ININFA 02677
INSTITUTO DE INVESTIGACIONES FARMACOLOGICAS
Unidad Ejecutora - UE
artículos
Título:
Identification of inhibitors of the RGS homology domain of GRK2 by docking-based virtual screening
Autor/es:
VELEZ RUEDA, ANA JULIA; CABRERA, MAIA; BURGHI, VALERIA; FABIÁN, LUCAS; LORENZANO MENNA, PABLO; FERNÁNDEZ, NATALIA CRISTINA; VELEZ RUEDA, ANA JULIA; CABRERA, MAIA; BURGHI, VALERIA; FABIÁN, LUCAS; LORENZANO MENNA, PABLO; FERNÁNDEZ, NATALIA CRISTINA; ECHEVERRÍA, EMILIANA; JURITZ, EZEQUIEL; DAVIO, CARLOS; ECHEVERRÍA, EMILIANA; JURITZ, EZEQUIEL; DAVIO, CARLOS
Revista:
LIFE SCIENCES
Editorial:
PERGAMON-ELSEVIER SCIENCE LTD
Referencias:
Año: 2019 vol. 239
ISSN:
0024-3205
Resumen:
G protein-coupled receptor (GPCR) kinases (GRKs) are mainly involved in the desensitization of GPCRs. Among them, GRK2 has been described to be upregulated in many pathological conditions and its crucial role in cardiac hypertrophy, hypertension, and heart failure promoted the search for pharmacological inhibitors of its activity. There have been several reports of potent and selective inhibitors of GRK2, most of them directed to the kinase domain of the protein. However, the homologous to the regulator of G protein signaling (RH) domain of GRK2 has also been shown to regulate GPCRs signaling. Herein, we searched for potential inhibitors of receptor desensitization mediated by RH domain of GRK2.
