Target Information
| Target General Information | Top | |||||
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| Target ID |
T37541
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| Target Name |
Carbonic anhydrase VII (CA-VII)
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| Synonyms |
Carbonic anhydrase 7; Carbonate dehydratase VII
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| Gene Name |
CA7
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| Target Type |
Patented-recorded target
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[1] | ||||
| Function |
Reversible hydration of carbon dioxide.
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| BioChemical Class |
Alpha-carbonic anhydrase
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| UniProt ID | ||||||
| EC Number |
EC 4.2.1.1
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| Sequence |
MTGHHGWGYGQDDGPSHWHKLYPIAQGDRQSPINIISSQAVYSPSLQPLELSYEACMSLS
ITNNGHSVQVDFNDSDDRTVVTGGPLEGPYRLKQFHFHWGKKHDVGSEHTVDGKSFPSEL HLVHWNAKKYSTFGEAASAPDGLAVVGVFLETGDEHPSMNRLTDALYMVRFKGTKAQFSC FNPKCLLPASRHYWTYPGSLTTPPLSESVTWIVLREPICISERQMGKFRSLLFTSEDDER IHMVNNFRPPQPLKGRVVKASFRA Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T74SFH | |||||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Acetazolamide | Ligand Info | |||||
| Structure Description | Crystal structure of the C183S/C217S mutant of human CA VII in complex with acetazolamide | PDB:3ML5 | ||||
| Method | X-ray diffraction | Resolution | 2.05 Å | Mutation | Yes | [2] |
| PDB Sequence |
GHHGWGYGQD
10 DGPSHWHKLY20 PIAQGDRQSP30 INIISSQAVY40 SPSLQPLELS50 YEACMSLSIT 60 NNGHSVQVDF70 NDSDDRTVVT80 GGPLEGPYRL90 KQFHFHWGKK100 HDVGSEHTVD 110 GKSFPSELHL120 VHWNAKKYST130 FGEAASAPDG140 LAVVGVFLET150 GDEHPSMNRL 160 TDALYMVRFK170 GTKAQFSCFN180 PKSLLPASRH190 YWTYPGSLTT200 PPLSESVTWI 210 VLREPISISE220 RQMGKFRSLL230 FTSEDDERIH240 MVNNFRPPQP250 LKGRVVKASF 260 RA
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| Ligand Name: Ethoxzolamide | Ligand Info | |||||
| Structure Description | Crystal Structure of Human Carbonic Anhydrase VII [isoform 1], CA7 | PDB:3MDZ | ||||
| Method | X-ray diffraction | Resolution | 2.32 Å | Mutation | No | [3] |
| PDB Sequence |
MHGWGYGQDD
13 GPSHWHKLYP23 IAQGDRQSPI33 NIISSQAVYS43 PSLQPLELSY53 EACMSLSITN 63 NGHSVQVDFN73 DSDDRTVVTG83 GPLEGPYRLK93 QFHFHWGKKH103 DVGSEHTVDG 113 KSFPSELHLV123 HWNAKKYSTF133 GEAASAPDGL143 AVVGVFLETG153 DEHPSMNRLT 163 DALYMVRFKG173 TKAQFSCFNP183 KCLLPASRHY193 WTYPGSLTTP203 PLSESVTWIV 213 LREPICISER223 QMGKFRSLLF233 TSEDDERIHM243 VNNFRPPQPL253 KGRVVKASF |
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| Nitrogen metabolism | hsa00910 | Affiliated Target |
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| Class: Metabolism => Energy metabolism | Pathway Hierarchy | ||
| Chemical Structure based Activity Landscape of Target | Top |
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| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| References | Top | |||||
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| REF 1 | Carbonic anhydrase inhibitors as antitumor/antimetastatic agents: a patent review (2008-2018).Expert Opin Ther Pat. 2018 Oct;28(10):729-740. | |||||
| REF 2 | Crystal structure of the C183S/C217S mutant of human CA VII in complex with acetazolamide. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5023-6. | |||||
| REF 3 | Crystal Structure of Human Carbonic Anhydrase VII [isoform 1], CA7 | |||||
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