Synthesis and Biological Activity of a VHL-Based PROTAC Specific for p38α

Synthesis and Biological Activity of a VHL-Based PROTAC Specific for p38α

We report a series of small molecule proteolysis-targeting chimeras (PROTACs) that target the protein kinase p38α for degradation. These PROTACs are based on a ligand of the VHL E3 ubiquitin ligase, which is linked to an ATP competitive inhibitor of p38α. We provide evidence that these compounds can...

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Bibliographic Details
Main Authors: Mónica Cubillos-Rojas, Guillem Loren, Yusuf Z. Hakim, Xavier Verdaguer, Antoni Riera, Angel R. Nebreda
Format: Article
Language:English
Published: MDPI AG 2023-01-01
Series:Cancers
Subjects:
p38 MAPK
PROTAC
protein degradation
VHL
Online Access:https://www.mdpi.com/2072-6694/15/3/611

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