carbonic anhydrase 14

Target id: 2598

Nomenclature: carbonic anhydrase 14

Family: 4.2.1.1 Carbonate dehydratases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for carbonic anhydrase 14 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 337 1q21 CA14 carbonic anhydrase 14
Mouse - 337 3 F2.1 Car14 carbonic anhydrase 14
Rat - 337 2 Car14 carbonic anhydrase 14
Previous and Unofficial Names
carbonic anhydrase XIV
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
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Enzyme Reaction
EC Number: 4.2.1.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
dorzolamide Hs Inhibition 7.8 pKi 3
pKi 7.8 (Ki 1.5x10-8 M) [3]
ethoxzolamide Hs Inhibition 7.6 pKi 4
pKi 7.6 (Ki 2.5x10-8 M) [4]
methazolamide Hs Inhibition 7.6 pKi 4
pKi 7.6 (Ki 2.7x10-8 M) [4]
acetazolamide Hs Inhibition 7.4 – 7.6 pKi 1-2
pKi 7.4 – 7.6 (Ki 4.1x10-8 – 2.5x10-8 M) [1-2]
chlorthalidone Hs Inhibition 5.4 pKi 6
pKi 5.4 (Ki 4.13x10-6 M) [6]
brinzolamide Hs Inhibition 4.2 pKi 5
pKi 4.2 (Ki 7x10-5 M) [5]
Inhibitor Comments
Acetazolamide inhibits carbonic anhydrases I, IV and XIV, but has 10-fold lower affinity for XIV.
Methazolamide inhibits carbonic anhydrases I, IV and XIV with similar affinity.
Chlorthalidone is an approved drug inhibitor of carbonic anhydrase activity. We have tagged CA VII and XII as the primary targets for this drug as affinity is highest at these two isozymes [6]. .

References

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1. Avvaru BS, Wagner JM, Maresca A, Scozzafava A, Robbins AH, Supuran CT, McKenna R. (2010) Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. Bioorg. Med. Chem. Lett.20 (15): 4376-81. [PMID:20605094]

2. Garaj V, Puccetti L, Fasolis G, Winum JY, Montero JL, Scozzafava A, Vullo D, Innocenti A, Supuran CT. (2004) Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties. Bioorg. Med. Chem. Lett.14 (21): 5427-33. [PMID:15454239]

3. Innocenti A, Firnges MA, Antel J, Wurl M, Scozzafava A, Supuran CT. (2005) Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides. Bioorg. Med. Chem. Lett.15 (4): 1149-54. [PMID:15686931]

4. Nishimori I, Vullo D, Innocenti A, Scozzafava A, Mastrolorenzo A, Supuran CT. (2005) Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides. Bioorg. Med. Chem. Lett.15 (17): 3828-33. [PMID:16039848]

5. Parr JS, Khalifah RG. (1992) Inhibition of carbonic anhydrases I and II by N-unsubstituted carbamate esters. J. Biol. Chem.267 (35): 25044-50. [PMID:1460006]

6. Temperini C, Cecchi A, Scozzafava A, Supuran CT. (2009) Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference. Bioorg. Med. Chem.17 (3): 1214-21. [PMID:19119014]

How to cite this page

4.2.1.1 Carbonate dehydratases: carbonic anhydrase 14. Last modified on 30/03/2016. Accessed on 17/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2598.