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carbonic anhydrase 14

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Target not currently curated in GtoImmuPdb

Target id: 2598

Nomenclature: carbonic anhydrase 14

Abbreviated Name: CA XIV

Family: Carbonic anhydrases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 337 1q21.2 CA14 carbonic anhydrase 14
Mouse 1 337 3 F2.1 Car14 carbonic anhydrase 14
Rat 1 337 2q34 Ca14 carbonic anhydrase 14
Previous and Unofficial Names Click here for help
carbonic anhydrase XIV | Car14
Database Links Click here for help
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
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Pharos
RefSeq Nucleotide
RefSeq Protein
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Enzyme Reaction Click here for help
EC Number: 4.2.1.1

Download all structure-activity data for this target as a CSV file go icon to follow link

Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
L-histidine Small molecule or natural product Click here for species-specific activity table Hs Activation - - 7
[7]
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
dorzolamide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pKi 3
pKi 7.8 (Ki 1.5x10-8 M) [3]
ethoxzolamide Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 pKi 4
pKi 7.6 (Ki 2.5x10-8 M) [4]
methazolamide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.6 pKi 4
pKi 7.6 (Ki 2.7x10-8 M) [4]
acetazolamide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure 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 Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 5.4 pKi 6
pKi 5.4 (Ki 4.13x10-6 M) [6]
brinzolamide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure 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]

7. Temperini C, Scozzafava A, Vullo D, Supuran CT. (2006) Carbonic anhydrase activators. Activation of isozymes I, II, IV, VA, VII, and XIV with l- and d-histidine and crystallographic analysis of their adducts with isoform II: engineering proton-transfer processes within the active site of an enzyme. Chemistry, 12 (27): 7057-66. [PMID:16807956]

How to cite this page

Carbonic anhydrases: carbonic anhydrase 14. Last modified on 25/07/2019. Accessed on 27/11/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2598.