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carbonic anhydrase 7

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Target not currently curated in GtoImmuPdb

Target id: 2749

Nomenclature: carbonic anhydrase 7

Abbreviated Name: CA VII

Family: Carbonic anhydrases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 264 16q22.1 CA7 carbonic anhydrase 7
Mouse - 264 8 D3 Car7 carbonic anhydrase 7
Rat - 264 19p14 Car7 carbonic anhydrase 7
Previous and Unofficial Names Click here for help
carbonic anhydrase VII
Database Links Click here for help
Alphafold P43166 (Hs), Q9ERQ8 (Mm)
BRENDA 4.2.1.1
CATH/Gene3D 3.10.200.10
ChEMBL Target CHEMBL2326 (Hs), CHEMBL2216 (Mm)
DrugBank Target P43166 (Hs)
Ensembl Gene ENSG00000168748 (Hs), ENSMUSG00000031883 (Mm), ENSRNOG00000012371 (Rn)
Entrez Gene 766 (Hs), 12354 (Mm), 291819 (Rn)
Human Protein Atlas ENSG00000168748 (Hs)
KEGG Enzyme 4.2.1.1
KEGG Gene hsa:766 (Hs), mmu:12354 (Mm), rno:291819 (Rn)
OMIM 114770 (Hs)
Pharos P43166 (Hs)
RefSeq Nucleotide NM_005182 (Hs), NM_053070 (Mm), NM_001106165 (Rn)
RefSeq Protein NP_005173 (Hs), NP_444300 (Mm), NP_001099635 (Rn)
SynPHARM 79197 (in complex with acetazolamide)
79201 (in complex with ethoxzolamide)
UniProtKB P43166 (Hs), Q9ERQ8 (Mm)
Wikipedia CA7 (Hs)
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
histamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Activation - - 4
⤷ KA 37500 nM. [4]
L-histidine Small molecule or natural product Click here for species-specific activity table Hs Activation - - 6
⤷ [6]
amphetamine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Activation - - 4
⤷ KA 910 nM. [4]
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
ethoxzolamide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.1 pKi 3
⤷ pKi 9.1 (Ki 8x10-10 M) [3]
topiramate Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.1 pKi 3
⤷ pKi 9.1 (Ki 9x10-10 M) [3]
methazolamide Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.7 pKi 3
⤷ pKi 8.7 (Ki 2.1x10-9 M) [3]
acetazolamide 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 8.6 pKi 1
⤷ pKi 8.6 (Ki 2.5x10-9 M) [1]
brinzolamide 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 8.6 pKi 3
⤷ pKi 8.6 (Ki 2.8x10-9 M) [3]
chlorthalidone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.6 pKi 5
⤷ pKi 8.6 (Ki 2.8x10-9 M) [5]
dorzolamide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pKi 3
⤷ pKi 8.5 (Ki 3.5x10-9 M) [3]
salvianolic acid A Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.2 pKi 2
⤷ pKi 7.2 (Ki 7.14x10-8 M) [2]
zonisamide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.9 pKi 3
⤷ pKi 6.9 (Ki 1.17x10-7 M) [3]
indisulam Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.9 pKi 3
⤷ pKi 6.9 (Ki 1.22x10-7 M) [3]
sulpiride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 5.4 pKi 3
⤷ pKi 5.4 (Ki 3.63x10-6 M) [3]
Inhibitor Comments
Carbonic anhydrase (CA) inhibitors are active over a number of CA isozymes. We tag those isozymes with the highest drug affinity as the primary molecular target of each of the drugs, with the caveat that the drugs interact with other CA isozymes.

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. Karioti A, Ceruso M, Carta F, Bilia AR, Supuran CT. (2015) New natural product carbonic anhydrase inhibitors incorporating phenol moieties. Bioorg Med Chem, 23 (22): 7219-25. [PMID:26498393]

3. Sethi KK, Vullo D, Verma SM, Tanç M, Carta F, Supuran CT. (2013) Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety. Bioorg Med Chem, 21 (19): 5973-82. [PMID:23965175]

4. Tanini D, Capperucci A, Supuran CT, Angeli A. (2019) Sulfur, selenium and tellurium containing amines act as effective carbonic anhydrase activators. Bioorg Chem, 87: 516-522. [PMID:30928874]

5. 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]

6. 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 7. Last modified on 16/01/2024. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2749.