Abstract: The present application describes stapled peptide degron chimeras, which act as protein degradation inducing moieties, either by combining a stapled peptide that binds a disease-related protein with a small molecule degron, such as a cereblon- or VHL-binding small molecule as the degron, or a polypeptide sequence degron, such as a Cop1-binding Trib peptide as the degron; or by combining a stapled peptide degron with a peptide, such as a stapled peptide, or a small molecule that binds a disease-related protein. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of stapled peptide degron chimeras which can be utilized in the treatment of proliferative disorders or other conditions whereby elimination of a disease-causing or disease-related protein would have a therapeutic benefit. The present application also provides methods for making compounds of the application and intermediates thereof.

Abstract: The disclosure relates to cell-permeable stabilized peptide modules and methods of use for e.g., cellular delivery of cargoes.

Abstract: Structurally stabilized, e.g., stapled, peptides with the ability to translocate through microbial cell membranes to the interior of microbial cells and exert a biological activity there are provided, as are methods of designing, making and using such peptides.

Abstract: This disclosure features structurally-stabilized oncolytic peptides and related compositions and methods of making same. Also disclosed are methods of using such structurally-stabilized peptides in the treatment of cancer, e.g., a hematological cancer, e.g., a leukemia, a lymphoma, or multiple myeloma, and/or in the inhibition of proliferation of a cancer cell, e.g., a hematological cancer, e.g., a leukemia and/or a lymphoma and/or a multiple myeloma cell. Also disclosed are methods of using such structurally-stabilized peptides for killing cancer cells or dual-killing cancer cell and micro-organisms, and thus providing therapeutics to treat cancer with or without simultaneously preventing or treating infection, while avoiding toxicity to normal, non-cancerous cells.

Abstract: Methods of generating and optimizing stabilized (e.g., stapled and/or stitched) anti-microbial peptides (StAMPs) for the prophylaxis and treatment of antibiotic-resistant (e.g., colistin-resistant, methicillin resistant, meropenem-resistant) bacterial infections (e.g., Gram-negative, Gram-positive), and methods for using such peptides for experimental investigation, livestock management, management of crops/trees/plants, and/or therapeutic benefit. Also featured are methods for reducing renal toxicity of a StAMP.

Abstract: A system for visually representing peptide sequences includes a memory configured to store instructions and a processor to execute the instructions to perform operations. The operations include receiving data representing a peptide sequence. The data includes an index representing a position for each amino acid in the peptide sequence. The operations further include categorizing each amino acid in the peptide sequence and assigning each amino acid a value associated with the category. The operations additionally include determining relationship groups, each group including two amino acids in the peptide sequence, based upon a geometrical structure of the peptide sequence. The operations also include filtering the relationship groups to remove groups based upon the category of at least one of the two amino acids that make up the group; and producing a visual representation that includes a representation of each amino acid of the filtered relationship groups.

Abstract: The disclosure relates to cell-permeable stabilized peptide modules and methods of use for e.g., cellular delivery of cargoes.

Abstract: This disclosure describes stabilized peptides and methods for detecting a biomarker on, outside, or within a live cell or tissue, or in a cell or tissue that has been fixed for an immunological assay or histopathologic evaluation. The present disclosure further describes stabilized peptides and methods for diagnosing and/or monitoring the progression of a disease in a subject, or for monitoring the efficacy of a disease treatment in a subject, based on the presence of a biomarker, the amount of a biomarker, and/or the localization of a biomarker in a live or fixed cell or tissue obtained from a subject.

Abstract: The present application describes stapled peptide degron chimeras, which act as protein degradation inducing moieties, either by combining a stapled peptide that binds a disease-related protein with a small molecule degron, such as a cereblon- or VHL-binding small molecule as the degron, or a polypeptide sequence degron, such as a Cop1-binding Trib peptide as the degron; or by combining a stapled peptide degron with a peptide, such as a stapled peptide, or a small molecule that binds a disease-related protein. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of stapled peptide degron chimeras which can be utilized in the treatment of proliferative disorders or other conditions whereby elimination of a disease-causing or disease-related protein would have a therapeutic benefit. The present application also provides methods for making compounds of the application and intermediates thereof.

Abstract: Structurally stabilized, e.g., stapled, peptides with the ability to translocate through microbial cell membranes to the interior of microbial cells and exert a biological activity there are provided, as are methods of designing, making and using such peptides.

Abstract: The present invention provides methods of designing and making structurally stabilized anti-microbial peptides for the prophylaxis and treatment of infection. Methods are also disclosed for designing stabilized anti-microbial peptides that are selectively lytic/cytotoxic to bacteria, allowing for internal use of anti-microbial peptides without mammalian membrane disruption and cytotoxicity.

Abstract: Methods of generating and optimizing stabilized (e.g., stapled and/or stitched) anti-microbial peptides (StAMPs) for the prophylaxis and treatment of antibiotic-resistant (e.g., colistin-resistant, methicillin resistant, meropenem-resistant) bacterial infections (e.g., Gram-negative, Gram-positive), and methods for using such peptides for experimental investigation, livestock management, management of crops/trees/plants, and/or therapeutic benefit. Also featured are methods for reducing renal toxicity of a StAMP.

Abstract: The present invention provides methods of designing and making structurally stabilized anti-microbial peptides for the prophylaxis and treatment of infection. Methods are also disclosed for designing stabilized anti-microbial peptides that are selectively lytic/cytotoxic to bacteria, allowing for internal use of anti-microbial peptides without mammalian membrane disruption and cytotoxicity.

Abstract: Structurally stabilized, e.g., stapled, peptides with the ability to translocate through microbial cell membranes to the interior of microbial cells and exert a biological activity there are provided, as are methods of designing, making and using such peptides.

Abstract: The present invention provides methods of designing and making structurally stabilized anti-microbial peptides for the prophylaxis and treatment of infection. Methods are also disclosed for designing stabilized anti-microbial peptides that are selectively lytic/cytotoxic to bacteria, allowing for internal use of anti-microbial peptides without mammalian membrane disruption and cytotoxicity.