Digestive lipases: inactivation by phosphonates.
Biochim Biophys Acta
; 1210(2): 157-66, 1994 Jan 03.
Article
em En
| MEDLINE
| ID: mdl-8280765
ABSTRACT
Phosphonates mimicking the transition state which occurs during carboxyester hydrolysis were synthesized and investigated as potential inactivators of human pancreatic (HPL) and gastric (HGL) lipases. Their efficiency as inactivators was studied on the basis of the alkyl chain length, the nature of the leaving group and the influence of the ester substituent. In each case, HGL was found to be more sensitive than HPL towards these phosphonates. The released p-nitrophenol to enzyme ratio indicates that a 11 complex was formed. In the absence of substrate, the most powerful inactivator was O-methyl O-(p-nitrophenyl) n-pentylphosphonate (4A), which has a short alkyl chain, a small methoxy substituent and a good leaving group.
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Base de dados:
MEDLINE
Assunto principal:
Compostos Organofosforados
/
Lipase
/
Nitrofenóis
Limite:
Humans
Idioma:
En
Ano de publicação:
1994
Tipo de documento:
Article