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BioAssay: AID 464319

Activation of human recombinant carbonic anhydrase isoenzyme 2 by stopped flow CO2 hydration method

The protein encoded by the NCE103 gene of Candida glabrata, a beta-carbonic anhydrase (CA, EC 4.2.1.1) designated as CgCA, was investigated for its activation with amines and amino acids. CgCA was weakly activated by amino acids such as l-/d-His, l-Phe, l-DOPA, and l-Trp and by histamine or dopamine (K(A)s of 21.2-37microM) but more effectively activated by d-Phe, d-DOPA, d-Trp as well as more ..
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 Tested Compounds
 Tested Compounds
All(19)
 
 
Active(16)
 
 
Unspecified(3)
 
 
 Tested Substances
 Tested Substances
All(19)
 
 
Active(16)
 
 
Unspecified(3)
 
 
AID: 464319
Data Source: ChEMBL (615182)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-09-27
Modify Date: 2014-08-25

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Carbonic anhydrase 2; AltName: Full=Carbonate dehydratase II; AltName: Full=Carbonic anhydrase C; Short=CAC; AltName: Full=Carbonic anhydrase II; Short=CA-II
Description ..   
Protein Family: alpha_CA_I_II_III_XIII
Comment ..   

Gene:CA2     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 16
Description:
Title: Carbonic anhydrase activators: Activation of the beta-carbonic anhydrase from the pathogenic yeast Candida glabrata with amines and amino acids.

Abstract: The protein encoded by the NCE103 gene of Candida glabrata, a beta-carbonic anhydrase (CA, EC 4.2.1.1) designated as CgCA, was investigated for its activation with amines and amino acids. CgCA was weakly activated by amino acids such as l-/d-His, l-Phe, l-DOPA, and l-Trp and by histamine or dopamine (K(A)s of 21.2-37microM) but more effectively activated by d-Phe, d-DOPA, d-Trp as well as serotonin, pyridyl-alkylamines, aminoethyl-piperazine/morpholine (K(A)s of 10.1-16.7microM). The best activators were l-/d-Tyr, with activation constants of 7.1-9.5microM. This study may bring a better understanding of the catalytic/activation mechanisms of beta-CAs from pathogenic fungi.
(PMID: 20129782)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Protein Target Class: enzyme lyase
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 valueFloatμM

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
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