Bookmark and Share
BioAssay: AID 305776

Activation of human recombinant carbonic anhydrase 5A by stopped-flow CO2 hydrase method

The mitochondrial isozymes of human carbonic anhydrase (hCA, EC 4.2.1.1), hCA VA and hCA VB, were investigated for activation with a series of amino acids and amines. D-His, L-DOPA, histamine, dopamine, and 4-(2-aminoethyl)morpholine were excellent hCA VA activators, with KAs in the range of 10-130 nM. Good hCA VB activating effects were identified for L-His, D-Phe, D-DOPA, L-Trp, L-Tyr, more ..
_
   
 Tested Compounds
 Tested Compounds
All(17)
 
 
Active(17)
 
 
 Tested Substances
 Tested Substances
All(17)
 
 
Active(17)
 
 
 Related BioAssays
 Related BioAssays
AID: 305776
Data Source: ChEMBL (453802)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2013-11-19

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Carbonic anhydrase 5A, mitochondrial; AltName: Full=Carbonate dehydratase VA; AltName: Full=Carbonic anhydrase VA; Short=CA-VA; Flags: Precursor
Description ..   
Protein Family: alpha_CA_V
Comment ..   

Gene:CA5A     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 17
Description:
Title: Carbonic anhydrase activators: an activation study of the human mitochondrial isoforms VA and VB with amino acids and amines.

Abstract: The mitochondrial isozymes of human carbonic anhydrase (hCA, EC 4.2.1.1), hCA VA and hCA VB, were investigated for activation with a series of amino acids and amines. D-His, L-DOPA, histamine, dopamine, and 4-(2-aminoethyl)morpholine were excellent hCA VA activators, with KAs in the range of 10-130 nM. Good hCA VB activating effects were identified for L-His, D-Phe, D-DOPA, L-Trp, L-Tyr, serotonin, and 2-(2-aminoethyl)-pyridine, with KAs in the range of 44-110 nM. All these activators enhanced kcat, having no effect on KM, favoring thus the rate-determining step in the catalytic cycle, the proton transfer reactions between the active site and environment. The activation pattern of the two mitochondrial isoforms is very different from each other and as compared to those of the cytosolic isoforms hCA I and II.
(PMID: 17174092)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 11042

ChEMBL Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1KA activity commentKA activity commentString
2KA standard flagKA standard flagInteger
3KA qualifierKA qualifierString
4KA published valueKA published valueFloatμM
5KA standard valueKA standard valueFloatnM

Data Table (Concise)
Classification
PageFrom: