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Stabilized SOS1 peptides

  • US 10,087,215 B2
  • Filed: 03/14/2014
  • Issued: 10/02/2018
  • Est. Priority Date: 03/15/2013
  • Status: Active Grant
First Claim
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1. An internally cross-linked polypeptide comprising the amino acid sequence A0B0C0D0E0F0G0 A1B1C1D1E1F1G1 A2B2 (SEQ ID NO:

  • 1) wherein;

    A0 is F;

    B0 is F;

    C0 is G;

    D0 is I;

    E0 is Y;

    F0 is L;

    G0 is T;

    A1 is N;

    B1 is I;

    C1 is L, K, or K substituted with a guanine nucleoside or guanine nucleoside analog;

    D1 is K or R;

    E1 is T;

    F1 is E;

    G1 is E, K, or K substituted with a guanine nucleoside or guanine nucleoside analog;

    A2 is G; and

    B2 is N;

    wherein the side chains of two amino acids of SEQ ID NO;

    1 separated by three or six amino acids are cross-linked by an internal hydrocarbon staple; and

    wherein the internally cross-linked polypeptide binds a wild type KRAS protein.

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