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• W3212009938 abstract "RAS proteins are central in the proliferation of many types of cancer, but a general approach toward the identification of pan-mutant RAS inhibitors has remained unresolved. In this work, we describe the application of a binding pharmacophore identified from analysis of known RAS binding peptides to the design of novel peptides. Using a chemically divergent approach, we generated a library of small stapled peptides from which we identified compounds with weak binding activity. Exploration of structure-activity relationships (SARs) and optimization of these early compounds led to low-micromolar binders of KRAS that block nucleotide exchange." @default.
• W3212009938 created "2021-11-22" @default.
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• W3212009938 date "2021-11-17" @default.
• W3212009938 modified "2023-09-27" @default.
• W3212009938 title "Targeting a Novel KRAS Binding Site: Application of One-Component Stapling of Small (5–6-mer) Peptides" @default.
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• W3212009938 doi "https://doi.org/10.1021/acs.jmedchem.1c01334" @default.
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• W3212009938 hasPublicationYear "2021" @default.
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