Lazaroids U83836E and U74389G are potent, time-dependent inhibitors of caspase-1.
Chem Biol Drug Des
; 86(5): 1049-54, 2015 Nov.
Article
en En
| MEDLINE
| ID: mdl-25871734
ABSTRACT
Caspase-1 is involved in inflammatory processes and is overactive in autoimmunity and autoinflammation. Antioxidant small molecules also play a role in the immune response by decreasing inflammation. An 84-membered library of pro- and antioxidant small molecules was screened for potential inhibitors of caspase-1. Thirteen compounds were discovered to reduce the activity of caspase-1 below 30%. The most potent inhibitors were lazaroid antioxidant molecules, U83836E (B8) and U74389G (B9), displaying apparent Ki values of 48.0 and 50.0 nm, respectively. Both demonstrated a time-dependent and reversible inhibition.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Caspasa 1
/
Bibliotecas de Moléculas Pequeñas
/
Inhibidores de Caspasas
/
Antioxidantes
Límite:
Humans
Idioma:
En
Revista:
Chem Biol Drug Des
Asunto de la revista:
BIOQUIMICA
/
FARMACIA
/
FARMACOLOGIA
Año:
2015
Tipo del documento:
Article
País de afiliación:
Estados Unidos