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- SUR
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WordNet
- antidiabetic consisting of any of several drugs that reduce the level of glucose in the blood; used to treat diabetes mellitus
- a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
PrepTutorEJDIC
- =sense organ / 受信装置
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/05/06 02:06:55」(JST)
[Wiki en表示]
| ATP-binding cassette, sub-family C (CFTR/MRP), member 8 |
| Identifiers |
| Symbol |
ABCC8 |
| Alt. symbols |
SUR1 |
| Entrez |
6833 |
| HUGO |
59 |
| OMIM |
600509 |
| RefSeq |
NM_000352 |
| UniProt |
Q09428 |
| Other data |
| Locus |
Chr. 11 p15.1 |
| ATP-binding cassette, sub-family C (CFTR/MRP), member 9 |
| Identifiers |
| Symbol |
ABCC9 |
| Alt. symbols |
SUR2A, SUR2B |
| Entrez |
10060 |
| HUGO |
60 |
| OMIM |
601439 |
| RefSeq |
NM_005691 |
| UniProt |
O60706 |
| Other data |
| Locus |
Chr. 12 p12.1 |
In the field of molecular biology, the sulfonylurea receptors (SUR) are membrane proteins which are the molecular targets of the sulfonylurea class of antidiabetic drugs whose mechanism of action is to promote insulin release from pancreatic beta cells. More specifically, SUR proteins are subunits of the inward-rectifier potassium ion channels Kir6.x (6.1 and 6.2).[1] The association of four Kir6.x and four SUR subunits form an ion conducting channel commonly referred to as the KATP channel.[2]
There are three forms of the sulfonylurea receptor, SUR1 encoded by the ABCC8 gene and SUR2A and SUR2B which are splice variants arising from a single ABCC9 gene.[3]
Contents
- 1 Function
- 2 Tissue distribution
- 3 Disease linkage
- 4 References
Function
The primary function of the sulfonylurea receptor is to sense intracellular levels of the nucleotides ATP and ADP and in response facilitate the open or closing its associated Kir6.x potassium channel. Hence the KATP channel monitors the energy balance within the cell.[4]
Depending on the tissue in which the KATP channel is expressed, altering the membrane potential can trigger a variety of down stream events. For example, in pancreatic beta cells, high levels of glucose lead to increased production of ATP which in turn binds to the KATP channel resulting in channel closure. The increase in membrane potential in turn opens voltage-dependent calcium channels increasing intracellular calcium concentrations which triggers exocytosis of insulin.
Under cerebral ischemic conditions SUR1, the regulatory subunit of the KATP- and the NCCa-ATP-channels, is expressed in neurons, astrocytes, oligodendrocytes, endothelial cells[5] and by reactive microglia.[6] Blockade of SUR1 receptors with glibenclamide has been involved in improved outcome in animal stroke models and investigational human studies by preventing brain swelling [7] and enhancing neuroprotection.[6]
Tissue distribution
The isoforms of the sulfonylurea receptor have the following tissue distribution:
- adipose tissue - SUR2B/Kir6.1
- pancreatic beta cells - SUR1/Kir6.2
- cardiac myocytes - SUR2A
- skeletal muscle - SUR2A
- smooth muscle - SUR2B
- brain - SUR1, SUR2A and SUR2B [5][6]
Disease linkage
The SUR1 protein is coded by the ABCC8 gene and is associated with congenital hyperinsulinism[8] and susceptibility to type 2 diabetes.[9]
References
- ^ Campbell, J. D.; Sansom, M. S.; Ashcroft, F. M. (2003). "Potassium channel regulation". EMBO Reports 4 (11): 1038–42. doi:10.1038/sj.embor.embor7400003. PMC 1326373. PMID 14593442.
- ^ sulfonylurea receptor at the US National Library of Medicine Medical Subject Headings (MeSH)
- ^ Aguilar-Bryan L, Clement JP 4th, Gonzalez G, Kunjilwar K, Babenko A, Bryan J (1 January 1998). "Toward understanding the assembly and structure of KATP channels". Physiol Rev 78 (1): 227–45. PMID 9457174.
- ^ Nichols, C. G. (2006). "KATP channels as molecular sensors of cellular metabolism". Nature 440 (7083): 470–6. doi:10.1038/nature04711. PMID 16554807.
- ^ a b Simard JM, Woo SK, Schwartzbauer GT, Gerzanich V (June 2012). "Sulfonylurea receptor 1 in central nervous system injury: A focused review". J Cereb Blood Flow Metab 32 (9): 1699–1717. doi:10.1038/jcbfm.2012.91. PMC 3434627. PMID 22714048.
- ^ a b c Ortega, F. J.; Gimeno-Bayon, J; Espinosa-Parrilla, J. F.; Carrasco, J. L.; Batlle, M; Pugliese, M; Mahy, N; Rodríguez, M. J. (2012). "ATP-dependent potassium channel blockade strengthens microglial neuroprotection after hypoxia-ischemia in rats". Experimental Neurology 235 (1): 282–96. doi:10.1016/j.expneurol.2012.02.010. PMID 22387180.
- ^ Simard, J. M.; Chen, M; Tarasov, K. V.; Bhatta, S; Ivanova, S; Melnitchenko, L; Tsymbalyuk, N; West, G. A.; Gerzanich, V (2006). "Newly expressed SUR1-regulated NC(Ca-ATP) channel mediates cerebral edema after ischemic stroke". Nature Medicine 12 (4): 433–40. doi:10.1038/nm1390. PMC 2740734. PMID 16550187.
- ^ Fournet, J. C.; Junien, C (2004). "Genetics of congenital hyperinsulinism". Endocrine pathology 15 (3): 233–40. PMID 15640549.
- ^ Reis, A. F.; Velho, G (2002). "Sulfonylurea receptor -1 (SUR1): Genetic and metabolic evidences for a role in the susceptibility to type 2 diabetes mellitus". Diabetes & metabolism 28 (1): 14–9. PMID 11938023.
|
Membrane proteins, carrier proteins: membrane transport proteins ABC-transporter (TC 3A1)
|
|
| A |
- A1
- A2
- A3
- A4
- A7
- A8
- A12
- A13
|
|
| B |
- B1
- B2-3 (B2
- B3)
- B4
- B5
- B6
- B7
- B9
- B11
|
|
| C |
- C1
- C2
- C3
- C4
- C5
- C6
- C7
- C8-9 (C8, C9)
- C10
- C11
- C13
|
|
| D |
|
|
| E |
|
|
| F |
|
|
| G |
- G1
- G2
- G4
- Sterolin (G5, G8)
|
|
|
see also ABC transporter disorders
|
|
UpToDate Contents
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English Journal
- ABCC8 Polymorphisms Are Associated with Triglyceride Concentration in Type 2 Diabetics on Sulfonylurea Therapy.
- Nikolac N, Simundic AM, Saracevic A, Katalinic D.Source1 University Department of Chemistry, Medical School University Hospital Sestre Milosrdnice , Zagreb, Croatia .
- Genetic testing and molecular biomarkers.Genet Test Mol Biomarkers.2012 Apr 25. [Epub ahead of print]
- Background: The failure of therapy with oral hypoglycemic drugs leads to not only poorly regulated glycemic status, but also dyslipidemia and increased body weight and body mass index (BMI). Sulfonylureas act as insulin secretagogues by binding to the sulfonylurea receptor (SUR-1) encoded by the gen
- PMID 22533711
- Sulfonylurea receptor as a target for molecular imaging of pancreas beta cells with (99m)Tc-DTPA-glipizide.
- Oh CS, Kohanim S, Kong FL, Song HC, Huynh N, Mendez R, Chanda M, Edmund Kim E, Yang DJ.SourceDivision of Diagnostic Imaging, The University of Texas M.D. Anderson Cancer Center, 1515 Holcombe Blvd., Unit 59, Houston, TX, 77030, USA.
- Annals of nuclear medicine.Ann Nucl Med.2012 Apr;26(3):253-61. Epub 2012 Jan 13.
- OBJECTIVE: This study was aimed to assess pancreas beta cell activity using (99m)Tc-diethyleneaminepentaacetic acid-glipizide (DTPA-GLP), a sulfonylurea receptor agent. The effect of DTPA-GLP on the blood glucose level in rats was also evaluated.METHODS: DTPA dianhydride was conjugated with GLP in t
- PMID 22237676
Japanese Journal
- ATP-Binding Cassette Proteins Involved in Glucose and Lipid Homeostasis
- MATSUO Michinori
- Bioscience, biotechnology, and biochemistry 74(5), 899-907, 2010-05-23
- … Sulfonylurea receptor (SUR) is a subunit of the ATP-sensitive potassium channels, which regulate insulin secretion from pancreatic β-cells by sensing cellular metabolic levels. …
- NAID 10027554433
- Effects of Metformin on Rosiglitazone-Induced Cardiac Hypertrophy in Mice
- Lee Hsiu-Hao,Yeh Ching-Hua,Chen Yu-Tai,Chi Tzong-Cherng,Cheng Juei-Tang,Lo Shih-Hsiang
- Biological & Pharmaceutical Bulletin 33(9), 1506-1510, 2010
- … Reverse transcription-polymerase chain reaction (RT-PCR) and Western blot were applied to evaluate expression of sulfonylurea receptor 2A (SUR2A) and Kir 6.2. … The activities of peroxisome proliferator activated receptor α (PPARα) in the myocardium were also observed. …
- NAID 130000322347
★リンクテーブル★
[★]
- 英
- sulfonylurea receptor SUR
- 関
- SU受容体
[★]
- 同
- sulfonylurea receptor
[★]
スルホニル尿素、スルホニルウレア、スルホニル尿素系薬剤、スルホニル尿素薬、スルホニル尿素剤、((俗))SU薬
- ATP感受性K+チャネル阻害によりインスリンを分泌させる抗糖尿病薬