Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00212

Target Information
NameCarbonic anhydrase XII    
Type of targetResearch target    
SynonymsCA-XII    
Carbonate dehydratase XII    
Tumor antigen HOM-RCC-3.1.3    
DiseaseColorectal cancer
[ICD9: 153, 154   ICD10: C18-C21]
[1]
Gastrointestinal cancers
[ICD9: 150-159   ICD10: C15-C26]
[1]
Pancreatic cancer
[ICD9: 157   ICD10: C25]
[1]
Renal failure
[ICD9: 584, 585   ICD10: N17, N18, N19]
[2]
BioChemical ClassCarbon-oxygen lyases    
EC NumberEC 4.2.1.1
PathwayNitrogen metabolism
UniProt IDO43570
PDB Structure1JCZ; 1JD0.    
FunctionReversible hydration of carbon dioxide.    
SequenceMPRRSLHAAAVLLLVILKEQPSSPAPVNGSKWTYFGPDGENSWSKKYPSCGGLLQSPIDL HSDILQYDASLTPLEFQGYNLSANKQFLLTNNGHSVKLNLPSDMHIQGLQSRYSATQLHL HWGNPNDPHGSEHTVSGQHFAAELHIVHYNSDLYPDASTASNKSEGLAVLAVLIEMGSFN PSYDKIFSHLQHVKYKGQEAFVPGFNIEELLPERTAEYYRYRGSLTTPPCNPTVLWTVFR NPVQISQEQLLALETALYCTHMDDPSPREMINNFRQVQKFDERLVYTSFSQVQVCTAAGL SLGIILSLALAGILGICIVVVVSIWLFRRKSIKKGDNKGVIYKPATKMETEAHA
Target ValidationClick to Find Target Validation Information.    
Inhibitor1,4-Dihydro-1-methyl-4-oxo-3-pyridinesulfonamide[3]
1-Benzyl-1,4-dihydro-4-oxo-3-pyridinesulfonamide[3]
2,2,2-Trifluoro-N- (4-sulfamoyl-phenyl)-acetamide[4]
2,2-Dimethyl-N- (4-sulfamoyl-phenyl)-propionamide[4]
2,3-dihydro-1H-indene-5-sulfonamide[5]
2,4-Disulfamyltrifluoromethylaniline[6]
2-Amino-benzenesulfonamide[6]
2-Hydrazino-benzenesulfonamide[6]
2-acetamido-2,3-dihydro-1H-indene-5-sulfonic acid[5]
2-amino-2,3-dihydro-1H-indene-5-sulfonamide[5]
2-amino-2,3-dihydro-1H-indene-5-sulfonic acid[5]
2-oxo-2H-chromene-3-carboxylic acid[7]
2-oxo-2H-thiochromene-3-carboxylic acid[7]
3- ([8]
3- (3-Phenyl-ureido)-benzenesulfonamide[4]
3- (4'-Aminophenyl)diazenylbenzenesulfonamide[8]
3- (4'-Hydroxyphenyl)diazenylbenzenesulfonamide[8]
3-Amino-benzenesulfonamide[9]
4,4'-thiodipyridine-3-sulfonamide[10]
4- (2-Amino-ethyl)-benzenesulfonamide[6]
4- (2-Hydroxy-ethyl)-benzenesulfonamide[6]
4- (2-Methyl-8-quinolinoxy)-3-pyridinesulfonamide[10]
4- (2-Propynylthio)pyridine-3-sulfonamide[10]
4- (4'-Hydroxyphenyl)diazenylbenzenesulfonamide[8]
4- (4'-N-Methylphenyl)diazenylbenzenesulfonamide[8]
4- (4-Cyanophenoxy)-3-pyridinesulfonamide[10]
4- (4-Fluorophenoxy)-3-pyridinesulfonamide[10]
4- (5-Methyl-2-pirazolino)-3-pyridinesulfonamide[10]
4- (Allylamino)-3-pyridinesulfonamide[10]
4- (Carbamolymethylthio)pyridine-3-sulfonamide[10]
4- (Cyanomethylthio)pyridine-3-sulfonamide[10]
4- (Methylhydrazino)-3-pyridinesulfonamide[10]
4- (N-Methyl-hydrazino)-benzenesulfonamide[6]
4- (N-Oxide-2-pyridylthio)pyridine-3-sulfonamide[10]
4- (Quinolinoxy)-3-pyridinesulfonamide[10]
4-Amino-3-bromo-benzenesulfonamide[6]
4-Amino-3-chloro-benzenesulfonamide[6]
4-Amino-3-fluoro-benzenesulfonamide[6]
4-Amino-3-iodo-benzenesulfonamide[6]
4-Benzenesulfonylamino-benzenesulfonamide[4]
4-Benzythiopyridine-3-sulfonamide[10]
4-CYANOPHENOL[11]
4-Ethoxy-3-pyridinesulfonamide[10]
4-Hydrazino-3-pyridinesulfonamide[10]
4-Hydrazino-benzenesulfonamide[9]
4-Hydroxymethyl-benzenesulfonamide[6]
4-Methanesulfonylamino-benzenesulfonamide[4]
4-Methoxy-3-pyridinesulfonamide[10]
4-Methylamino-benzenesulfonamide[6]
4-Methylthiopyridine-3-sulfonamide[10]
4-[2- (3-Phenyl-ureido)-ethyl]-benzenesulfonamide[4]
5-amino-1,3,4-thiadiazole-2-sulfonamide[12]
6- (aminomethyl)-2H-chromen-2-one[7]
6- (hydroxymethyl)-2H-chromen-2-one[7]
6-Hydroxy-benzothiazole-2-sulfonic acid amide[6]
6-methoxy-2-oxo-2H-chromene-3-carboxylic acid[7]
6-methyl-2-oxo-2H-chromene-3-carboxylic acid[7]
7- (benzyloxy)-2H-chromen-2-one[7]
7-butoxy-2H-chromen-2-one[7]
7-methoxy-2-oxo-2H-chromene-4-carboxylic acid[7]
7-phenethoxy-2H-chromen-2-one[7]
7-propoxy-2H-chromen-2-one[7]
8-methoxy-2-oxo-2H-chromene-3-carboxylic acid[7]
ACETYLSULFANILAMIDE[4]
BENZOLAMIDE[6]
CATECHIN[13]
CATECHOL[14]
COUMARIN[7]
COUMATE[15]
CURCUMIN[13]
Carzenide,   Para-Carboxybenzenesulfonamide (Weak Carbonic Anhydrase Inhibitor)[6]
ELLAGIC ACID[14]
ETHOXYCOUMARIN[7]
FERULIC ACID[14]
GALLICACID[14]
HERNIARIN[7]
INDISULAM[3]
MAFENIDE[16]
N- (4-Sulfamoyl-phenyl)-benzamide[4]
N- (4-Sulfamoyl-phenyl)-butyramide[4]
N- (4-Sulfamoyl-phenyl)-isobutyramide[4]
N- (4-Sulfamoyl-phenyl)-propionamide[4]
N- (4-cyanophenyl)sulfamide[17]
N- (pentafluorophenyl)sulfamide[17]
N-hydroxysulfamide[18]
N-propynyl amidebenzenesulphonide[19]
N1- (2-aminoethyl)ethane-1,2-diamine[20]
N1- (naphthalen-1-yl)ethane-1,2-diamine[20]
O-propynylamide benzenesulphonamide[19]
P-TOLUENESULFONAMIDE[6]
PARABEN[14]
PHENOL[13]
Pentanoic acid (4-sulfamoyl-phenyl)-amide[4]
RESORCINOL[11]
SACCHARIN[21]
SALICYLATE[11]
Sodium N-methylphenylaminomethanesulfonate[8]
Sodium phenylaminomethanesulfonate[8]
Syringic Acid[14]
Thioureido sulfonamide[22]
Thioureido sulfonamide[22]
Thioureido sulfonamide[22]
decane-1,10-diyl disulfamate[23]
decyl sulfamate[23]
ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate[7]
hexane-1,6-diamine[20]
octane-1,8-diyl disulfamate[23]
octyl sulfamate[23]
p-Coumaric Acid[14]
pentane-1,5-diamine[20]
sulfanilamide derivative [24]
sulfanilamide derivative [24]
sulfanilamide derivative [24]
sulfanilamide derivative [24]
sulfanilamide derivative [24]
sulfanilamide derivative [24]
sulfanilamide derivative [24]
sulfanilamide derivative [24]
sulfanilamide derivative [24]
sulfanilamide derivative [24]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Expression of transmembrane carbonic anhydrase isoenzymes IX and XII in normal human pancreas and pancreatic tumours. Histochem Cell Biol. 2000 Sep;114(3):197-204. To Reference
Ref 2Physiology and molecular biology of renal carbonic anhydrase. J Nephrol. 2002 Mar-Apr;15 Suppl 5:S61-74. To Reference
Ref 3Eur J Med Chem. 2010 Sep;45(9):3656-61. Epub 2010 May 12.Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII. To Reference
Ref 4Bioorg Med Chem Lett. 2005 Nov 1;15(21):4862-6.Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides. To Reference
Ref 5Eur J Med Chem. 2008 Dec;43(12):2853-60. Epub 2008 Feb 29.Indanesulfonamides as carbonic anhydrase inhibitors and anticonvulsant agents: structure-activity relationship and pharmacological evaluation. To Reference
Ref 6Bioorg Med Chem Lett. 2005 Feb 15;15(4):963-9.Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs? To Reference
Ref 7J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins. To Reference
Ref 8Bioorg Med Chem. 2009 Oct 15;17(20):7093-9. Epub 2009 Sep 6.Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XII over the cytosolic isoforms I and II. To Reference
Ref 9Bioorg Med Chem Lett. 2005 Sep 1;15(17):3828-33.Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides. To Reference
Ref 10Eur J Med Chem. 2010 Jun;45(6):2396-404. Epub 2010 Feb 12.Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with 4-substituted 3-pyridinesulfonamides. To Reference
Ref 11Bioorg Med Chem. 2008 Aug 1;16(15):7424-8. Epub 2008 Jun 13.Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. To Reference
Ref 12Bioorg Med Chem Lett. 2010 Aug 1;20(15):4376-81. Epub 2010 Jun 17.Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. To Reference
Ref 13Bioorg Med Chem Lett. 2010 Sep 1;20(17):5050-3. Epub 2010 Jul 13.Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV. To Reference
Ref 14Bioorg Med Chem. 2010 Mar 15;18(6):2159-64. Epub 2010 Feb 6.Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. To Reference
Ref 15Bioorg Med Chem Lett. 2008 Aug 1;18(15):4282-6. Epub 2008 Jul 5.Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. To Reference
Ref 16J Med Chem. 2010 Apr 8;53(7):2913-26.Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. To Reference
Ref 17Bioorg Med Chem Lett. 2005 May 2;15(9):2353-8.Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with N-hydroxysulfamides--a new zinc-binding function in the design of inhibitors. To Reference
Ref 18Bioorg Med Chem Lett. 2010 Jun 15;20(12):3601-5. Epub 2010 Apr 28.Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. To Reference
Ref 19Bioorg Med Chem Lett. 2007 Feb 15;17(4):987-92. Epub 2006 Nov 17.Inhibition of membrane-associated carbonic anhydrase isozymes IX, XII and XIV with a library of glycoconjugate benzenesulfonamides. To Reference
Ref 20J Med Chem. 2010 Aug 12;53(15):5511-22.Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. To Reference
Ref 21Bioorg Med Chem Lett. 2008 Jan 15;18(2):836-41. Epub 2007 Nov 13.Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of the tumor-associated isoforms IX and XII. To Reference
Ref 22Bioorg Med Chem Lett. 2005 Sep 1;15(17):3821-7.Carbonic anhydrase inhibitors: design of thioureido sulfonamides with potent isozyme II and XII inhibitory properties and intraocular pressure lowering activity in a rabbit model of glaucoma. To Reference
Ref 23J Med Chem. 2009 Oct 8;52(19):5990-8.Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. To Reference
Ref 24Bioorg Med Chem Lett. 2005 Jun 15;15(12):3096-101.Carbonic anhydrase inhibitors. Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with Schiff's bases incorporating chromone and aromatic sulfonamide moieties, and their zinc complexes. To Reference



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543