Abstract: The present disclosure provides a large combinatorial library of cell-permeable bicyclic peptides. The bicyclic peptides described herein include the first ring consisted of randomized peptide sequences for potential binding to a target of interest while the second ring featured a family of different cell-penetrating motifs, for both cell penetration and target binding. The library was screened against the I?B kinase ?/? (IKK?/?)-binding domain of NF-?B essential modulator (NEMO), resulting in the discovery of several cell-permeable bicyclic peptides which inhibited the NEMO-IKK? interaction, thereby selectively inhibiting canonical NF-?B signaling in mammalian cells and the proliferation of cisplatin-resistant ovarian cancer cells.

Abstract: The present invention provides a composition comprising specific self-assembling peptides, which are capable of self-assembly at a pH below 7.5 and at least physiologic ionic strength, e.g., PI 1-4. PI 1-8, PI 1-14, PI 1-13, PI 1-12, PI 1-28, PI 1-29, PI 1-2, PI 1-5, PI 1-17, PI 1-19, PI 1-20, PI 1-12, PI 1-16, PI 1-18, PI 1-26 or PI 1-31 for use in treating an oral disease selected from the group consisting of gingivitis, periodontitis and/or peri-implantitis in a subject. Said composition may be used, after suitable cleaning procedures, for filling pockets formed adjacent to teeth in said diseases, which enhances tissue regeneration. The composition may be suitable for controlled release of an active agent, e.g., an antimicrobial or antibiotic agent. The invention also provides a kit suitable for said treatment further comprising self-assembling peptides suitable for forming a second layer on top of the first composition.

Abstract: The present invention relates to Fc binding proteins comprising one or more domains with Cysteine in the C-terminal helical region. The invention further relates to affinity matrices comprising the Fc binding proteins of the invention. The invention also relates to a use of these Fc binding proteins or affinity matrices for affinity purification of immunoglobulins and to methods of affinity purification using the Fc binding proteins of the invention.

Abstract: Methods for treating cancer with a stabilized BCL9 peptide are encompassed, wherein the stabilized peptide comprises a portion of the HD2 domain of the BCL9 protein containing a hydrocarbon crosslinker generated using ?,?-disubstituted amino acids.

Abstract: Disclosed are analogs of elamipretide (MTP-131). The compounds are useful for the treatment and prevention of ischemia-reperfusion injury (e.g., cardiac ischemia-reperfusion injury) or myocardial infarction.

Abstract: Described herein is a peptide or peptidomimetic with a length of at least 6 residues comprising, consisting essentially of, or consisting of the sequence motif Xaa1-Trp-Xaa2-Xaa3-Xaa4-Xaa5 (SEQ ID NO:1), wherein: Xaa1 represents an aromatic residue (Phe, Tyr, Trp, His), Cys or Ser; Xaa2, Xaa3 and Xaa4 represent any residue; and Xaa5 represents Gly, lie or Val.

Abstract: Provided are a method for producing a peptide compound including a step of using a compound represented by Formula (1); a protective group-forming reagent including the compound; and the compound. At least one of R1 to R8 or Y2 has RA, RA represents an aliphatic hydrocarbon group or an organic group having an aliphatic hydrocarbon group, and the number of carbon atoms in at least one aliphatic hydrocarbon group is 12 or more. However, RA does not have a silyl group and a hydrocarbon group having a silyloxy structure.

Abstract: A method is provided for a condition related to the activity of a protease through the administration of a ?-defensin, analog, or derivative is described. Suitable proteases include metalloproteases and cysteine proteases such as Cathepsin-C. The ?-defensin, analog, or derivative can be effectively administered parenterally, topically, or orally.

Abstract: Among the various aspects of the present disclosure is the provision of targeting TPL2 kinase as a novel strategy to block oncogenic KRAS-driven signaling, detection of TPL2 mutations, and uses of TPL2 inhibiting agents alone or in combination with chemotherapy in subjects having TPL2- or RAS-associated cancer.

Abstract: Provided herein are charge complementary peptides that can be optionally coupled to a cargo polypeptide that are capable of self-assembling under stimulating conditions. The charge complementary peptides can be capable of forming supramolecular structures. Also provided herein are methods of using the charge complementary peptides provided herein.

Abstract: Disclosed are prodrugs of cytotoxic anthracyclines (such as doxorubicin) and other therapeutic agents that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of cytotoxic and other agents to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compounds comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, fibrosis, and inflammation.

Abstract: Provided are methods and compositions for delivering a nucleic acid, protein, and/or ribonucleoprotein payload to a cell. Also provided are delivery molecules that include a peptide targeting ligand conjugated to a protein or nucleic acid payload (e.g., an siRNA molecule), or conjugated to a charged polymer polypeptide domain (e.g., poly-arginine such as 9R or a poly-histidine such as 6H, and the like). The targeting ligand provides for (i) targeted binding to a cell surface protein, and (ii) engagement of a long endosomal recycling pathway. As such, when the targeting ligand engages the intended cell surface protein, the delivery molecule enters the cell (e.g., via endocytosis) but is preferentially directed away from the lysosomal degradation pathway.

Abstract: Provided are keratin BD-4, an encoding nucleic acid molecule thereof, an expression vector, a host cell, and a pharmaceutical composition containing the keratin. The keratin BD-4 can be used for preparing drugs having antipyretic and analgesic, antitussive and expectorant, and antiepileptic effects.

Abstract: The present invention relates to a fusion peptide having one of the following formulae: P1-L-P2 (I) or P2-L-P1 (II) wherein P1 is chosen from the proline-rich antimicrobial peptides; Lisa peptide linker; and P2 has the following formula (III): wherein m is 0 or 1; n is an integer comprised between 0 and 9; p is an integer comprised between 0 and 10; r is 0, 1 or 2; s is 0 or 1; Gln is glutamine; R1 is the side chain of arginine or lysine; R2 is for example a —(CH2)—C3-6-cycloalkyl group optionally substituted; R3 is for example a C1-8-alkyl group; R4 is in particular a C1-8-alkyl group optionally substituted by a C3-6-cycloalkyl group; R5 is for example a —(CH2)—C3-6-cycloalkyl group; R6 is in particular —COOH, wherein, when the fusion peptide has the formula (II), its C-terminus contains a —CO— group engaged in a peptide bond with said linker.

Abstract: The present disclosure provides isolated polypeptides comprising variable lymphocyte receptors that specifically bind the brain extracellular matrix, compositions, and methods of use. Methods of using the variable lymphocyte receptors for the detection and treatment of disease or injury, specifically, for example, cancers including glioblastoma are provided.

Abstract: Provided herein are drug delivery systems comprising a peptide targeting agent and a pharmaceutical agent for delivery of chemotherapeutic agents. Also provided are methods of treating cancer comprising administration of the drug delivery system disclosed herein.

Abstract: The present invention relates to crystalline polymorphs of an echinocandin antifungal agent and novel methods for their preparation.

Abstract: Disclosed are prodrugs of cytotoxic anthracyclines (such as doxorubicin) and other therapeutic agents that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of cytotoxic and other agents to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compounds comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, fibrosis, and inflammation.

Abstract: The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of CD137. The invention also includes drug conjugates comprising said peptides, conjugated to one or more effector and/or functional groups, to pharmaceutical compositions comprising said peptide ligands and drug conjugates and to the use of said peptide ligands and drug conjugates in preventing, suppressing or treating a disease or disorder mediated by CD137.

Abstract: Disclosed are prodrugs of cytotoxic anthracyclines (such as doxorubicin) and other therapeutic agents that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of cytotoxic and other agents to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compounds comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, fibrosis, and inflammation.