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Therapeutic strategies to target RAS-mutant cancers

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Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS–SOS1 interaction

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Ras Conformational Ensembles, Allostery, and Signaling

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Inhibition of RAS function through targeting an allosteric regulatory site

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In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C

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Drugging Ras GTPase: a comprehensive mechanistic and signaling structural view

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RAS: Striking at the Core of the Oncogenic Circuitry

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Expanding the scope of electrophiles capable of targeting K-Ras oncogenes

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Discovery of High-Affinity Noncovalent Allosteric KRAS Inhibitors That Disrupt Effector Binding

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Crystal Structure of a Human K-Ras G12D Mutant in Complex with GDP and the Cyclic Inhibitory Peptide KRpep-2d

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Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations

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Identification of a New Potent Inhibitor Targeting KRAS in Non-small Cell Lung Cancer Cells

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Structural insights into small-molecule KRAS inhibitors for targeting KRAS mutant cancers

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Suppressing nucleotide exchange to inhibit KRAS-mutant tumors

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RAS Mutations in Advanced Colorectal Cancer: Mechanisms, Clinical Implications, and Novel Therapeutic Approaches

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Data from Delineating the RAS Conformational Landscape

Parker, M. I., Meyer, J. E., Golemis, E. A., & Dunbrack (2023) · doi:10.1158/0008-5472.c.6513960

Abstract 1791: RADIL regulates RAS downstream signaling

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Suppression of Ras-Induced Apoptosis by the Rac GTPase

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The role of wild-type RAS in oncogenic RAS transformation

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Abstract 413: WT RAS signaling is an essential therapeutic target in RAS mutated cancers

Sealover, N. E., & Kortum, R. L. (2022) · Cancer Research · doi:10.1158/1538-7445.am2022-413

Abstract B033: Wild-type RAS signaling is an essential therapeutic target in RAS-mutated cancers

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