AI & the Hunt for the Holy Grail of Cancer Targets
<p>The human mutant K-Ras protein, long considered the ‘holy grail’ of cancer targets, is implicated in about 30% of all human cancers, acting much like a central on-off switch. Despite extensive research, it earned the label of being “undruggable” due to daunting challenges related to its structure and biological functions.</p>
<p>Targeting the enzyme’s active site, which binds GTP, proved to be one such obstacle. Many similar enzymes are involved in essential cellular processes, and the enzyme binds its natural substrate, GTP, very tightly so it is challenging to compete it out with inhibitors. Additionally, it is crucial for any effective cancer treatment to selectively inhibit the mutated, overactive form of K-Ras without affecting the non-mutated form, which plays vital roles in healthy tissues.</p>
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