CDK4/6 Inhibitors Explored in KRAS-Mutant Cancers

Erin M. Burns, PhD, MSPH
Published: Tuesday, Oct 31, 2017
Geoffrey I. Shapiro, MD, PhD
Geoffrey I. Shapiro, MD, PhD
Although the roles of cyclin-dependent kinases (CDKs) were established more than 20 years ago, early anticancer inhibitors in the class resulted in high toxicity levels. Now, a new generation of more selective inhibitors of CDK4 and CDK6 has entered the clinic in combination therapies for patients with breast cancer.

 

Figure. Relationship of KRAS Signaling to CDKs2

Relationship of KRAS Signaling
Mutations in KRAS are among the earliest and most important drivers of disease progression. When KRAS is mutated, several downstream pathways, such as the MEK/ ERK and PI3K/AKT signaling pathways, become constitutively activated.
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