Abstract: The present invention provides a pharmaceutical composition, and methods of use thereof, for treating ocular boundary deficiency, symptoms associated therewith, or undesired condition that is associated with or causes ocular boundary deficiency at the ocular surface. The pharmaceutical composition of the present invention comprises a human PRG4 protein, a lubricant fragment, homolog, or isoform thereof, suspended in an ophthalmically acceptable balanced salt solution. The pharmaceutical composition of the present invention may also comprise one or more ophthalmically acceptable agents selected from the group consisting of an ophthalmically acceptable demulcent, excipient, astringent, vasoconstrictor, emollient, sodium hyaluronate, hyaluronic acid, and surface active phospholipids, in a pharmaceutically acceptable carrier for topical administration.

Abstract: The present invention provides inhibitors and/or antagonists of plasma kallikrein. Also provided are methods of utilizing the inhibitors as therapeutics.

Abstract: The present invention relates to a method or composition for glycemic control in a subject, which is effective for treating diabetes mellitus, comprising administering the subject with a pharmaceutical composition comprising a therapeutically effective amount of an aliphatic alcohol having a general formula of CH3(CH2)nCH2OH, wherein n is an integer from 10 to 40, such as tetracosanol, and a pharmaceutically acceptable carrier.

Abstract: The present invention provides peptide analogues of ?-MSH and ?-MSH, comprising the amino acid sequence of human ?-MSH or ?-MSH, or variants thereof, and having a branched amino acid probe in the N-terminal part of the peptide.

Abstract: The present invention relates to novel muteins derived from human tear lipocalin having affinity to human c-Met receptor tyrosin kinase (c-Met). The invention also refers to a corresponding nucleic acid molecule encoding such a mutein and to a method for its generation. The invention further refers to a method for producing such a mutein. Finally, the invention is directed to a pharmaceutical composition comprising such a lipocalin mutein as well as to various uses of the mutein.

Abstract: The present invention is directed to novel cytotoxic spliceostatin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.

Abstract: The present invention relates to micelle-forming poly(ethylene oxide)-block-poly(ester) block copolymers having reactive groups on the polyester block therein. The biodegradability of these copolymers and their biocompatibilities with a large number of bioactive agents make them suitable as carriers for various bioactive agents. The bioactive agents, such as DNA, RNA, oligonucleotide, protein, peptide, drug and the like, can be coupled to the reactive groups on the polyester block of the copolymer.

Abstract: The invention relates to peptide mimetics comprising the residues P4-P3-P2-P1, which were cyclized between the side chains of P3 and P2 amino acid and are, as inhibitors of the serine protease plasmin, suitable to be used to inhibit fibrinolysis and thus to reduce blood loss in hyperfibrinolytic conditions, for example during surgery.

Abstract: The present invention relates to prodrugs of parent drug compounds containing heteroaromatic NH groups.

Abstract: A novel selenium-containing compound, a method of producing the selenium-containing compound, an analysis method using the selenium-containing compound, and use of the selenium-containing compound as an antioxidant, are disclosed. A novel selenium-containing compound shown by any of chemical formulas 1 to 4 is obtained by extracting a selenium-containing compound from a sample using an organic solvent or water, and purifying the selenium-containing compound. The novel selenium-containing compound may be used for a novel analysis method, or may be used as an antioxidant.

Abstract: The invention relates to a compound suited as entity carrier, having the general formula (I) wherein X is an amine-containing residue further defined herein. The invention further relates to the use of such compounds, a nanocarrier system, a kit comprising such compounds and methods for gene silencing and anti-cancer treatment.

Abstract: The present invention relates to methods and compositions for modulating angiogenesis. In particular, the present invention relates to Pigment Epithelial-derived Factor (PEDF) fragments for use in modulating angiogenesis and treating angiogenesis mediated disease.

Abstract: Oligomeric reagents are provided comprising a moiety of atoms arranged in a specific order, wherein the moiety is positioned between a water-soluble, non-peptidic oligomer and a pharmaceutically active agent. The oligomeric reagents are useful for, among other things, forming oligomer active agent conjugates. Related methods, compositions, preparations, and so forth are also provided.

Abstract: Prodrug formulations of bioactive polypeptides are provided wherein the bioactive polypeptide has been modified by the linkage of a dipeptide to the bioactive polypeptide through an ester linkage. The prodrugs disclosed herein in some embodiments have extended half lives of at least 1.5 hours (e.g., at least 10 hours), and more typically greater than 20 hours and less than 70 hours, and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.

Abstract: The present invention relates to the targeted delivery of molecules to cells expressing toll-like receptors (TLRs). Aspects of the invention provide compounds comprising a positively charged group linked to a TLR ligand. These compounds are useful for in vitro and in vivo methods of transfection of TLR-expressing cells. Other aspects of the invention relate to the use of such compounds for repression of gene expression and DNA vaccination approaches.

Abstract: Stably cross-linked a polypeptides related to human MAML are described. These cross-linked polypeptides contain at least two modified amino acids that together form an internal cross-link or tether that can help to stabilize the alpha-helical secondary structure that is thought to be important for binding of MAML peptides to the Notch transcription complex, a complex that includes ICN and CSL.

Abstract: Dye conjugates of template-fixed ?-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 14 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, or Pro or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have CXCR4 antagonizing properties, and are useful for cancer therapy; diagnostic imaging; for detection of tumors and other abnormalities; for photoacoustic tumor imaging, detection and therapy; and for sonofluorescence tumor imaging, detection and therapy. The various dyes forming part of these conjugates are useful over the range of 300-1200 nm, the exact range being dependent upon the particular dye. These dye conjugates of ?-hairpin peptidomimetic can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

Abstract: The present invention provides a peptide and a composition which are suitable for oral ingestion, and which have a skin aging-inhibiting activity, a collagen-production promoting activity, an epidermal turnover promoting activity, and a cutaneous cell-proliferating effect. The present invention also provides a medicament and a functional food which have a skin aging-inhibiting activity, a collagen-production promoting activity, and a cutaneous cell-proliferation promoting activity. The present invention provides a composition including at least one peptide of Asn-lle-Pro-Pro-Leu, lle-Pro-Pro-Leu, lle-Pro-Pro, Pro-Val-Val-Val-Pro-Pro, Val-Pro-Pro-Phe, Val-Pro-Pro, Phe-Pro-Pro-Gln, and Leu-Pro-Pro-Thr.

Abstract: A method of producing a molecularly-imprinted material comprises synthesizing a peptide, oligosaccharide or oligonucleotide on a disposable surface modified support to produce a support surface-attached peptide, oligosaccharide or oligonucleotide, providing a selected monomer mixture, contacting the monomer mixture with the support surface-attached peptide, oligosaccharide or oligonucleotide, initiating polymerisation or at least one crosslinking reaction, dissolving or degrading the support surface-attached peptide, oligosaccharide or oligonucleotide and support, and obtaining molecularly imprinted material.

Abstract: Disclosed embodiments concern a method for making substantial quantities of desired macrocycles. Disclosed ring closing reactions make the macrocycle with desired olefin geometry in excellent yield and E/Z ratio. Particular embodiments of the current method concern intermediates that are obtained from commercially available starting materials in a small number of steps, thereby illustrating the commercial importance and applicability of the disclosed method. The macrocycle produced by the ring closing reaction can be further derivatized to provide analogs of the macrocyclic compounds.