PubReading [181] - Degraders: The Ultimate Weapon Against Amplified Driver Kinases in Cancer - P. Torres-Ayuso and J. Brognard

<p>Amplification of pro-oncogenic <strong>kinases</strong> is a common genetic alteration driving tumorigenic <strong>phenotypes</strong>. Cancer cells rely on the amplified kinases to sustain cell proliferation, survival, and growth, presenting an opportunity to develop therapies targeting the amplified kinases. Utilizing small molecule catalytic <strong>inhibitors</strong> as therapies to target amplified kinases is plagued by de novo resistance driven by increased expression of the target, and amplified kinases can drive tumorigenic phenotypes independent of catalytic activity. Here, we discuss the emergence of proteolysis-targeting <strong>chimeras</strong> that provide an opportunity to target these oncogenic drivers effectively.</p><p><em>doi.org/10.1124/molpharm.121.000306 - 2022</em></p>