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貨期:
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用途:
For Research Use Only. Not for use in diagnostic or therapeutic procedures.
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one molecule of endogenous dicarboxylic acid (glutarate, ketoglutarate, etc). Mediates the sodium-independent uptake of 2,3-dimercapto-1-propanesulfonic acid (DMPS). Mediates the sodium-independent uptake of p-aminohippurate (PAH), ochratoxin (OTA), acyclovir (ACV), 3'-azido-3-'deoxythymidine (AZT), cimetidine (CMD), 2,4-dichloro-phenoxyacetate (2,4-D), hippurate (HA), indoleacetate (IA), indoxyl sulfate (IS) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF), cidofovir, adefovir, 9-(2-phosphonylmethoxyethyl) guanine (PMEG), 9-(2-phosphonylmethoxyethyl) diaminopurine (PMEDAP) and edaravone sulfate. PAH uptake is inhibited by p-chloromercuribenzenesulphonate (PCMBS), diethyl pyrocarbonate (DEPC), sulindac, diclofenac, carprofen, glutarate and okadaic acid. PAH uptake is inhibited by benzothiazolylcysteine (BTC), S-chlorotrifluoroethylcysteine (CTFC), cysteine S-conjugates S-dichlorovinylcysteine (DCVC), furosemide, steviol, phorbol 12-myristate 13-acetate (PMA), calcium ionophore A23187, benzylpenicillin, furosemide, indomethacin, bumetamide, losartan, probenecid, phenol red, urate, and alpha-ketoglutarate.
基因功能參考文獻:
is richly expressed in the kidney, where it plays critical roles in the secretion, from the blood to urine, of clinically important drugs. PMID: 29422382
Our findings suggest that because OAT1 is capable of transporting d-luc, it can also be used to improve visualization and monitoring of luciferase-expressing cells. PMID: 29273507
SLC22A6 variants were not significantly associated with hyperuricemia and gout in a New Zealand Maori and Pacific cohort. PMID: 28371506
this is the first demonstration that Nedd4-1 regulates hOAT1 ubiquitination, expression, and transport activity through its WW2 and WW3 domains PMID: 27226107
both Nedd4-1 and Nedd4-2 are important regulators for hOAT1 ubiquitination, expression, and function PMID: 26823285
Uremic toxins, p-cresyl sulfate and indoxyl sulfate, are transported into endothelial cells by OAT1/OAT3. PMID: 28472795
high capacity p-cresyl sulfate trasnporter PMID: 24185403
OAT1 and NaDC3 in the basolateral membrane and OAT4 in the luminal membrane of proximal tubule cells are responsible for the avid renal secretion of N-carbamoylglutamate. PMID: 25354943
BCL6 constitutes a promising candidate gene for the regulation of human OAT1 transcription PMID: 25234312
Clopidogrel/clopidogrel carboxylate are weak inhibitors of OAT1. PMID: 24530383
The results confirmed that OAT1, OAT3, OCT2, MATE1, and MATE2-K were coexpressed in tubular epithelial cells. PMID: 23630107
transport of xanthurenic acid by OAT1 and OAT3 PMID: 23832370
PKC isoform PKCalpha was responsible for OAT1 ubiquitination. PMID: 23640180
It was shown that human OAT3 and OAT1 cannot be involved in the renal extraction of glutathione from blood, but OAT1 could support intracellular glutathione synthesis by taking up cysteinyl glycine. PMID: 23255614
Both hOAT1 and hOAT3 markedly stimulated the uptake of kynurenic acid into oocytes. PMID: 22108572
High urine OAT1 and OAT3 and low OAT4 is associated with early reversible proximal tubular damage. PMID: 21945944
The data reveal alpha-ketoglutarate as a common high-affinity substrate of NaDC3, OAT1, and OAT3 PMID: 21865262
Intergenic polymorphism rs10792367 between OAT1 and OAT3 is not associated with hypertension, but appears to be involved in between-individual variations in antihypertensive responses to hydrochlorothiazide. PMID: 21164499
Our results are the first to highlight the central role of TM 12 in maintaining the stability and in promoting the maturation efficiency of hOAT1. PMID: 19892921
results suggest that genetic polymorphisms may not be a significant contributing factor to variations in the hOAT2 expression or hOAT2 transport activity PMID: 19854166
elucidation of the molecular mechanism for renal tetracycline transport by human organic anion transporters (hOATs) using proximal tubular cells stably expressing hOATs PMID: 11855680
cimetidine was found to be substrate for fROAT/hOAT1; organic anion transporters likely contribute to cimetidine excretion in proximal tubules PMID: 12429554
hOAT1 transports urate,and is not responsible for familial juvenile gouty nephropathy in the two sisters examined in this study. PMID: 12472777
PKC-induced hOAT1 downregulation is achieved through carrier retrieval from the cell membrane and does not involve phosphorylation of the predicted classic hOAT1 PKC consensus sites PMID: 12874449
stimulation of basolateral organic anion uptake by EGF or PGE2 is a widespread (if not general) regulatory mechanism, and the signal transduction pathway involved seems to be general PMID: 14644751
glycosylation has a role in the targeting of OAT1 onto the plasma membrane PMID: 14749323
The level of human OAT1 mRNA is significantly lower in the kidney of patients with renal diseases than in the normal controls. PMID: 14984259
...provide evidence for a general expression of the recently identified splice-variants of hOTA1...Their expression is restricted to the kidney cortex. p. 430 PMID: 15039295
Leu-30 and Thr-36 in transmembrane domain 1 are critical determinants of hOAT1 function PMID: 15145940
Organic anion transporter(s) likely play prominent role in basolateral transport of mercuric ions by proximal tubular cells and in nephropathy induced by Hg(2+). PMID: 15200431
mercuric conjugates of Hcy are potential transportable substrates of OAT1. PMID: 15284288
the coding region of OAT1 has low genetic and functional diversity and its variants may not contribute substantially to interindividual differences in renal elimination of xenobiotics PMID: 15864112
hOAT1 has been suggested as the basis of nephrotoxicity induced by nucleoside phosphonate analogs PMID: 15914676
hOAT1 exists in the plasma membrane as a homooligomer, possibly trimer, and higher order of oligomer PMID: 16046403
The clustering of OAT genes in the genome raises the possibility that nucleotide polymorphisms in SLC22A6 could also effect SLC22A8 expression, and vice versa. PMID: 16648942
the C terminus of hOAT1 has a central role in its function PMID: 16920720
identified two new residues, Tyr(230) and Phe(438), which are important for substrate/protein interactions PMID: 17038320
this paper reports the first characterization of the human OAT1 promoter and the first gene in the kidney whose promoter activity is regulated by HNF-4alpha PMID: 17344191
it is concluded that Arg(466) influences the binding of glutarate, but not interaction with p-aminohippurate, and interacts with chloride, which is a major determinant in substrate translocation PMID: 17353191
Both hOAT1 and hOAT3 are responsible for the basolateral uptake of edaravone sulfate in the kidney. PMID: 17502342
hOAT1 did not mediate rosuvastatin uptake PMID: 17585018
The data provide a model for the concerted action of OAT1 mediating basolateral secretion of glutarate derivatives from proximal tubule cells PMID: 18365245
OAT1 undergoes constitutive and protein kinase C-regulated trafficking through a dynamin- and clathrin-dependent pathway PMID: 18818201
The renal expression of OAT1 and OAT3 should be taken into account in order to improve pharmacotherapeutic efficacy and to prevent drug toxicity during the onset of this hepatic disease. PMID: 19034961
Gaboxadol could be taken up into the kidney by hOAT1 followed by glucuronidation and efflux of the conjugate into urine via MRP4. PMID: 19082692
ANG II inhibited hOAT1 activity through activation of PKCalpha, which led to the redistribution of the transporter from the cell surface to the intracellular compartments. PMID: 19088254
OAT1 appears to be one of the major contributors to renal basolateral uptake of citrulline, and impaired activities of these transporters may contribute substantially to the increase in plasma citrulline in renal failure. PMID: 19403644
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亞細胞定位:
Cell membrane; Multi-pass membrane protein.
蛋白家族:
Major facilitator (TC 2.A.1) superfamily, Organic cation transporter (TC 2.A.1.19) family
組織特異性:
Strongly expressed in kidney and to a lower extent in liver, skeletal muscle, brain and placenta. Found at the basolateral membrane of the proximal tubule.