC00243
SCOP2	1edp / SCOPe / SUPFAM
OPM superporodica	147
OPM protein	3cmh
Pfam
Dostupne proteinske strukture:
Pfam	strukture / ECOD
PDB	RCSB PDB; PDBe; PDBj
PDBsum	sažetak strukture

Endotelini su peptidi sa receptorskim i drugim efektima na mnoge tjelesne organe.^[1]^[2]^[3] Endotelin sužava krvne sudove i podiže krvni pritisak. Endotelini se normalno održavaju u ravnoteži drugim mehanizmima, ali kada prekomjerno eksprimiraju, doprinose visokom krvnom pritisku (hipertenzija, srčanim i potencijalno drugim bolestima).^[1]^[4]

Endotelin 2

Identifikatori

Simbol

Ostali podaci

Hrom. 1 p34

Pretraga za
Strukture	Swiss-model
Domene	InterPro

Endotelin 3
Identifikatori
Simbol	EDN3
HGNC	3178
RefSeq	NM_000114
Ostali podaci
Lokus	Hrom. 20 q13.2-q13.3

Endotelini su 21-aminokiselinaki vazokonstrikcijski peptidi proizvedeni prvenstveno u endotelu, koji imaju ključnu ulogu u vaskularnoj homeostazi. Endotelini su uključeni u vaskularne bolesti nekoliko organskih sistema, uključujući srce, pluća, bubrege i mozak.^[5]^[6] Od 2018., endotelini ostaju pod opsežnim osnovnim i kliničkim istraživanjem, kako bi se definirala njihova uloga u nekoliko organskih sistema.^[1]^[7]^[8]^[9]

Izoforme i distribucija

Poznate su tri izoforme (ET-1, -2, -3), sa različitim regionima ispoljavanja, i dva ključna tipa receptora, ET_A i ET_B.

ET_A receptori su nađeni u glatkim mišićnim tkivima krvnih sudova. Vezanje endotelina za ET_A uvećava vazokonstrikciju i zadržavanja natrija, što podiže krvni pritisak.^[10]
ET_B je poglavito lociran na endotelnim ćelijama koje pokrivaju unutrašnjost krvnih sudova. Kad se veže za receptore ET_B, dolazi do oslobađanja dušik-oksida (endotelni faktor relaksacije), natriureze i diureze i mehanizama koji obaraju krvni pritisak.
U nervnom sistemu nađena sum oba tipa ET receptora, gdje posreduju u neurotransmisiji i vaskularnim funkcijama.^[11]

Mozak i nervi

Receptori za endotelin su različitoo ispoljeni u tijelu. Oni su prisutni u krvnim sudovima i ćelijama mozga, horoidnom pleksusu i perifernim nervima. Kada je ubrizgan direktno na mozak pacova u pikomolarnim količinama kao modelni organizam endotelin-1 uzrokuje snažnu metaboličku stimulaciju moždanog udara i epileptičke napade sa znatnim sniženjem dotoka krvi do pogođenih moždanih područja. Oba efekta su posredovana kalcijskim kanalima.^[12]

Reference

^ ^a ^b ^c Davenport AP, Hyndman KA, Dhaun N, Southan C, Kohan DE, Pollock JS, et al. (april 2016). "Endothelin". Pharmacological Reviews. 68 (2): 357–418. doi:10.1124/pr.115.011833. PMC 4815360. PMID 26956245.
^ Kawanabe Y, Nauli SM (januar 2011). "Endothelin". Cellular and Molecular Life Sciences. 68 (2): 195–203. doi:10.1007/s00018-010-0518-0. PMC 3141212. PMID 20848158.
^ Kedzierski RM, Yanagisawa M (2001). "Endothelin system: the double-edged sword in health and disease". Annual Review of Pharmacology and Toxicology. 41: 851–76. doi:10.1146/annurev.pharmtox.41.1.851. PMID 11264479.
^ Maguire JJ, Davenport AP (decembar 2014). "Endothelin@25 - new agonists, antagonists, inhibitors and emerging research frontiers: IUPHAR Review 12". British Journal of Pharmacology. 171 (24): 5555–72. doi:10.1111/bph.12874. PMC 4290702. PMID 25131455.
^ Agapitov AV, Haynes WG (mart 2002). "Role of endothelin in cardiovascular disease". Journal of the Renin-Angiotensin-Aldosterone System. 3 (1): 1–15. doi:10.3317/jraas.2002.001. PMID 11984741.
^ Schinelli S (2006). "Pharmacology and physiopathology of the brain endothelin system: an overview". Current Medicinal Chemistry. 13 (6): 627–38. doi:10.2174/092986706776055652. PMID 16529555.
^ Kuang HY, Wu YH, Yi QJ, Tian J, Wu C, Shou WN, Lu TW (mart 2018). "The efficiency of endothelin receptor antagonist bosentan for pulmonary arterial hypertension associated with congenital heart disease: A systematic review and meta-analysis". Medicine. 97 (10): e0075. doi:10.1097/MD.0000000000010075. PMC 5882424. PMID 29517668.
^ Iljazi A, Ayata C, Ashina M, Hougaard A (mart 2018). "The Role of Endothelin in the Pathophysiology of Migraine-a Systematic Review". Current Pain and Headache Reports. 22 (4): 27. doi:10.1007/s11916-018-0682-8. PMID 29557064.
^ Lu YP, Hasan AA, Zeng S, Hocher B (2017). "Plasma ET-1 Concentrations Are Elevated in Pregnant Women with Hypertension -Meta-Analysis of Clinical Studies". Kidney & Blood Pressure Research. 42 (4): 654–663. doi:10.1159/000482004. PMID 29212079.
^ Hynynen MM, Khalil RA (2006). "The vascular endothelin system in hypertension--recent patents and discoveries". Recent Pat Cardiovasc Drug Discov. 1 (1): 95–108. doi:10.2174/157489006775244263. PMC 1351106. PMID 17200683.
^ Barnes K, Turner AJ (1997). "The endothelin system and endothelin-converting enzyme in the brain: molecular and cellular studies". Neurochem. Res. 22 (8): 1033–40. doi:10.1023/A:1022435111928. PMID 9239759. Nepoznati parametar |month= zanemaren (pomoć)
^ Gross PM, Zochodne DW, Wainman DS, Ho LT, Espinosa FJ, Weaver DF (1992). "Intraventricular endothelin-1 uncouples the blood flow: metabolism relationship in periventricular structures of the rat brain: involvement of L-type calcium channels". Neuropeptides. 22 (3): 155–65. doi:10.1016/0143-4179(92)90158-S. PMID 1331845. Nepoznati parametar |month= zanemaren (pomoć)CS1 održavanje: više imena: authors list (link)

Vanjski linkovi

Endothelins na US National Library of Medicine Medical Subject Headings (MeSH)

Šablon:Peptidergici

[pr-1] Davenport AP, Hyndman KA, Dhaun N, Southan C, Kohan DE, Pollock JS, et al. (april 2016). "Endothelin". Pharmacological Reviews. 68 (2): 357–418. doi:10.1124/pr.115.011833. PMC 4815360. PMID 26956245.

[cmls-2] Kawanabe Y, Nauli SM (januar 2011). "Endothelin". Cellular and Molecular Life Sciences. 68 (2): 195–203. doi:10.1007/s00018-010-0518-0. PMC 3141212. PMID 20848158.

[arpt-3] Kedzierski RM, Yanagisawa M (2001). "Endothelin system: the double-edged sword in health and disease". Annual Review of Pharmacology and Toxicology. 41: 851–76. doi:10.1146/annurev.pharmtox.41.1.851. PMID 11264479.

[4] Maguire JJ, Davenport AP (decembar 2014). "Endothelin@25 - new agonists, antagonists, inhibitors and emerging research frontiers: IUPHAR Review 12". British Journal of Pharmacology. 171 (24): 5555–72. doi:10.1111/bph.12874. PMC 4290702. PMID 25131455.

[pmid11984741-5] Agapitov AV, Haynes WG (mart 2002). "Role of endothelin in cardiovascular disease". Journal of the Renin-Angiotensin-Aldosterone System. 3 (1): 1–15. doi:10.3317/jraas.2002.001. PMID 11984741.

[pmid16529555-6] Schinelli S (2006). "Pharmacology and physiopathology of the brain endothelin system: an overview". Current Medicinal Chemistry. 13 (6): 627–38. doi:10.2174/092986706776055652. PMID 16529555.

[7] Kuang HY, Wu YH, Yi QJ, Tian J, Wu C, Shou WN, Lu TW (mart 2018). "The efficiency of endothelin receptor antagonist bosentan for pulmonary arterial hypertension associated with congenital heart disease: A systematic review and meta-analysis". Medicine. 97 (10): e0075. doi:10.1097/MD.0000000000010075. PMC 5882424. PMID 29517668.

[8] Iljazi A, Ayata C, Ashina M, Hougaard A (mart 2018). "The Role of Endothelin in the Pathophysiology of Migraine-a Systematic Review". Current Pain and Headache Reports. 22 (4): 27. doi:10.1007/s11916-018-0682-8. PMID 29557064.

[9] Lu YP, Hasan AA, Zeng S, Hocher B (2017). "Plasma ET-1 Concentrations Are Elevated in Pregnant Women with Hypertension -Meta-Analysis of Clinical Studies". Kidney & Blood Pressure Research. 42 (4): 654–663. doi:10.1159/000482004. PMID 29212079.

[pmid17200683-10] Hynynen MM, Khalil RA (2006). "The vascular endothelin system in hypertension--recent patents and discoveries". Recent Pat Cardiovasc Drug Discov. 1 (1): 95–108. doi:10.2174/157489006775244263. PMC 1351106. PMID 17200683.

[pmid9239759-11] Barnes K, Turner AJ (1997). "The endothelin system and endothelin-converting enzyme in the brain: molecular and cellular studies". Neurochem. Res. 22 (8): 1033–40. doi:10.1023/A:1022435111928. PMID 9239759. Nepoznati parametar |month= zanemaren (pomoć)

[pmid1331845-12] Gross PM, Zochodne DW, Wainman DS, Ho LT, Espinosa FJ, Weaver DF (1992). "Intraventricular endothelin-1 uncouples the blood flow: metabolism relationship in periventricular structures of the rat brain: involvement of L-type calcium channels". Neuropeptides. 22 (3): 155–65. doi:10.1016/0143-4179(92)90158-S. PMID 1331845. Nepoznati parametar |month= zanemaren (pomoć)CS1 održavanje: više imena: authors list (link)

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