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BioAssay: AID 375786

Activation of human recombinant carbonic anhydrase 4 lacking 20 amino terminal residues by stopped-flow CO2 hydrase method

An activation study of the membrane-associated carbonic anhydrase (CA, EC 4.2.1.1) isoform XV with a series of natural and non-natural amino acids and aromatic/heterocyclic amines is reported. Murine CA XV was strongly activated by some amino acids (d-Phe, l-/d-DOPA, d-Trp, l-Tyr) and amines (dopamine, serotonin, l-adrenaline and 4-(2-aminoethyl)-morpholine) with activation constants in the range more ..
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 Tested Compounds
 Tested Compounds
All(18)
 
 
Active(18)
 
 
 Tested Substances
 Tested Substances
All(18)
 
 
Active(18)
 
 
AID: 375786
Data Source: ChEMBL (523815)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-08-23

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Carbonic anhydrase 4; AltName: Full=Carbonate dehydratase IV; AltName: Full=Carbonic anhydrase IV; Short=CA-IV; Flags: Precursor
Description ..   
Protein Family: alpha_CA_IV_XV_like
Comment ..   

Gene:CA4     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 18
Description:
Title: Carbonic anhydrase activators. Activation of the membrane-associated isoform XV with amino acids and amines.

Abstract: An activation study of the membrane-associated carbonic anhydrase (CA, EC 4.2.1.1) isoform XV with a series of natural and non-natural amino acids and aromatic/heterocyclic amines is reported. Murine CA XV was strongly activated by some amino acids (d-Phe, l-/d-DOPA, d-Trp, l-Tyr) and amines (dopamine, serotonin, l-adrenaline and 4-(2-aminoethyl)-morpholine) with activation constants in the range of 4.0-9.5muM. l-/d-His, l-Phe, histamine and several other heterocyclic amines showed less efficient activation (K(A)s in the range of 11.6-33.4muM). The activation profile of CA XV is quite different from that of the cytosolic isoforms CA I and II or the membrane-associated CA IV. All mammalian isoforms CA I-XV are thus characterized for their interaction with this set of amino acid and amine activators, some of which are biogenic amines or neurotransmitters present in sufficiently high amounts in various tissues for exerting significant biologic responses.
(PMID: 19464888)
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 valueFloatnM

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