BICYCLIC PEPTIDYL PAN-RAS INHIBITORS

    公开(公告)号:US20240368224A1

    公开(公告)日:2024-11-07

    申请号:US18572885

    申请日:2022-06-22

    Abstract: Disclosed are Ras inhibiting bicyclic peptides. Also provided herein are methods of treating cancer in a subject, including human subject, and animal. The methods include administering to a subject an effective amount of one or more of the compounds or compositions described. The disclosed methods can optionally include identifying a patient who is or can be in need of treatment of a cancer.

    KRAS-SPECIFIC CAPTURE AGENTS, COMPOSITIONS, AND METHODS OF MAKING AND USING

    公开(公告)号:US20220402971A1

    公开(公告)日:2022-12-22

    申请号:US17815805

    申请日:2022-07-28

    Inventor: James R. Heath

    Abstract: Disclosed are compounds, compositions, and methods involving cyclic peptides that can bind to KRAS (G12D) oncogenic protein. For example, disclosed are cyclic peptides that selectively bind KRAS (G12D) oncogenic protein. Also disclosed are methods of inhibiting KRAS (G12D) oncogenic protein in a cancer cell expressing KRAS (G12D) oncogenic protein. In some forms, the method comprises incubating the cancer cell with any one or more of the disclosed cyclic peptides. In some forms, the method comprises bringing into contact the cancer cell with any one or more of the disclosed cyclic peptides.

    DI-SULFIDE CONTAINING CELL PENETRATING PEPTIDES AND METHODS OF MAKING AND USING THEREOF

    公开(公告)号:US20190282654A1

    公开(公告)日:2019-09-19

    申请号:US16348706

    申请日:2017-11-09

    Abstract: Disclosed is a general, reversible bicyclization strategy to increase both the proteolytic stability and cell permeability of peptidyl drugs. A peptide drug is fused with a short cell-penetrating motif and converted into a conformationally constrained bicyclic structure through the formation of a pair of disulfide bonds. The resulting bicyclic peptide has greatly enhanced proteolytic stability as well as cell-permeability. Once inside the cell, the disulfide bonds are reduced to produce a linear, biologically active peptide. This strategy was applied to generate a cell-permeable bicyclic peptidyl inhibitor against the NEMO-IKK interaction.

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