Article

Discovery of cell active macrocyclic peptides with on-target inhibition of KRAS signaling

2021-09-12

Abstract excerpt

RAS is the most commonly mutated oncogene in human cancers and RAS-driven tumors are amongst the most difficult to treat. Historically, discovery of therapeutics targeting this protein has proven challenging due to a lack of deep hydrophobic pockets to which a small molecule might bind. The single such pocket available is normally occupied by GDP or GTP which have millimolar cellular concentrations and picomolar a...

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Identifiers and source

Literature Corpus work: d0748604-9a53-5f6e-aef0-53c87b3b3747
DOI: 10.1101/2021.09.11.459913

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