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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.
Showing the molecule this term concerns: Sotorasib.
Shares Palbociclib, CDK4/6 inhibitors, PROTACs & molecular glues (targeted protein degradation).
Shares Palbociclib, CDK4/6 inhibitors, Small-molecule kinase inhibitors.
Shares Targeted therapy, PROTACs & molecular glues (targeted protein degradation), Olaparib, Small-molecule kinase inhibitors.
Shares Palbociclib, CDK4/6 inhibitors, Small-molecule kinase inhibitors.
Shares Palbociclib, CDK4/6 inhibitors, Small-molecule kinase inhibitors.
Shares Agonist and antagonist, Targeted therapy, Palbociclib, CDK4/6 inhibitors.