Target Information
Target General Infomation | |||||
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Target ID |
T31992
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Former ID |
TTDR00213
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Target Name |
Carbonic anhydrase XIV
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Gene Name |
CA14
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Synonyms |
CA-XIV; Carbonate dehydratase XIV; UNQ690/PRO1335; CA14
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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] | |||||
Inborn error of metabolism [ICD10: E88.9] | |||||
Function |
Reversible hydration of carbon dioxide.
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BioChemical Class |
Carbon-oxygen lyases
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Target Validation |
T31992
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UniProt ID | |||||
EC Number |
EC 4.2.1.1
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Sequence |
MLFSALLLEVIWILAADGGQHWTYEGPHGQDHWPASYPECGNNAQSPIDIQTDSVTFDPD
LPALQPHGYDQPGTEPLDLHNNGHTVQLSLPSTLYLGGLPRKYVAAQLHLHWGQKGSPGG SEHQINSEATFAELHIVHYDSDSYDSLSEAAERPQGLAVLGILIEVGETKNIAYEHILSH LHEVRHKDQKTSVPPFNLRELLPKQLGQYFRYNGSLTTPPCYQSVLWTVFYRRSQISMEQ LEKLQGTLFSTEEEPSKLLVQNYRALQPLNQRMVFASFIQAGSSYTTGEMLSLGVGILVG CLCLLLAVYFIARKIRKKRLENRKSVVFTSAQATTEA |
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Drugs and Mode of Action | |||||
Drug(s) | MAFENIDE | Drug Info | Approved | Bacterial infection | [530765] |
TRIENTINE | Drug Info | Approved | Inborn error of metabolism | [551871] | |
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] | |
SPERMINE | Drug Info | Terminated | Discovery agent | [542107], [546483] | |
Inhibitor | 2,3-dihydro-1H-indene-5-sulfonamide | Drug Info | [529417] | ||
2,4-Disulfamyltrifluoromethylaniline | Drug Info | [527654] | |||
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 | [527654] | |||
2-Amino-indan-5-sulfonic acid | Drug Info | [529417] | |||
2-oxo-2H-chromene-3-carboxylic acid | Drug Info | [530514] | |||
2-oxo-2H-thiochromene-3-carboxylic acid | Drug Info | [530514] | |||
3-Amino-benzenesulfonamide | Drug Info | [527654] | |||
4,4'-thiodipyridine-3-sulfonamide | Drug Info | [530766] | |||
4-(2-Amino-ethyl)-benzenesulfonamide | Drug Info | [527654] | |||
4-(2-Hydroxy-ethyl)-benzenesulfonamide | Drug Info | [527654] | |||
4-(2-Methyl-8-quinolinoxy)-3-pyridinesulfonamide | Drug Info | [530766] | |||
4-(2-Propynylthio)pyridine-3-sulfonamide | 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 | [527654] | |||
4-(Methylhydrazino)-3-pyridinesulfonamide | Drug Info | [530766] | |||
4-(Quinolinoxy)-3-pyridinesulfonamide | Drug Info | [530766] | |||
4-Amino-3-bromo-benzenesulfonamide | Drug Info | [527654] | |||
4-Amino-3-chloro-benzenesulfonamide | Drug Info | [527654] | |||
4-Amino-3-fluoro-benzenesulfonamide | Drug Info | [527654] | |||
4-Amino-3-iodo-benzenesulfonamide | Drug Info | [527654] | |||
4-AMINOPHENOL | Drug Info | [529562] | |||
4-Benzythiopyridine-3-sulfonamide | Drug Info | [530766] | |||
4-Ethoxy-3-pyridinesulfonamide | Drug Info | [530766] | |||
4-Hydrazino-3-pyridinesulfonamide | Drug Info | [530766] | |||
4-Hydrazino-benzenesulfonamide | Drug Info | [527654] | |||
4-Methylthiopyridine-3-sulfonamide | Drug Info | [530766] | |||
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 | [527654] | |||
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 | [527654] | |||
Beta-D-Mannose | Drug Info | [551393] | |||
Carzenide | Drug Info | [527654] | |||
CATECHIN | Drug Info | [531068] | |||
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 | [527654] | |||
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] | |||
PARABEN | Drug Info | [530751] | |||
Pentane-1,5-diamine | Drug Info | [530998] | |||
PHENOL | Drug Info | [531068] | |||
Prop-2-ynyl 4-sulfamoylbenzoate | Drug Info | [528574] | |||
RESORCINOL | Drug Info | [529562] | |||
SPERMINE | Drug Info | [530998] | |||
Syringic Acid | Drug Info | [530751] | |||
TRIENTINE | Drug Info | [530998] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Nitrogen metabolism | ||||
Reactome | Reversible hydration of carbon dioxide | ||||
WikiPathways | Reversible Hydration of Carbon Dioxide | ||||
References | |||||
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 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 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 527654 | Bioorg Med Chem Lett. 2005 Sep 1;15(17):3828-33.Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides. | ||||
Ref 528574 | Bioorg 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 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 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 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 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 530766 | Eur 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 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. |
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