Synthesis of novel phosphonic-type activity-based probes for neutrophil serine proteases and their application in spleen lysates of different organisms.
Chembiochem
; 15(17): 2605-12, 2014 Nov 24.
Article
em En
| MEDLINE
| ID: mdl-25236966
ABSTRACT
Neutrophils are a type of granulocyte important in the "first line of defense" of the innate immune system. Upon activation, they facilitate the destruction of invading microorganisms by the production of superoxide radicals, as well as the release of the enzymatic contents of their lysozymes. These enzymes include specific serine proteases cathepsin G, neutrophil elastase, proteinase 3, as well as the recently discovered neutrophil serine protease 4 (NSP4). Under normal conditions, the proteolytic activity of neutrophil proteases is tightly regulated by endogenous serpins; however, this mechanism can be subverted during tissue stress, thereby resulting in the uncontrolled activity of serine proteases, which induce chronic inflammation and subsequent pathology. Herein, we describe the development of low-molecular-weight activity-based probes that specifically target the active sites of neutrophil proteases.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ácidos Fosforosos
/
Baço
/
Extratos de Tecidos
/
Sondas Moleculares
/
Inibidores de Proteínas Quinases
/
Serina Proteases
/
Neutrófilos
Limite:
Humans
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article