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carbonic anhydrase 9

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Target not currently curated in GtoImmuPdb

Target id: 3055

Nomenclature: carbonic anhydrase 9

Abbreviated Name: CA IX

Family: Carbonic anhydrases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 459 9p13.3 CA9 carbonic anhydrase 9 3-4
Mouse 1 437 4 A5 Car9 carbonic anhydrase 9
Rat 1 437 5q22 Ca9 carbonic anhydrase 9
Previous and Unofficial Names Click here for help
Car9 | CAIX | carbonic anhydrase IX
Database Links Click here for help
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 4.2.1.1
Description Reaction Reference
Reversible hydration of gaseous CO2 to carbonic acid H(2)CO(3) <=> CO(2) + H(2)O

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
SLC-0111 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pKi 2
pKi 7.3 (Ki 4.5x10-8 M) [2]
compound 5a [PMID: 31287314] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pKi 1
pKi 6.4 (Ki 4.159x10-7 M) [1]
compound 5b [PMID: 31287314] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition <5.0 pKi 1
pKi <5.0 (Ki >1x10-5 M) [1]
Tissue Distribution Comments
CA IX is one of two known tumour-associated carbonic anhydrase isoenzymes, the other being CA XII, where it is associated with cell proliferation, transformation and metastasis. It is not detected in most normal tissues.
General Comments
CA IX is a membrane anchored carbonic anhydrase, and is one of two known tumour-associated carbonic anhydrase isoenzymes, the other being CA XII. Its activity in the hypoxic tumour microenvironment is associated with mechanisms that support cell proliferation, transformation and metastasis.

References

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1. Berrino E, Milazzo L, Micheli L, Vullo D, Angeli A, Bozdag M, Nocentini A, Menicatti M, Bartolucci G, di Cesare Mannelli L et al.. (2019) Synthesis and Evaluation of Carbonic Anhydrase Inhibitors with Carbon Monoxide Releasing Properties for the Management of Rheumatoid Arthritis. J. Med. Chem., 62 (15): 7233-7249. [PMID:31287314]

2. Congiu C, Onnis V, Deplano A, Balboni G, Dedeoglu N, Supuran CT. (2015) Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity. Bioorg. Med. Chem. Lett., 25 (18): 3850-3. [PMID:26233435]

3. Nakagawa Y, Uemura H, Hirao Y, Yoshida K, Saga S, Yoshikawa K. (1998) Radiation hybrid mapping of the human MN/CA9 locus to chromosome band 9p12-p13. Genomics, 53 (1): 118-9. [PMID:9787087]

4. Opavský R, Pastoreková S, Zelník V, Gibadulinová A, Stanbridge EJ, Závada J, Kettmann R, Pastorek J. (1996) Human MN/CA9 gene, a novel member of the carbonic anhydrase family: structure and exon to protein domain relationships. Genomics, 33 (3): 480-7. [PMID:8661007]

How to cite this page

Carbonic anhydrases: carbonic anhydrase 9. Last modified on 24/07/2019. Accessed on 27/11/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3055.