Design, Synthesis, and Biological Evaluation of Proteolysis-Targeting Chimeras as Highly Selective and Efficient Degraders of Extracellular Signal-Regulated Kinase 5
Pengming Pan,
Tongtong Geng,
Zhongtang Li
et al.
Abstract:Extracellular signal-regulated kinase
5 (ERK5) is recognized as
a key member of the mitogen-activated protein kinase family and is
involved in tumor growth, migration, and angiogenesis. However, the
results of ERK5 inhibition in multiple studies are controversial,
and a highly specific ERK5-targeting agent is required to confirm
physiological functions. Using proteolysis-targeting chimera technology,
we designed the selective ERK5 degrader PPM-3 and examined
its biological effect on cancer cells. Interestingly… Show more
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