Target Information
Target General Infomation | |||||
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Target ID |
T43920
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Former ID |
TTDS00304
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Target Name |
Carbonic anhydrase
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Target Type |
Successful
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Disease | Breast cancer [ICD9: 174, 175; ICD10: C50] | ||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Hypertension; Congestive heart failure [ICD9:401, 428; ICD10: I10-I16, I50] | |||||
Obesity [ICD9: 278; ICD10: E66] | |||||
BioChemical Class |
Carbon-oxygen lyases
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Target Validation |
T43920
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EC Number |
EC 4.2.1.1
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Drugs and Mode of Action | |||||
Drug(s) | MAFENIDE | Drug Info | Approved | Bacterial infection | [530765] |
Quinethazone | Drug Info | Approved | Hypertension; Congestive heart failure | [538464], [542309], [551871] | |
SALICYLATE | Drug Info | Phase 4 | Discovery agent | [524105] | |
Curcumin | Drug Info | Phase 3 | Cancer | [532348], [542031] | |
PARABEN | Drug Info | Phase 3 | Discovery agent | [524059] | |
Phentermine+topiramate | Drug Info | Phase 3 | Obesity | [536869] | |
PHENOL | Drug Info | Phase 2/3 | Discovery agent | [525296] | |
COUMATE | Drug Info | Phase 2 | Breast cancer | [531371] | |
SULFAMIDE | Drug Info | Phase 1 | Discovery agent | [524873] | |
CLIOQUINOL | Drug Info | Withdrawn from market | Discovery agent | [522766] | |
SPERMINE | Drug Info | Terminated | Discovery agent | [542107], [546483] | |
Inhibitor | (2-bromophenyl)difluoromethanesulfonamide | Drug Info | [527782] | ||
(4-bromophenyl)difluoromethanesulfonamide | Drug Info | [527782] | |||
1-(3,4-dichlorophenyl)-3-hydroxyurea | Drug Info | [528240] | |||
2,3-dihydro-1H-indene-5-sulfonamide | Drug Info | [529417] | |||
2,4-Disulfamyltrifluoromethylaniline | Drug Info | [529948] | |||
2,5-difluorophenol | Drug Info | [529562] | |||
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 | [529948] | |||
2-Amino-indan-5-sulfonic acid | Drug Info | [529417] | |||
2-hydrazinylbenzenesulfonamide | Drug Info | [529948] | |||
2-oxo-2H-chromene-3-carboxylic acid | Drug Info | [530514] | |||
2-oxo-2H-thiochromene-3-carboxylic acid | Drug Info | [530514] | |||
3,5-difluorophenol | Drug Info | [529489] | |||
3-(4-sulfamoylphenyl)propanoic acid | Drug Info | [530146] | |||
3-Amino-benzenesulfonamide | Drug Info | [527292] | |||
3-bromophenyl-difluoromethanesulfonamide | Drug Info | [527782] | |||
3-Nitro-benzenesulfonamide | Drug Info | [527253] | |||
4-(2-Amino-ethyl)-benzenesulfonamide | Drug Info | [527408] | |||
4-(2-aminopyrimidin-4-ylamino)benzenesulfonamide | Drug Info | [529948] | |||
4-(2-Hydroxy-ethyl)-benzenesulfonamide | Drug Info | [529948] | |||
4-(2-Phenylacetamido)-3-bromobenzenesulfonamide | Drug Info | [530219] | |||
4-(2-Phenylacetamido)-3-chlorobenzenesulfonamide | Drug Info | [530219] | |||
4-(2-Phenylacetamido)-3-fluorobenzenesulfonamide | Drug Info | [530219] | |||
4-(2-Phenylacetamido)benzenesulfonamide | Drug Info | [530219] | |||
4-(2-Phenylacetamidoethyl)benzenesulfonamide | Drug Info | [530219] | |||
4-(2-Phenylacetamidomethyl)benzenesulfonamide | Drug Info | [530219] | |||
4-(2-Pyridin-2-ylacetamido)benzenesulfonamide | Drug Info | [530219] | |||
4-(2-Pyridin-4-ylacetamido)benzenesulfonamide | Drug Info | [530219] | |||
4-(hydroxymethyl)benzenesulfonamide | Drug Info | [529948] | |||
4-amino-3,5-dibromobenzenesulfonamide | Drug Info | [529030] | |||
4-Amino-3-bromo-benzenesulfonamide | Drug Info | [529948] | |||
4-Amino-3-chloro-benzenesulfonamide | Drug Info | [529948] | |||
4-amino-3-fluoro-5-iodobenzenesulfonamide | Drug Info | [529030] | |||
4-Amino-3-fluoro-benzenesulfonamide | Drug Info | [529948] | |||
4-Amino-3-iodo-benzenesulfonamide | Drug Info | [529948] | |||
4-amino-6-chlorobenzene-1,3-disulfonamide | Drug Info | [529948] | |||
4-amino-N-(4-sulfamoylbenzyl)benzenesulfonamide | Drug Info | [529948] | |||
4-AMINOPHENOL | Drug Info | [529562] | |||
4-azidobenzenesulfonamide | Drug Info | [529609] | |||
4-bromophenylboronic acid | Drug Info | [530086] | |||
4-butylphenylboronic acid | Drug Info | [530086] | |||
4-CYANOPHENOL | Drug Info | [529562] | |||
4-Hydrazino-benzenesulfonamide | Drug Info | [529948] | |||
4-methoxyphenylboronic acid | Drug Info | [530086] | |||
4-methylphenyl-difluoromethanesulfonamide | Drug Info | [527782] | |||
4-Nitro-benzenesulfonamide | Drug Info | [527253] | |||
4-nitrophenyl phosphate | Drug Info | [531156] | |||
4-nitrophenyl-difluoromethanesulfonamide | Drug Info | [527782] | |||
4-phenoxyphenylboronic acid | Drug Info | [530086] | |||
4-Thiocyanato-benzenesulfonamide | Drug Info | [527253] | |||
4-[2-(2-Thienyl)acetamidoethyl]benzenesulfonamide | Drug Info | [530219] | |||
4-[2-(2-Thienyl)acetamido]benzenesulfonamide | Drug Info | [530219] | |||
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 | [529948] | |||
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] | |||
BENZOLAMIDE | Drug Info | [529948] | |||
Benzothiazole-2-sulfonic acid amide | Drug Info | [527408] | |||
Beta-Mercaptoethanol | Drug Info | [551393] | |||
Beta-naphthylboronic acid | Drug Info | [530086] | |||
Biphenyl-4-ylboronic acid | Drug Info | [530086] | |||
Carzenide | Drug Info | [529948] | |||
CATECHIN | Drug Info | [531068] | |||
CATECHOL | Drug Info | [530751] | |||
CLIOQUINOL | Drug Info | [529489] | |||
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 | [529948] | |||
N-(5-ethyl-1,3,4-thiadiazol-2-yl)sulfamide | Drug Info | [529794] | |||
N-(5-phenyl-1,3,4-thiadiazol-2-yl)sulfamide | Drug Info | [529794] | |||
N-(5-tert-butyl-1,3,4-thiadiazol-2-yl)sulfamide | Drug Info | [529794] | |||
N-[5-(ethylthio)-1,3,4-thiadiazol-2-yl]sulfamide | Drug Info | [529794] | |||
N-[5-(methylthio)-1,3,4-thiadiazol-2-yl]sulfamide | Drug Info | [529794] | |||
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 | [529948] | |||
P-tolylboronic acid | Drug Info | [530086] | |||
PARABEN | Drug Info | [530751] | |||
PARAOXON | Drug Info | [531156] | |||
Pentane-1,5-diamine | Drug Info | [530998] | |||
PHENOL | Drug Info | [531068] | |||
Phentermine+topiramate | Drug Info | [536710] | |||
Phenyl Boronic acid | Drug Info | [528141] | |||
Phenylarsonic acid | Drug Info | [528141] | |||
PHENYLDIFLUOROMETHANESULFONAMIDE | Drug Info | [527782] | |||
PHENYLMETHANESULFONAMIDE | Drug Info | [527782] | |||
PRONTOCIL | Drug Info | [529030] | |||
Quinethazone | Drug Info | [536672] | |||
RESORCINOL | Drug Info | [529562] | |||
SACCHARIN | Drug Info | [530466] | |||
SALICYLATE | Drug Info | [529489] | |||
Sodium maleate | Drug Info | [530027] | |||
SPERMINE | Drug Info | [530998] | |||
SULFAMATE | Drug Info | [528141] | |||
SULFAMIDE | Drug Info | [530922] | |||
Syringic Acid | Drug Info | [530751] | |||
References | |||||
Ref 522766 | ClinicalTrials.gov (NCT00963495) Study Evaluating the Tolerance and Biological Activity of Oral Clioquinol in Patients With Relapsed or Refractory Hematological Malignancy. U.S. National Institutes of Health. | ||||
Ref 524059 | ClinicalTrials.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 524105 | ClinicalTrials.gov (NCT01712295) 17% Salicylate Versus 17% Salicylate-Ethyl Pyruvate for Plantar Foot Warts. U.S. National Institutes of Health. | ||||
Ref 524873 | ClinicalTrials.gov (NCT02216669) Trial to Determine Optimal Phase II Dose of the Oral Dual CAIX Inhibitor/ Radiosensitizer. U.S. National Institutes of Health. | ||||
Ref 525296 | ClinicalTrials.gov (NCT02527187) Determination of the Sensitivity and Specificity of Prick Test Betula Verrucosa. | ||||
Ref 530765 | J Med Chem. 2010 Apr 8;53(7):2913-26.Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. | ||||
Ref 531371 | Irosustat: a first-generation steroid sulfatase inhibitor in breast cancer. Expert Rev Anticancer Ther. 2011 Feb;11(2):179-83. | ||||
Ref 532348 | Nanocurcumin: a promising therapeutic advancement over native curcumin. Crit Rev Ther Drug Carrier Syst. 2013;30(4):331-68. | ||||
Ref 536869 | Adjunctive topiramate enhances the risk of hypothermia associated with valproic acid therapy. J Clin Pharm Ther. 2008 Oct;33(5):513-9. | ||||
Ref 538464 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 013264. | ||||
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 542107 | (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: 710). | ||||
Ref 542309 | (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: 7289). | ||||
Ref 527253 | Bioorg Med Chem Lett. 2004 Nov 15;14(22):5703-7.Carbonic anhydrase inhibitors: inhibition of human cytosolic isozyme II and mitochondrial isozyme V with a series of benzene sulfonamide derivatives. | ||||
Ref 527292 | Bioorg Med Chem Lett. 2004 Dec 20;14(24):6001-6.Carbonic anhydrase inhibitors. Inhibition of the prokariotic beta and gamma-class enzymes from Archaea with sulfonamides. | ||||
Ref 527408 | Bioorg Med Chem Lett. 2005 Feb 15;15(4):971-6.Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. | ||||
Ref 527782 | Bioorg 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. | ||||
Ref 528141 | Bioorg Med Chem Lett. 2006 Jun 15;16(12):3139-43. Epub 2006 Apr 18.Carbonic anhydrase inhibitors: inhibition of the cytosolic human isozyme VII with anions. | ||||
Ref 528240 | Bioorg Med Chem Lett. 2006 Aug 15;16(16):4316-20. Epub 2006 Jun 12.N-hydroxyurea--a versatile zinc binding function in the design of metalloenzyme inhibitors. | ||||
Ref 529030 | Bioorg Med Chem. 2007 Dec 1;15(23):7229-36. Epub 2007 Aug 25.Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides. | ||||
Ref 529417 | Eur 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 529489 | Bioorg Med Chem Lett. 2008 Jun 15;18(12):3593-6. Epub 2008 May 4.Carbonic anhydrase inhibitors: Inhibition of the new membrane-associated isoform XV with phenols. | ||||
Ref 529562 | Bioorg 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 529605 | Bioorg 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 529609 | Bioorg Med Chem Lett. 2008 Aug 15;18(16):4624-7. Epub 2008 Jul 10.Inhibition of human mitochondrial carbonic anhydrases VA and VB with para-(4-phenyltriazole-1-yl)-benzenesulfonamide derivatives. | ||||
Ref 529794 | Bioorg Med Chem Lett. 2008 Dec 15;18(24):6332-5. Epub 2008 Nov 1.Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV. | ||||
Ref 529948 | J 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. | ||||
Ref 530027 | Bioorg Med Chem. 2009 Apr 1;17(7):2654-7. Epub 2009 Mar 5.Carbonic anhydrase inhibitors. Inhibition of the beta-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with aliphatic and aromatic carboxylates. | ||||
Ref 530086 | Bioorg Med Chem Lett. 2009 May 15;19(10):2642-5. Epub 2009 Apr 5.Carbonic anhydrase inhibitors. Inhibition of the fungal beta-carbonic anhydrases from Candida albicans and Cryptococcus neoformans with boronic acids. | ||||
Ref 530146 | Bioorg Med Chem. 2009 Jul 1;17(13):4503-9. Epub 2009 May 8.Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. | ||||
Ref 530219 | Bioorg Med Chem. 2009 Jul 15;17(14):4894-9. Epub 2009 Jun 9.Carbonic anhydrase inhibitors. Aromatic/heterocyclic sulfonamides incorporating phenacetyl, pyridylacetyl and thienylacetyl tails act as potent inhibitors of human mitochondrial isoforms VA and VB. | ||||
Ref 530359 | J 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 530466 | Bioorg Med Chem Lett. 2009 Dec 1;19(23):6649-54. Epub 2009 Oct 7.Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c. | ||||
Ref 530514 | J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins. | ||||
Ref 530751 | Bioorg 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 530922 | Bioorg 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 530998 | J Med Chem. 2010 Aug 12;53(15):5511-22.Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. | ||||
Ref 531013 | Bioorg 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 531068 | Bioorg 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 531156 | Bioorg Med Chem Lett. 2010 Nov 1;20(21):6208-12. Epub 2010 Aug 26.Paraoxon, 4-nitrophenyl phosphate and acetate are substrates of |A- but not of |A-, |?- and |?-carbonic anhydrases. |
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