Target Information

Target General Infomation
Target ID
T16987
Former ID
TTDR00212
Target Name
Carbonic anhydrase XII
Gene Name
CA12
Synonyms
CA-XII; Carbonate dehydratase XII; Tumor antigen HOM-RCC-3.1.3; CA12
Target Type
Clinical Trial
Disease Breast cancer [ICD9: 174, 175; ICD10: C50]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Function
Reversible hydration of carbon dioxide.
BioChemical Class
Carbon-oxygen lyases
Target Validation
T16987
UniProt ID
O43570
EC Number
EC 4.2.1.1
Sequence
MPRRSLHAAAVLLLVILKEQPSSPAPVNGSKWTYFGPDGENSWSKKYPSCGGLLQSPIDL
HSDILQYDASLTPLEFQGYNLSANKQFLLTNNGHSVKLNLPSDMHIQGLQSRYSATQLHL
HWGNPNDPHGSEHTVSGQHFAAELHIVHYNSDLYPDASTASNKSEGLAVLAVLIEMGSFN
PSYDKIFSHLQHVKYKGQEAFVPGFNIEELLPERTAEYYRYRGSLTTPPCNPTVLWTVFR
NPVQISQEQLLALETALYCTHMDDPSPREMINNFRQVQKFDERLVYTSFSQVQVCTAAGL
SLGIILSLALAGILGICIVVVVSIWLFRRKSIKKGDNKGVIYKPATKMETEAHA
Drugs and Mode of Action
Drug(s) MAFENIDE Drug Info Approved Bacterial infection [530765]
SALICYLATE Drug Info Phase 4 Discovery agent [524105]
Curcumin Drug Info Phase 3 Cancer [532348], [542031]
PARABEN Drug Info Phase 3 Discovery agent [524059]
PHENOL Drug Info Phase 2/3 Discovery agent [525296]
COUMATE Drug Info Phase 2 Breast cancer [531371]
Inhibitor 1,4-Dihydro-1-methyl-4-oxo-3-pyridinesulfonamide Drug Info [530978]
1-Benzyl-1,4-dihydro-4-oxo-3-pyridinesulfonamide Drug Info [530978]
2,2,2-Trifluoro-N-(4-sulfamoyl-phenyl)-acetamide Drug Info [527743]
2,2-Dimethyl-N-(4-sulfamoyl-phenyl)-propionamide Drug Info [527743]
2,3-dihydro-1H-indene-5-sulfonamide Drug Info [529417]
2,4-Disulfamyltrifluoromethylaniline Drug Info [527407]
2-acetamido-2,3-dihydro-1H-indene-5-sulfonic acid Drug Info [529417]
2-amino-2,3-dihydro-1H-indene-5-sulfonamide Drug Info [529417]
2-Amino-benzenesulfonamide Drug Info [527407]
2-Amino-indan-5-sulfonic acid Drug Info [529417]
2-hydrazinylbenzenesulfonamide Drug Info [527407]
2-oxo-2H-chromene-3-carboxylic acid Drug Info [530514]
2-oxo-2H-thiochromene-3-carboxylic acid Drug Info [530514]
3-((4-aminophenyl)diazenyl)benzenesulfonamide Drug Info [530399]
3-((4-hydroxyphenyl)diazenyl)benzenesulfonamide Drug Info [530399]
3-(3-Phenyl-ureido)-benzenesulfonamide Drug Info [527743]
3-(4'-Hydroxyphenyl)diazenylbenzenesulfonamide Drug Info [530399]
3-Amino-benzenesulfonamide Drug Info [527654]
4,4'-thiodipyridine-3-sulfonamide Drug Info [530766]
4-((4-hydroxyphenyl)diazenyl)benzenesulfonamide Drug Info [530399]
4-(2-Amino-ethyl)-benzenesulfonamide Drug Info [527407]
4-(2-Hydroxy-ethyl)-benzenesulfonamide Drug Info [527407]
4-(2-Methyl-8-quinolinoxy)-3-pyridinesulfonamide Drug Info [530766]
4-(2-Propynylthio)pyridine-3-sulfonamide Drug Info [530766]
4-(4'-N-Methylphenyl)diazenylbenzenesulfonamide Drug Info [530399]
4-(4-Cyanophenoxy)-3-pyridinesulfonamide Drug Info [530766]
4-(4-Fluorophenoxy)-3-pyridinesulfonamide Drug Info [530766]
4-(5-Methyl-2-pirazolino)-3-pyridinesulfonamide Drug Info [530766]
4-(Allylamino)-3-pyridinesulfonamide Drug Info [530766]
4-(Carbamolymethylthio)pyridine-3-sulfonamide Drug Info [530766]
4-(Cyanomethylthio)pyridine-3-sulfonamide Drug Info [530766]
4-(hydroxymethyl)benzenesulfonamide Drug Info [527407]
4-(Methylhydrazino)-3-pyridinesulfonamide Drug Info [530766]
4-(N-Methyl-hydrazino)-benzenesulfonamide Drug Info [527407]
4-(N-Oxide-2-pyridylthio)pyridine-3-sulfonamide Drug Info [530766]
4-(Quinolinoxy)-3-pyridinesulfonamide Drug Info [530766]
4-Amino-3-bromo-benzenesulfonamide Drug Info [527407]
4-Amino-3-chloro-benzenesulfonamide Drug Info [527407]
4-Amino-3-fluoro-benzenesulfonamide Drug Info [527407]
4-Amino-3-iodo-benzenesulfonamide Drug Info [527407]
4-Benzenesulfonylamino-benzenesulfonamide Drug Info [527743]
4-Benzythiopyridine-3-sulfonamide Drug Info [530766]
4-CYANOPHENOL Drug Info [529562]
4-Ethoxy-3-pyridinesulfonamide Drug Info [530766]
4-Hydrazino-3-pyridinesulfonamide Drug Info [530766]
4-Hydrazino-benzenesulfonamide Drug Info [527654]
4-Methanesulfonylamino-benzenesulfonamide Drug Info [527743]
4-Methoxy-3-pyridinesulfonamide Drug Info [530766]
4-Methylamino-benzenesulfonamide Drug Info [527407]
4-Methylthiopyridine-3-sulfonamide Drug Info [530766]
4-[2-(3-Phenyl-ureido)-ethyl]-benzenesulfonamide Drug Info [527743]
5-amino-1,3,4-thiadiazole-2-sulfonamide Drug Info [531013]
6-(aminomethyl)-2H-chromen-2-one Drug Info [530514]
6-(hydroxymethyl)-2H-chromen-2-one Drug Info [530514]
6-Hydroxy-benzothiazole-2-sulfonic acid amide Drug Info [527407]
6-methoxy-2-oxo-2H-chromene-3-carboxylic acid Drug Info [530514]
6-methyl-2-oxo-2H-chromene-3-carboxylic acid Drug Info [530514]
7-(benzyloxy)-2H-chromen-2-one Drug Info [530514]
7-butoxy-2H-chromen-2-one Drug Info [530514]
7-methoxy-2-oxo-2H-chromene-4-carboxylic acid Drug Info [530514]
7-phenethoxy-2H-chromen-2-one Drug Info [530514]
7-propoxy-2H-chromen-2-one Drug Info [530514]
8-methoxy-2-oxo-2H-chromene-3-carboxylic acid Drug Info [530514]
ACETYLSULFANILAMIDE Drug Info [527743]
BENZOLAMIDE Drug Info [527407]
Carzenide Drug Info [527407]
CATECHIN Drug Info [531068]
CATECHOL Drug Info [530751]
COUMARIN Drug Info [530514]
COUMATE Drug Info [529605]
Curcumin Drug Info [531068]
Decane-1,10-diyl disulfamate Drug Info [530359]
Decyl sulfamate Drug Info [530359]
ELLAGIC ACID Drug Info [530751]
ETHOXYCOUMARIN Drug Info [530514]
Ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate Drug Info [530514]
FERULIC ACID Drug Info [530751]
GALLICACID Drug Info [530751]
HERNIARIN Drug Info [530514]
Hexane-1,6-diamine Drug Info [530998]
MAFENIDE Drug Info [530765]
N-(4-cyanophenyl)sulfamide Drug Info [527520]
N-(4-Sulfamoyl-phenyl)-benzamide Drug Info [527743]
N-(4-Sulfamoyl-phenyl)-butyramide Drug Info [527743]
N-(4-Sulfamoyl-phenyl)-isobutyramide Drug Info [527743]
N-(4-Sulfamoyl-phenyl)-propionamide Drug Info [527743]
N-(pentafluorophenyl)sulfamide Drug Info [527520]
N-hydroxysulfamide Drug Info [530922]
N-propynyl amidebenzenesulphonide Drug Info [528574]
N1-(2-aminoethyl)ethane-1,2-diamine Drug Info [530998]
N1-(naphthalen-1-yl)ethane-1,2-diamine Drug Info [530998]
Octane-1,8-diyl disulfamate Drug Info [530359]
Octyl sulfamate Drug Info [530359]
P-Coumaric Acid Drug Info [530751]
P-TOLUENESULFONAMIDE Drug Info [527407]
PARABEN Drug Info [530751]
Pentane-1,5-diamine Drug Info [530998]
Pentanoic acid (4-sulfamoyl-phenyl)-amide Drug Info [527743]
PHENOL Drug Info [531068]
Prop-2-ynyl 4-sulfamoylbenzoate Drug Info [528574]
RESORCINOL Drug Info [529562]
SACCHARIN Drug Info [529179]
SALICYLATE Drug Info [529562]
Sodium N-methylphenylaminomethanesulfonate Drug Info [530399]
Sodium phenylaminomethanesulfonate Drug Info [530399]
Sulfanilamide derivative Drug Info [527560]
Syringic Acid Drug Info [530751]
Thioureido sulfonamide Drug Info [527655]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Nitrogen metabolism
NetPath Pathway TGF_beta_Receptor Signaling Pathway
Reactome Reversible hydration of carbon dioxide
WikiPathways Reversible Hydration of Carbon Dioxide
miR-targeted genes in muscle cell - TarBase
miR-targeted genes in leukocytes - TarBase
miR-targeted genes in epithelium - TarBase
References
Ref 524059ClinicalTrials.gov (NCT01688479) Trial Comparing Calendula Officinalis With Aqueous Cream "Essex" to Treat Skin Reactions From Radiotherapy of Breast Cancer. U.S. National Institutes of Health.
Ref 524105ClinicalTrials.gov (NCT01712295) 17% Salicylate Versus 17% Salicylate-Ethyl Pyruvate for Plantar Foot Warts. U.S. National Institutes of Health.
Ref 525296ClinicalTrials.gov (NCT02527187) Determination of the Sensitivity and Specificity of Prick Test Betula Verrucosa.
Ref 530765J Med Chem. 2010 Apr 8;53(7):2913-26.Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases.
Ref 531371Irosustat: a first-generation steroid sulfatase inhibitor in breast cancer. Expert Rev Anticancer Ther. 2011 Feb;11(2):179-83.
Ref 532348Nanocurcumin: a promising therapeutic advancement over native curcumin. Crit Rev Ther Drug Carrier Syst. 2013;30(4):331-68.
Ref 542031(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7000).
Ref 527407Bioorg 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?.
Ref 527520Bioorg 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.
Ref 527560Bioorg 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.
Ref 527654Bioorg Med Chem Lett. 2005 Sep 1;15(17):3828-33.Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides.
Ref 527655Bioorg 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.
Ref 527743Bioorg 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.
Ref 528574Bioorg 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.
Ref 529179Bioorg 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 potentinhibitors of the tumor-associated isoforms IX and XII.
Ref 529417Eur 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.
Ref 529562Bioorg 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.
Ref 529605Bioorg 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.
Ref 530359J 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.
Ref 530399Bioorg 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 XIIover the cytosolic isoforms I and II.
Ref 530514J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins.
Ref 530751Bioorg 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.
Ref 530765J Med Chem. 2010 Apr 8;53(7):2913-26.Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases.
Ref 530766Eur 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.
Ref 530922Bioorg 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.
Ref 530978Eur 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.
Ref 530998J Med Chem. 2010 Aug 12;53(15):5511-22.Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule.
Ref 531013Bioorg 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 acetazolamideresides in a less utilized binding pocket than most hydrophobic inhibitors.
Ref 531068Bioorg 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.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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