Inhibitor
A drug that blocks a specific protein from doing its job, usually by lodging in the pocket the protein needs to work. Most targeted cancer drugs are named after what they inhibit.
Inhibitors can bind reversibly (competing with the natural substrate) or irreversibly (forming a permanent bond, as afatinib does with EGFR), and can bind the active site or a separate pocket that distorts the protein (allosteric inhibition, as sotorasib does with KRAS G12C). The name usually tells you the target: PARP inhibitor, CDK4/6 inhibitor, checkpoint inhibitor, aromatase inhibitor. Because inhibitors only block rather than remove a protein, the cell can escape by making more of it, mutating the pocket, or rerouting the signal; degraders, which destroy the protein, are one answer.
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not linked directly; found by shared links- TermHormone therapy
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- Key paperCodeBreaK 200: sotorasib versus docetaxel in KRAS G12C-mutated lung cancer, a modest win for the first KRAS drug
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- PersonKevan M. Shokat
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- TermProtein
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Shares Sotorasib, KRAS & RAS inhibitors, Drug resistance (primary and acquired).