Target Information

Target General Infomation
Target ID
T06569
Former ID
TTDR00210
Target Name
Carbonic anhydrase VI
Gene Name
CA6
Synonyms
CA-VI; Carbonate dehydratase VI; Salivary carbonic anhydrase; Secreted carbonic anhydrase; CA6
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. Its role in saliva is unknown.
BioChemical Class
Carbon-oxygen lyases
Target Validation
T06569
UniProt ID
P23280
EC Number
EC 4.2.1.1
Sequence
MRALVLLLSLFLLGGQAQHVSDWTYSEGALDEAHWPQHYPACGGQRQSPINLQRTKVRYN
PSLKGLNMTGYETQAGEFPMVNNGHTVQISLPSTMRMTVADGTVYIAQQMHFHWGGASSE
ISGSEHTVDGIRHVIEIHIVHYNSKYKSYDIAQDAPDGLAVLAAFVEVKNYPENTYYSNF
ISHLANIKYPGQRTTLTGLDVQDMLPRNLQHYYTYHGSLTTPPCTENVHWFVLADFVKLS
RTQVWKLENSLLDHRNKTIHNDYRRTQPLNHRVVESNFPNQEYTLGSEFQFYLHKIEEIL
DYLRRALN
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]
COUMATE Drug Info Phase 2 Breast cancer [531371]
SPERMINE Drug Info Terminated Discovery agent [542107], [546483]
Inhibitor 2,4-Disulfamyltrifluoromethylaniline Drug Info [529948]
2-Amino-benzenesulfonamide Drug Info [529948]
2-hydrazinylbenzenesulfonamide Drug Info [529948]
4-(2-aminopyrimidin-4-ylamino)benzenesulfonamide Drug Info [529948]
4-(2-Hydroxy-ethyl)-benzenesulfonamide Drug Info [529948]
4-(hydroxymethyl)benzenesulfonamide Drug Info [529948]
4-Amino-3-bromo-benzenesulfonamide Drug Info [529948]
4-Amino-3-chloro-benzenesulfonamide Drug Info [529948]
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-CYANOPHENOL Drug Info [529562]
4-Hydrazino-benzenesulfonamide Drug Info [529948]
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]
7-butoxy-2H-chromen-2-one Drug Info [530514]
7-propoxy-2H-chromen-2-one Drug Info [530514]
BENZOLAMIDE Drug Info [529948]
Carzenide Drug Info [529948]
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]
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]
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]
PARABEN Drug Info [530751]
Pentane-1,5-diamine Drug Info [530998]
SALICYLATE Drug Info [529562]
SPERMINE Drug Info [530998]
Syringic Acid Drug Info [530751]
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 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 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 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 546483Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008464)
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 529948J 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 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 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 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.

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