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BioAssay: AID 458784

Activation of Candida albicans beta-carbonic anhydrase Nce103 by stopped flow CO2 hydration assay

The proteins encoded by the Nce103 genes of Candida albicans and Cryptococcus neoformans are catalytically active beta-carbonic anhydrases (CAs, EC 4.2.1.1) playing various roles in the life cycle of these fungal pathogens, such as CO(2) sensing, regulation of capsule biosynthesis, filamentation, and adaptation of the organism to various pH and CO(2) conditions in various niches where the fungi more ..
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 Tested Compounds
 Tested Compounds
All(18)
 
 
Active(18)
 
 
 Tested Substances
 Tested Substances
All(18)
 
 
Active(18)
 
 
AID: 458784
Data Source: ChEMBL (609842)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-07-30
Modify Date: 2014-05-26

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Carbonic anhydrase; AltName: Full=Carbonate dehydratase; AltName: Full=Non-classical export protein 103
Description ..   
Protein Family: beta_CA_cladeA
Comment ..   

Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 18
Description:
Title: Carbonic anhydrase activators: activation of the beta-carbonic anhydrases from the pathogenic fungi Candida albicans and Cryptococcus neoformans with amines and amino acids.

Abstract: The proteins encoded by the Nce103 genes of Candida albicans and Cryptococcus neoformans are catalytically active beta-carbonic anhydrases (CAs, EC 4.2.1.1) playing various roles in the life cycle of these fungal pathogens, such as CO(2) sensing, regulation of capsule biosynthesis, filamentation, and adaptation of the organism to various pH and CO(2) conditions in various niches where the fungi grow. Here, we report the first activation study of these two enzymes, CaNce103 and Can2, respectively, with amines and amino acids. The C. albicans enzyme, CaNce103 was activated by amino acids such as L-/D-His, L-D-Trp, L-Tyr with K(A)s in the range of 19.5-46 microM. More effective activators were some amines such as histamine, dopamine, 2-aminoethyl-piperazine, and L-adrenaline (K(A)s of 13.2-18.5 microM). The best CaNce103 activators were L- and D-Dopa, with K(A)s of 0.96-2.5 microM. The C. neoformans enzyme, Can2, showed much lower propensity to be activated by all these amino acids and amines, which had activation constants in the range of 28.7-47.2 microM. The best Can2 activator was L-Trp. This study may help to better understand the catalytic/activation mechanisms of the beta-CAs and eventually to design CA activity modulators of such widespread enzymes in pathogenic fungi.
(PMID: 20061162)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

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 valueFloatμM

Data Table (Concise)
Classification
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