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

Abstract: New improved formulations are described, comprising at least one composition, with or without another composition (at least one second composition), in which the at least one composition, a first composition, is an inhibitor of lipid A deacetylase resulting in permeabilization of an outer membrane of a susceptible microorganism to which it is provided to. The at least one second composition may be a streptogramin. The first composition, alone or in combination with another, may be used to improve and/or treat a wide variety of bacterial infections, providing, on its own better efficacy, bioavailability, and/or pharmacokinetics, as compared with at least other or alternative inhibitors of lipid A deacetylase, as well as no expected cardiotoxicity. When provided to a susceptible microorganism as a combination described herein, the combination may be provided independently or may be provided together (co-combined in a same formulation, or in different formulations).

Abstract: The present invention relates to a pharmaceutical composition and a health functional food composition for preventing, alleviating or treating inflammatory diseases, including Toxoplasma gondii GRA9 protein or a gene encoding the protein as an active ingredient. The present inventors have identified the C-terminal region essential for the NLRP3-mediated mechanism of action and function of Toxoplasma gondii GRA9 in macrophages, which are host immune cells and confirmed the substantial anti-inflammatory and antibacterial effects and the antiseptic effect in vivo. Accordingly, Toxoplasma gondii GRA9 protein or a gene encoding the protein is expected to be usefully utilized in the field of prevention or treatment of inflammatory diseases caused by an abnormal NLRP3-mediated inflammatory response, including sepsis.

Abstract: Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative 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 undesirable fibrosis and undesirable inflammation.

Abstract: The invention relates to methods for synthesizing amanitin derivatives having an amino group attached to position 6? of the central tryptophan moiety. The invention furthermore relates to an amanitin derivative having an amino group attached to position 6? of the central tryptophan moiety, conjugates of such amanitin derivative, and pharmaceutical compositions comprising such conjugates.

Abstract: This disclosure relates to recombinant or chimeric FVIII proteins, variants, and vectors encoding the proteins containing one or more ancestral mutations. In certain embodiments, one or more protein domains comprise amino acid sequences that are derived from ancestrally reconstructed amino acid sequences. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising the proteins or vectors and related methods of inducing blood clotting.

Abstract: The present invention is directed to novel lyophilized pharmaceutical preparations comprising a cytotoxic dipeptides such as melphalan flufenamide and one or more excipient(s) selected from the group comprising a polysorbate; a polyethylene glycol; ?-cyclodextrin; ocyclodextrin; hydroxypropyl-?-cyclodextrin; sulfobutylether-?-cyclodextrin; lactose; benzyl alcohol; disodium succinate; propylene glycol; Cremophor EL; Dimethyl sulfoxide; D-mannitol; Trehalose; Sucrose and an amino acid. This preparation may be further formulated and is useful in cancer therapy.

Abstract: The present invention generally relates to antibodies, antigen-binding fragments thereof, polypeptides, and immunoconjugates that bind to CD123 antigen (the ? chain of the interleukine 3 receptor, or IL-3R?). The present invention also relates to methods of using such CD123-binding molecules for diagnosing and treating diseases, such as B-cell malignancies.

Abstract: Analogues of an alternatively spliced form of atrial natriuretic peptide (MANP) that exhibit pGC-A gain of function and can be used to treat cardiorenal and metabolic disease are described herein.

Abstract: The present invention relates to a composition for prevention or treatment of hair loss. The composition is effectively delivered into hair papilla cells in a hair loss area, which is a target area, wherein a cytokine or enzyme highly expressed in the hair loss area causes a drug to be separated from a compound contained in the composition so that the drug effectively exhibits activity, which ultimately promotes hair growth and/or hair regrowth.

Abstract: The present invention relates to peptides, in particular amyloid inhibitory peptides, and to pharmaceutical compositions comprising such peptides. Furthermore, the present invention relates to such peptides, in particular such amyloid inhibitory peptides, for use in methods of treating or diagnosing neurodegenerative diseases such as Alzheimer's disease, or for use in a method of treating or diagnosing type 2 diabetes. Furthermore, the present invention also relates to a kit for the in-vitro or in-vivo detection and, optionally, quantification of amyloidogenic polypeptides, amyloid fibrils or amyloid aggregates, and/or for the diagnosis of Alzheimer's disease or type 2 diabetes in a patient.

Abstract: The invention pertains to a recombinant polypeptide comprising a truncated von Willebrand Factor (VWF) for use in the treatment or prophylaxis of a blood coagulation disorder, said treatment or prophylaxis comprising administering the recombinant polypeptide and a Factor VIII protein (FVIII) extravascular to a subject having a blood coagulation disorder, wherein said recombinant polypeptide is capable of binding to said FVIII, and wherein the molar ratio of the recombinant polypeptide to be administered to the FVIII to be administered is higher than 50.

Abstract: The invention provides materials and methods for the treatment of obesity and excess weight, diabetes, and other associated metabolic disorders. In particular, the invention provides novel acylated glucagon analogue peptides effective in such methods. The peptides may mediate their effect by having increased selectivity for the GLP-1 receptor as compared to human glucagon.

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.

Abstract: Provided herein are thiosuccinyl-crosslinked hemoglobin conjugates useful as blood replacement agents and therapeutic proteins, pharmaceutical compositions comprising the same and the methods of use and preparation thereof.

Abstract: This disclosure relates to compositions comprising an antagonist of vasoactive intestinal polypeptide signaling coupled to a nanoparticle and methods of use related thereto. In certain embodiments, the nanoparticle is a poloxamer-stabilized polypropylene sulfide nanoparticle.

Abstract: The present invention relates generally to novel depsipeptides, to methods for the preparation of these novel depsipeptides, to pharmaceutical compositions comprising the novel depsipeptides; and to methods of using the novel depsipeptides to treat or inhibit various disorders.

Abstract: The present invention relates to a branched peptide that includes a first peptide chain and a second peptide chain having its C-terminal amino acid covalently linked to a sidechain of an amino acid residue of the first peptide chain, wherein the first peptide chain includes a plurality of aromatic amino acids and, optionally, an aromatic group linked to an amino terminus of the first peptide chain; and the second peptide chain includes a plurality of hydrophilic amino acids and an enzyme cleavage site. Pharmaceutical compositions containing the branched peptide and one or more therapeutic agents in an aqueous medium are disclosed, where the branched peptides form micelle structures in the aqueous medium. Methods of using the pharmaceutical composition to deliver therapeutic agents, and for treating various disease conditions are also described.

Abstract: A linker peptide for constructing a fusion protein. The linker peptide comprises a flexible peptide and a rigid peptide. The flexible peptide consists of one or more flexible units. The rigid peptide consists of one or more rigid units. The flexible unit comprises two or more amino acid residues selected from Gly, Ser, Ala, and Thr. The rigid unit comprises a human chorionic gonadotropin ?-subunit carboxy-terminal peptide (CTP) bearing a plurality of glycosylation sites. The linker peptide can more effectively eliminate mutual steric hindrance of two fusion molecules, decreasing a reduction/loss of polymerization or activity resulting from improper folding of an active protein or a conformational change. On the other hand, the negatively charged, highly sialylated CTP can resist renal clearance, further prolonging a half-life of a fused molecule and enhancing bioavailability of a fused protein.

Abstract: Compounds of Formula I: I and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.