Discovery of an orally active VHL-recruiting PROTAC that achieves robust HMGCR degradation and potent hypolipidemic activity in vivo.
Acta Pharm Sin B
; 11(5): 1300-1314, 2021 May.
Article
em En
| MEDLINE
| ID: mdl-34094835
CRBN, cereblon; CVD, cardiovascular disease; Cholesterol reduction; DC50, half degradation concentration; ER, endoplasmic reticulum; H&E, hematoxylin/eosin; HDAC, histone deacetylase; HMGCR; HMGCR, 3-hydroxy-3-methylglutaryl coenzyme A reductase; LDL-C, low-density lipoprotein cholesterol; MFD, medium fat diet; ORO, oil-red O; Oral bioavailability; PK, pharmacokinetic; PROTAC, proteolysis-targeting chimera; PROTACs; SAR, structureactivity relationship; TC, total cholesterol; TG, triglyceride; VHL, von Hippel-Lindau
Texto completo:
1
Base de dados:
MEDLINE
Tipo de estudo:
Guideline
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article