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BioAssay: AID 587132

Inhibition of Leptonychotes weddellii alpha-carbonic anhydrase after 15 mins by CO2 hydrase assay at pH 7.5

A high activity alpha-carbonic anhydrase (CA, EC 4.2.1.1) has been purified from various tissues of the Antarctic seal Leptonychotes weddellii. The new enzyme, denominated lwCA, has a catalytic activity for the physiologic CO(2) hydration to bicarbonate reaction, similar to that of the high activity human isoform hCA II, with a k(cat) of 1.1#10(6) s(-1), and a k(cat)/K(m) of 1.4#10(8) M(-1) more ..
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 Tested Compounds
 Tested Compounds
All(28)
 
 
Active(10)
 
 
Unspecified(18)
 
 
 Tested Substances
 Tested Substances
All(28)
 
 
Active(10)
 
 
Unspecified(18)
 
 
 Related BioAssays
 Related BioAssays
AID: 587132
Data Source: ChEMBL (735672)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2011-09-18
Modify Date: 2014-05-27

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 10
Description:
Title: Purification and inhibition studies with anions and sulfonamides of an alpha-carbonic anhydrase from the Antarctic seal Leptonychotes weddellii.

Abstract: A high activity alpha-carbonic anhydrase (CA, EC 4.2.1.1) has been purified from various tissues of the Antarctic seal Leptonychotes weddellii. The new enzyme, denominated lwCA, has a catalytic activity for the physiologic CO(2) hydration to bicarbonate reaction, similar to that of the high activity human isoform hCA II, with a k(cat) of 1.1#10(6) s(-1), and a k(cat)/K(m) of 1.4#10(8) M(-1) s(-1). The enzyme was highly inhibited by cyanate, thiocyanate, cyanide, bicarbonate, carbonate, as well as sulfamide, sulfamate, phenylboronic/phenylarsonic acids (K(I)s in the range of 46-100 muM). Many clinically used sulfonamides, such as acetazolamide, methazolamide, dorzolamide, brinzolamide and benzolamide were low nanomolar inhibitors, with K(I)s in the range of 5.7-67 nM. Dichlorophenamide, zonisamide, saccharin and hydrochlorothiazide were weaker inhibitors, with K(I)s in the range of 513-5390 nM. The inhibition profile with anions and sulfonamides of the seal enzyme was rather different from those of the human isoforms hCA I and II. The high sensitivity to bicarbonate inhibition of lwCA, unlike that of the human enzymes, may reflect an evolutionary adaptation to the deep water, high CO(2) partial pressure and hypoxic conditions in which Weddell seals spend much of their life.
(PMID: 21377369)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Putative Target:
ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Binding
Assay Data Source: Scientific Literature
Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ki*Ki PubChem standard valueFloatμM
2Ki activity commentKi activity commentString
3Ki standard flagKi standard flagInteger
4Ki qualifierKi qualifierString
5Ki published valueKi published valueFloatmM
6Ki standard valueKi standard valueFloatnM
7Ki data validityKi data validityString
8Ki activity commentKi activity commentString
9Ki standard flagKi standard flagInteger
10Ki qualifierKi qualifierString
11Ki published valueKi published valueFloatnM
12Ki standard valueKi standard valueFloatnM
13Ki data validityKi data validityString

* Activity Concentration.

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