Therapeutic Targets Database
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TTD Target ID: TTDS00116

Target Information
NameSolute carrier family 12 member 1    
Type of targetSuccessful target    
SynonymsBumetanide-sensitive sodium-(potassium)-chloride cotransporter 2    
Bumetanide-sensitive sodium-(potassium)Solute carrier family 12 member 1-chloride cotransporter 2    
Kidney-specific Na-K-Cl symporter    
NKCC2    
Na+/K+/2CL- co-transporter    
Solute carrier family 12 member    
DiseaseCongestive heart failure
[ICD9: 428.0   ICD10: I50]
[1]
Hypertension
[ICD9: 401   ICD10: I10, I11, I12, I13, I15]
[2]
Drug(s)BendroflumethiazideApprovedHigh blood pressure[3]
BumetanideApprovedEdema associated with congestive heart failure[4][5]
ChlorthalidoneApprovedHypertension[6]
Ethacrynic acidApprovedHigh blood pressure[7][8]
FurosemideApprovedEdema associated with congestive heart failure[9]
HydroflumethiazideApprovedEdema associated with congestive heart failure[3]
MethyclothiazideApprovedHypertension[3]
Potassium ChlorideApprovedHypokalemia[3]
TorasemideApprovedEdema associated with congestive heart failure[10][11][12]
TrichlormethiazideApprovedOedema and hypertension[13]
BioChemical ClassIon transport    
UniProt IDQ13621
FunctionElectrically silent transporter system. mediates sodium and chloride reabsorption. plays a vital role in the regulation of ionic balance and cell volume.    
SequenceMSLNNSSNVFLDSVPSNTNRFQVSVINENHESSAAADDNTDPPHYEETSFGDEAQKRLRI SFRPGNQECYDNFLQSGETAKTDASFHAYDSHTNTYYLQTFGHNTMDAVPKIEYYRNTGS ISGPKVNRPSLLEIHEQLAKNVAVTPSSADRVANGDGIPGDEQAENKEDDQAGVVKFGWV KGVLVRCMLNIWGVMLFIRLSWIVGEAGIGLGVLIILLSTMVTSITGLSTSAIATNGFVR GGGAYYLISRSLGPEFGGSIGLIFAFANAVAVAMYVVGFAETVVDLLKESDSMMVDPTND IRIIGSITVVILLGISVAGMEWEAKAQVILLVILLIAIANFFIGTVIPSNNEKKSRGFFN YQASIFAENFGPRFTKGEGFFSVFAIFFPAATGILAGANISGDLEDPQDAIPRGTMLAIF ITTVAYLGVAICVGACVVRDATGNMNDTIISGMNCNGSAACGLGYDFSRCRHEPCQYGLM NNFQVMSMVSGFGPLITAGIFSATLSSALASLVSAPKVFQALCKDNIYKALQFFAKGYGK NNEPLRGYILTFLIAMAFILIAELNTIAPIISNFFLASYALINFSCFHASYAKSPGWRPA YGIYNMWVSLFGAVLCCAVMFVINWWAAVITYVIEFFLYVYVTCKKPDVNWGSSTQALSY VSALDNALELTTVEDHVKNFRPQCIVLTGGPMTRPALLDITHAFTKNSGLCICCEVFVGP RKLCVKEMNSGMAKKQAWLIKNKIKAFYAAVAADCFRDGVRSLLQASGLGRMKPNTLVIG YKKNWRKAPLTEIENYVGIIHDAFDFEIGVVIVRISQGFDISQVLQVQEELERLEQERLA LEATIKDNECEEESGGIRGLFKKAGKLNITKTTPKKDGSINTSQSMHVGEFNQKLVEAST QFKKKQEKGTIDVWWLFDDGGLTLLIPYILTLRKKWKDCKLRIYVGGKINRIEEEKIVMA SLLSKFRIKFADIHIIGDINIRPNKESWKVFEEMIEPYRLHESCKDLTTAEKLKRETPWK ITDAELEAVKEKSYRQVRLNELLQEHSRAANLIVLSLPVARKGSISDLLYMAWLEILTKN LPPVLLVRGNHKNVLTFYS
Target ValidationClick to Find Target Validation Information.    
BlockerBendroflumethiazide[3]
Bumetanide[4][5]
Chlorthalidone[6]
Ethacrynic acid[7][8]
Furosemide[9]
Hydroflumethiazide[3]
Methyclothiazide[3]
Piretanide[14][15][1]
Piretanide[16]
Torasemide[10][11][12]
Trichlormethiazide[13]
BinderPotassium Chloride[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Piretanide, a potent diuretic with potassium-sparing properties, for the treatment of congestive heart failure. Clin Pharmacol Ther. 1986 Nov;40(5):587-94. To Reference
Ref 2NKCC2: a drug target in hypertension. J Hypertens. 2002 Apr;20(4):605-6. To Reference
Ref 3DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6. Epub 2007 Nov 29. To Reference
Ref 4Nerve Terminal GABAA Receptors Activate Ca2+/Calmodulin-dependent Signaling to Inhibit Voltage-gated Ca2+ Influx and Glutamate Release. J Biol Chem. 2009 Mar 27;284(13):8726-37. Epub 2009 Jan 13. To Reference
Ref 5Effect of L-ascorbate on chloride transport in freshly excised sinonasal epithelia. Am J Rhinol Allergy. 2009 May-Jun;23(3):294-9. To Reference
Ref 6The 45-year story of the development of an anti-aldosterone more specific than spironolactone. Mol Cell Endocrinol. 2004 Mar 31;217(1-2):45-52. To Reference
Ref 7Na-K-Cl cotransport regulates intracellular volume and monolayer permeability of trabecular meshwork cells. Am J Physiol. 1995 Apr;268(4 Pt 1):C1067-74. To Reference
Ref 8Inhibition of Na-K-2Cl cotransport and bumetanide binding by ethacrynic acid, its analogues, and adducts. Am J Physiol. 1993 May;264(5 Pt 1):C1270-7. To Reference
Ref 9Update of diuretics in the treatment of hypertension. Am J Ther. 2007 Mar-Apr;14(2):154-60. To Reference
Ref 10Genetic variation in the renal sodium transporters NKCC2, NCC, and ENaC in relation to the effects of loop diuretic drugs. Clin Pharmacol Ther. 2007 Sep;82(3):300-9. Epub 2007 Apr 25. To Reference
Ref 11Effects of loop diuretics on angiotensin II-stimulated vascular smooth muscle cell growth. Nephrol Dial Transplant. 2001;16 Suppl 1:14-7. To Reference
Ref 12Hypertension. 1999 Jul;34(1):138-43.Torasemide inhibits angiotensin II-induced vasoconstriction and intracellular calcium increase in the aorta of spontaneously hypertensive rats. To Reference
Ref 13Function and regulation of epithelial sodium transporters in the kidney of a salt-sensitive hypertensive rat model. J Hypertens. 2007 May;25(5):1065-72. To Reference
Ref 14Peripheral and central antinociceptive action of Na+-K+-2Cl- cotransporter blockers on formalin-induced nociception in rats. Pain. 2005 Mar;114(1-2):231-8. Epub 2005 Jan 26. To Reference
Ref 15Rat NKCC2/NKCC1 cotransporter selectivity for loop diuretic drugs. Naunyn Schmiedebergs Arch Pharmacol. 2002 Mar;365(3):193-9. Epub 2002 Feb 1. To Reference
Ref 16Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. To Reference



 

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