Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

CA2 (P00918) - Overview - Molecular Target Synopsis

Protein


CA2, Carbonic anhydrase 2
Enzyme Classification 4.2.1.1
UniProt P00918

Also Known as CAH2_HUMAN, CA2

Essential for bone resorption and osteoclast differentiation (By similarity). Reversible hydration of carbon dioxide. Can hydrate cyanamide to urea. Involved in the regulation of fluid secretion into the anterior chamber of the eye. Contributes to intracellular pH regulation in the duodenal upper villous epithelium during proton-coupled peptide absorption. Stimulates the chloride-bicarbonate exchange activity of SLC26A6. Interacts with SLC4A4. Interaction with SLC4A7 regulates SLC4A7 transporter activity. Interacts with SLC26A6 isoform 4 (via C-terminus cytoplasmic domain).

6GM9
HUMAN CARBONIC ANHYDRASE II IN COMPLEX WITH 4-METHYLBENZENESULFONAMIDE
RCSB/PDB
Inspect Structure
See all 3D Structures for CA2

Isoforms / Transcripts (Protein Coding)


Drugs


CA2 is targeted by Approved Drugs Methazolamide, Dichlorphenamide, Omeprazole, Brinzolamide, Ethoxzolamide, Dorzolamide, Acetazolamide. (see details)
Methazolamide
Dichlorphenamide
Omeprazole
Brinzolamide
Ethoxzolamide
Dorzolamide
Acetazolamide

Sub-cellular localization


UniProt: CA2 is active in the following subcellular-locations: cell membrane, cytoplasm.
GO terms: CA2 is active in the following subcellular-locations: apical part of cell, axon, basolateral plasma membrane, cytoplasm, cytosol, extracellular exosome, microvillus, myelin sheath, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CA2 has gain in 14 cell-lines, loss in 4 cell-lines and no signal in 987 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: OVCAR_3, IGROV1, HL_60

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NIH:OVCAR-3, G112, OV-90

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: MCF-7, HMEC, NHEK

(see details)

3D Structures


For CA2 there are:
758 structures (782 chains) solved
551 are solved in complex with at least one small molecule ligand
45 are solved with an approved drug

CA2 is solved in complex with the approved drug(s):

SUC/SUCROSE (4YWP_A),
OSP/SULTHIAME (2Q1Q_A),
CHD/CHOLIC ACID (4N16_A, 4PXX_A),
BZ1/BRINZOLAMIDE (4M2R_A, 4M2V_A, 6BBS_A),
HSM/HISTAMINE (1AVN_A),
EZL/ETHOXZOLAMIDE (3CAJ_A, 3DCW_A, 3DD0_A, 6BCC_A),
CEL/CELECOXIB (1OQ5_A),
HQE/HYDROQUINONE (4E3H_A),
AZM/ACETAZOLAMIDE (1YDA_A, 1YDB_A, 1YDD_A, 1ZSB_A, 2H4N_A, 3DC3_A, 3HS4_A, 3V2J_A, 3V2M_A, 4G0C_A, 4K0S_A, 6QEB_A),
BEZ/BENZOIC ACID (2Q1B_A, 2Q38_A, 3F8E_A, 3FFP_X, 3IEO_A),
ETS/DORZOLAMIDE (1CIL_A, 4K13_A, 4M2U_A, 4M2W_A, 6BC9_A),
TOR/TOPIRAMATE (3HKU_A),
BGC/DEXTROSE (6GDC_A, 6GM9_A),
COX/VALDECOXIB (2AW1_A),
SAL/SALICYLIC ACID (5M78_A),
NIO/NIACIN (6MBV_A),
FUN/FUROSEMIDE (1Z9Y_A),
RCO/RESORCINOL (4E49_A),
I7A/DICHLORPHENAMIDE (2POU_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CA2 has been screened with 8088 compounds (15262 bioactivities), 4746 compounds have bioactivities that show binding affinity of <= 500nM (8466 bioactivities). (see details)