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Furthermore, a covalent binding mode enabled inhibition of challenging targets for which noncovalent inhibitors could not successfully be developed, as illustrated by two recently approved first-in-class drugs: sotorasib (AMG 510) modifies Cys12 in the oncogenic KRAS G12C mutant [18] and mobocertinib (TAK788) modifies noncatalytic Cys797 of the EGFR ex20ins mutant [19]
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Coyne MJ, Reeves NC, Rosen DK (1997): Estimated prevalence of injection-site sarcomas in cats during 1992
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