A New Smoothened Antagonist Bearing the Purine Scaffold Shows Antitumour Activity In Vitro and In Vivo

A New Smoothened Antagonist Bearing the Purine Scaffold Shows Antitumour Activity In Vitro and In Vivo

The Smoothened (SMO) receptor is the most druggable target in the Hedgehog (HH) pathway for anticancer compounds. However, SMO antagonists such as vismodegib rapidly develop drug resistance. In this study, new SMO antagonists having the versatile purine ring as a scaffold were designed, synthesised,...

Full description

Bibliographic Details
Main Authors: Ana María Zárate, Christian Espinosa-Bustos, Simón Guerrero, Angélica Fierro, Felipe Oyarzún-Ampuero, Andrew F. G. Quest, Lucia Di Marcotullio, Elena Loricchio, Miriam Caimano, Andrea Calcaterra, Matías González-Quiroz, Adam Aguirre, Jaime Meléndez, Cristian O. Salas
Format: Article
Language:English
Published: MDPI AG 2021-08-01
Series:International Journal of Molecular Sciences
Subjects:
Hedgehog signalling pathway
smoothened receptor antagonists
purine derivatives
docking studies
in vivo assays
Online Access:https://www.mdpi.com/1422-0067/22/16/8372

Internet

https://www.mdpi.com/1422-0067/22/16/8372

Similar Items