A new small molecule inhibitor of soluble guanylate cyclase.
Bioorg Med Chem
; 23(17): 5303-10, 2015 Sep 01.
Article
en En
| MEDLINE
| ID: mdl-26264842
Soluble guanylate cyclase (sGC) is a haem containing enzyme that regulates cardiovascular homeostasis and multiple mechanisms in the central and peripheral nervous system. Commonly used inhibitors of sGC activity act through oxidation of the haem moiety, however they also bind haemoglobin and this limits their bioavailability for in vivo studies. We have discovered a new class of small molecule inhibitors of sGC and have characterised a compound designated D12 (compound 10) which binds to the catalytic domain of the enzyme with a KD of 11 µM in a SPR assay.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Quinoxalinas
/
Receptores Citoplasmáticos y Nucleares
/
Activadores de Enzimas
/
Bibliotecas de Moléculas Pequeñas
/
Guanilato Ciclasa
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2015
Tipo del documento:
Article
País de afiliación:
Reino Unido
Pais de publicación:
Reino Unido