327 research outputs found

    Figure S1 from Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

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    Activation loop residues 937-954 are more disordered in mutant vs. wildtype PI3Kα</p

    Table S3 from Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

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    RLY-2608 biochemical inhibition with liposome substrates</p

    Table S1 from Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

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    In vitro kinome profile of RLY-2608. RLY-2608 was tested at a concentration of 10 µM by SelectScreen (ThermoFisher Scientific)</p

    Table S1 from Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

    No full text
    In vitro kinome profile of RLY-2608. RLY-2608 was tested at a concentration of 10 µM by SelectScreen (ThermoFisher Scientific)</p

    Supplemental Text from Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

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    Synthesis of mutant-selective allosteric PI3Kα inhibitors</p

    Figure S2 from Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

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    PI3Kα KD Simulations</p

    Figure S2 from Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

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    PI3Kα KD Simulations</p

    Table S2 from Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

    No full text
    Time-dependence of biochemical inhibition and mutant selectivity of RLY-2608</p

    Figure S3 from Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

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    Binding kinetics and potency of [2] towards PI3Kα</p

    Supplemental Text from Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

    No full text
    Synthesis of mutant-selective allosteric PI3Kα inhibitors</p
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