Therapeutic Targets Database
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TTD Target ID: TTDR00211

Target Information
NameCarbonic anhydrase IX    
Type of targetResearch target    
SynonymsCA-IX    
CAIX    
Carbonate dehydratase IX    
G250 antigen (MN/CA IX/G250)    
Membrane antigen MN    
P54/58N    
PMW1    
RCC-associated antigen G250    
Renal cell carcinoma-associated antigen G250    
DiseaseBladder cancer
[ICD9: 188   ICD10: C67]
[1]
Head and neck squamous cell carcinomas
[ICD9: 199   ICD10: C44]
[2]
Pancreatic cancer
[ICD9: 157   ICD10: C25]
[3]
Renal cell carcinoma
[ICD9: 189   ICD10: C64]
[4][5][6]
BioChemical ClassCarbon-oxygen lyases    
EC NumberEC 4.2.1.1
PathwayNitrogen metabolism
UniProt IDQ16790
PDB Structure2HKF.    
FunctionReversible hydration of carbon dioxide. May be involved in the control of cell proliferation and transformation. Appears to be a novel specific biomarker for a cervical neoplasia.    
SequenceMAPLCPSPWLPLLIPAPAPGLTVQLLLSLLLLVPVHPQRLPRMQEDSPLGGGSSGEDDPL GEEDLPSEEDSPREEDPPGEEDLPGEEDLPGEEDLPEVKPKSEEEGSLKLEDLPTVEAPG DPQEPQNNAHRDKEGDDQSHWRYGGDPPWPRVSPACAGRFQSPVDIRPQLAAFCPALRPL ELLGFQLPPLPELRLRNNGHSVQLTLPPGLEMALGPGREYRALQLHLHWGAAGRPGSEHT VEGHRFPAEIHVVHLSTAFARVDEALGRPGGLAVLAAFLEEGPEENSAYEQLLSRLEEIA EEGSETQVPGLDISALLPSDFSRYFQYEGSLTTPPCAQGVIWTVFNQTVMLSAKQLHTLS DTLWGPGDSRLQLNFRATQPLNGRVIEASFPAGVDSSPRAAEPVQLNSCLAAGDILALVF GLLFAVTSVAFLVQMRRQHRRGTKGGVSYRPAEVAETGA
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor1-acetamido-5-sulfonamidoindane[7]
2-acetamido-5-sulfonamidoindane[7]
4-azidobenzenesulfonamide[8]
4-ethynyl benzene sulfonamide[9]
ACETYLSULFANILAMIDE[10]
Aminobenzolamide derivative[11]
Azide[12]
BENZOLAMIDE[13]
BICARBONATE[14]
CATECHIN[15]
CGS-27023A[16]
COUMARIN[17]
COUMATE[18]
CURCUMIN[15]
ELLAGIC ACID[19]
EMATE[20]
ETHOXYCOUMARIN[17]
FERULIC ACID[19]
GALLICACID[19]
HERNIARIN[17]
HYDROSULFIDE[12]
INDISULAM[21]
MAFENIDE[22]
N-hydroxysulfamide[23]
N1- (2-aminoethyl)ethane-1,2-diamine[24]
N1- (naphthalen-1-yl)ethane-1,2-diamine[24]
NSC-654077[25]
PARABEN[19]
PHENOL[15]
PHENYLDIFLUOROMETHANESULFONAMIDE[20]
PHENYLMETHANESULFONAMIDE[20]
PHENYLSULFAMATE[20]
Pentanoic acid (4-sulfamoyl-phenyl)-amide[10]
SACCHARIN[26]
SPERMINE[24]
SULFAMATE[14]
SULFAMIDE[14]
Sodium N-methylphenylaminomethanesulfonate[27]
Sodium phenylaminomethanesulfonate[27]
Syringic Acid[19]
UMBELLIFERONE[28]
decyl sulfamate[29]
hexane-1,6-diamine[24]
octyl sulfamate[29]
p-Coumaric Acid[19]
pentane-1,5-diamine[24]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The hypoxia-inducible genes VEGF and CA9 are differentially regulated in superficial vs invasive bladder cancer. Br J Cancer. 2002 Apr 22;86(8):1276-82. To Reference
Ref 2Carbonic anhydrase IX, an endogenous hypoxia marker, expression in head and neck squamous cell carcinoma and its relationship to hypoxia, necrosis, and microvessel density. Cancer Res. 2001 Jul 1;61(13):5262-7. To Reference
Ref 3Expression 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 4MN/CA IX antigen as a potential target for renal cell carcinoma. Hinyokika Kiyo. 2000 Oct;46(10):745-8. To Reference
Ref 5MN/CA IX/G250 as a potential target for immunotherapy of renal cell carcinomas. Br J Cancer. 1999 Oct;81(4):741-6. To Reference
Ref 6Quantification of G250 mRNA expression in renal epithelial neoplasms by real-time reverse transcription-PCR of dissected tissue from paraffin sections. Pathology. 2003 Dec;35(6):513-7. To Reference
Ref 7J Med Chem. 2006 May 4;49(9):2743-9.Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX. To Reference
Ref 8Bioorg Med Chem Lett. 2009 Apr 15;19(8):2273-6. Epub 2009 Feb 26.Inhibition of carbonic anhydrase isozymes with benzene sulfonamides incorporating thio, sulfinyl and sulfonyl glycoside moieties. To Reference
Ref 9J Med Chem. 2008 Mar 27;51(6):1945-53. Epub 2008 Feb 29.Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides. To Reference
Ref 10Bioorg 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 11Bioorg Med Chem Lett. 2004 Dec 6;14(23):5775-80.Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide. To Reference
Ref 12Bioorg Med Chem Lett. 2004 Dec 6;14(23):5769-73.Carbonic anhydrase inhibitors: inhibition of the membrane-bound human isozyme IV with anions. To Reference
Ref 13J Med Chem. 2009 Feb 12;52(3):646-54.Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV. To Reference
Ref 14Bioorg Med Chem Lett. 2005 Feb 1;15(3):567-71.Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V, and IX with anions isosteric and isoelectronic with sulfate, nitrate, and carbonate. To Reference
Ref 15Bioorg 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 16Bioorg Med Chem. 2007 Mar 15;15(6):2298-311. Epub 2007 Jan 19.Carbonic anhydrase and matrix metalloproteinase inhibitors. Inhibition of human tumor-associated isozymes IX and cytosolic isozyme I and II with sulfonylated hydroxamates. To Reference
Ref 17J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins. To Reference
Ref 18Bioorg 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 19Bioorg 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 20Bioorg Med Chem Lett. 2005 Dec 1;15(23):5192-6. Epub 2005 Oct 3.Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides. To Reference
Ref 21Eur 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 22J 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 23Bioorg 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 24J Med Chem. 2010 Aug 12;53(15):5511-22.Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. To Reference
Ref 25J Med Chem. 2008 Jun 12;51(11):3051-6. Epub 2008 Mar 19.Recent developments of carbonic anhydrase inhibitors as potential anticancer drugs. To Reference
Ref 26Bioorg 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 27Bioorg 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 28Bioorg Med Chem Lett. 2010 Dec 15;20(24):7255-8. Epub 2010 Oct 25.7,8-disubstituted- but not 6,7-disubstituted coumarins selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic ones I and II in the low nanomolar/subnanomolar range. To Reference
Ref 29J 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



 

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