Abstract: An acid-cleavable peptide linker comprising aspartic acid and proline residues is disclosed. The acid-cleavable peptide linker provides an altered sensitivity to acid-hydrolytic release of peptides of interest from fusion peptides of the formula PEP1-L-PEP2. The inventive linker, L, is described in various embodiments, each of which provides substantially more rapid acid-release of peptides of interest than does a single aspartic acid-proline pair. In an additional aspect, a method of increasing the stability of an acid cleavable linkage to acid hydrolysis is also provided.

Abstract: The present invention provides compositions and methods for inducing an immune response in a subject. In particular, the present invention provides compositions comprising immunostimulatory ligands (ISL) and methods of inducing an immune response in a subject therewith. Compositions and methods of the present invention find use in, among other things, clinical (e.g. therapeutic and preventative medicine (e.g., vaccination)) and research applications.

Abstract: A process for extraction of a peptide from a reaction mixture resulting from a peptide coupling reaction, the reaction mixture containing the peptide and a polar aprotic solvent selected from the group consisting of N,N-dimethylformamide, N,N-dimethylacetamide and N-methyl-2-pyrrolidone, whereby the process includes a step a) and a step b): step a) including the addition of a component a1) and a component a2), whereby component a1) is 2-methyltetrahydrofuran and component a2) is water, to the reaction mixture, so that a biphasic system with an organic layer and an aqueous layer is obtained; step b) including the subsequent separation of the organic layer containing the peptide from the aqueous layer. In an embodiment, a combination of 2-methyltetrahydrofuran and an organic solvent 1 selected from the group consisting of n-heptane, toluene, ethylacetate, isopropylacetate, acetonitrile and tetrahydrofuran is used for the process for extraction.

Abstract: Disclosed are RNA targeting compounds, methods for using the subject RNA targeting compounds to treat myotonic dystrophy and other diseases are also disclosed.

Abstract: Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating such diseases are also described.

Abstract: In one aspect, the present invention provides isolated novel peptides that can be used to modulate innate immunity in a subject and/or for the treatment of an immune-related disorder, including treating and preventing infection by modulating innate immunity. Also provided are an agent reactive with the peptide, a pharmaceutical composition that includes the peptide, an isolated nucleic acid molecule encoding the peptide, a recombinant nucleic acid construct that includes the nucleic acid molecule, at least one host cell comprising the recombinant nucleic acid construct, and a method of producing the peptide using the host cell. The present invention further provides a method for treating and/or preventing infection in a subject by administering the peptide of the invention to the subject, thereby modulating innate immunity in the subject. Additionally, the present invention provides a method for predicting whether a subject would be responsive to treatment with a peptide of the invention.

Abstract: The present invention relates to compounds of Formula I, IA, II, HA, III, or IHA and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, IA, II, IIA, III, or IIIA are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases).

Abstract: Latent fluorescent tags, including compounds of Formula I, methods of making latent fluorescent tags, and methods of fluorescently labeling living cells are provided. The compounds of Formula I have the structure: wherein each of the variables are as defined herein.

Abstract: The present invention relates to different forms of a HCV inhibitory compound.

Abstract: The present specification provides for methods for purifying fibroins, purified fibroins, methods of conjugating biological and synthetic molecules to fibroins, fibroins conjugated to such molecules, methods of making fibroin hydrogels, fibroin hydrogels and fibroin hydrogel formulations useful for a variety of medical uses, including, without limitation uses as bulking agents, tissue space fillers, templates for tissue reconstruction or regeneration, cell culture scaffolds for tissue engineering and for disease models, surface coating to improve medical device function, or drug delivery devices.

Abstract: Described herein are multi-dimensional networks that can include a recurring unit of Formula (I) and a recurring unit of Formula (II), and methods of synthesizing and using the same.

Abstract: The present invention provides novel peptides that inhibit and/or reduce the opening of mammalian tight junctions, i.e. peptide tight junction antagonists. The present invention also provides methods for the treatment of excessive or undesirable permeability of a tissue by administering to a subject suffering from such a condition a composition comprising a peptide tight junction antagonist of the invention.

Abstract: A solid phase peptide synthesis method for synthesizing a peptidyl contrast agent is disclosed. In one example, the method includes synthesizing an amino-chelator loaded resin, coupling of the amino-chelator loaded resin to the C-terminus and/or backbone of a peptide, cleaving the amino-chelator-peptide from a resin, and chelating a lanthanide metal to the amino-chelator-peptide.

Abstract: The present invention provides a polypeptides capable of modulating tissue transglutarmnase-induced cell behaviour wherein the polypeptide comprises or consists of either (a) the amino acid sequence of a heparin-binding site of a tissue transglutaminase, or a functional fragment, variant, fusion or derivative thereof, or a fusion of said fragment, variant or derivative thereof or (b) an antibody capable of binding to a heparin-binding site of a lissue transglutaminase, or an antigen-binding fragment or derivative thereof. In one embodiment, the heparin-binding site of a tissue transglutaminase comprises or consists of an amino acid sequence of SEQ ID NO: 1, The invention further provides medical uses of the polypeptides of the invention and methods of treatment using the same.

Abstract: Peptides activating dermatopontin in the skin and cosmetic compositions including such peptide, in a physiologically suitable medium, are described. Methods of treating the cutaneous signs of aging and photoaging, and in particular wrinkles, sagging, and loss of volume and elasticity of the skin are also described.

Abstract: A method for inhibiting dipeptidyl-peptidase IV is provided and includes administering a peptide to the dipeptidyl-peptidase IV, in which the peptide is isolated from a gelatin hydrolysate produced by enzymatic digestion with alcalase (ALA), bromelain (BRO), and flavourzyme (FLA).

Abstract: The present invention provides a peptide represented by formula (I) of X1-Leu-X2-Leu-X3 wherein X1 represents Glu or Asp, X2 represents His, Lys or Arg, X3 represents Asp or Glu, with Glu, Asp, Leu, His, Lys and Arg being respectively glutamic acid, aspartic acid, leucine, histidine, lysine and arginine; or a pharmaceutically acceptable salt thereof; a composition for the treatment or prevention of at least one selected from cartilage damage and arthritis, containing the same peptide or a pharmaceutically acceptable salt thereof as an active ingredient; and a composition containing the same peptide or a pharmaceutically acceptable salt thereof and TGF?1.

Abstract: A process of freeze drying of an essentially aqueous solution comprising at least one first step having a first temperature and pressure level (i.e. primary drying phase) and at least one second step having a second temperature and pressure level (i.e. secondary drying phase) following the first step, wherein in the secondary drying phase limited desorption energy input is applied.

Abstract: A compound having the general structure R1, R2, R3 and R4 being selected from the group consisting of a hydrogen atom (H) and a C1-C20 alkyl, and R5 being a phenyl radical.

Abstract: Peptide compounds of the general formula (I) R1-(AA)n-X1—X2-Arg-Glu-Met-Asn-Trp-X3-(AA)p-R2 modulating the survivin protein are described. Furthermore, cosmetic or pharmaceutical compositions, including at least one peptide of the general formula (I), in a physiologically acceptable medium are described. Additionally, methods for treating the cutaneous signs of ageing and photo-ageing, treating the skin against external aggressions, and limiting hair loss and/or stimulating hair growth are described.

Abstract: Complexes of heterocyclic radionuclides are prepared based upon ligands having substituted pyridyl and imidazolyl groups. The ligands are bifunctional, having amino acid residues that may act as a linker to a bioactive molecule, and a tridentate chelator that may complex the radionuclide. The bioactive molecule may be a peptide or somatostatin.

Abstract: The present invention relates to compounds, and pharmaceutically acceptable salts thereof, comprising a vascular disrupting agent (VDA) associated and a MMP proteolytic cleavage site. The compounds are useful in the treatment of cancer.

Abstract: Polypeptides labelled with a donor and acceptor pair of dyes selected from a dibenzorhodamine dye and a diamino-benzophenoxazine dye are peptide conjugates which are useful for intracellular and bead-based assays with fluorescence detection. Peptide conjugates with a caspase-recognition site undergo cleavage into peptide fragments which may be detected, located, and quantitated by the changes in fluorescence. Intracellular cleavage of peptide conjugates is correlated with apoptosis.

Abstract: Peptides useful in determining the presence of autoantibodies in patients suffering from rheumatoid arthritis are disclosed.

Abstract: Disclosed herein are isolated polypeptides, antibody preparations, treatment methods, diagnostic methods, and screening methods related to tauopathy. Generally, the isolated polypeptide includes a core pentapeptide, with the proviso that the isolated polypeptide is not a native full-length tau protein. Generally, the antibody preparations include antibody that specifically binds to SEQ ID NO:12. Generally, the treatment methods include administering to a subject a composition that includes the isolated polypeptide. Generally, the diagnostic methods includes contacting a sample from a subject with an antibody preparation that includes antibody that specifically binds to SEQ ID NO:12, and then detecting a ligand in the sample that specifically binds the antibody preparation.

Abstract: The present invention provides novel peptides that facilitate the opening of mammalian tight junctions, i.e. tight junction agonists. The present invention also provides methods for the treatment of disease by administering to a subject suffering from the disease a composition comprising a peptide tight junction agonist of the invention in combination with a therapeutically effective amount of an active agent.

Abstract: Cellular targets on cancer cells have been identified that can be used with targeted molecular imaging to detect the cancer cells in vivo. Non-invasive methods for detecting cancer cells, such as metastasized cancer cells, are therefore provided. Also provided are compositions and kits for use in the disclosed methods.

Abstract: The present disclosure provides targeting peptides and vectors containing a sequence that encodes targeting peptides that deliver agents to the brain.

Abstract: The present invention provides processes for preparation of eptifibatide that involve coupling of amino acids in a (2+5), (4+3) and (3+4) sequence method. The invention further provides products produced by the described processes, novel compounds that can be used as synthetic intermediates for the preparation of eptifibatide.

Abstract: Provided are methods, compositions and articles of manufacture for detecting biomarkers indicative of exposure of a mammal to organophosphate compounds. The interaction of such a biomarker with a receptor bound to a biopolymer results in an optical readout that reports the presence of the biomarker.

Abstract: The present invention provides a compound including a peptidomimetic which interacts sterically with the binding site of a F11R molecule, the peptidomimetic including a peptidomimetic having the SEQ ID NO: 4D. The present invention also provides a method for treating a disorder comprising administering peptide 4D to a mammal.

Abstract: Disclosed are conjugates of hydrophobic drugs linked to protected or unprotected amino acids or peptides. The disclosed conjugates are amphiphilic and can self assemble into nanotubes. Nanotubes comprising the conjugates are also described and can have high loading of the drug and protect it from degradation or elimination. The nanotubes are well suited to deliver hydrophobic and unstable drugs to individuals.

Abstract: The invention provides a compound of formula (I), wherein R1 is H, C(NH)NH2, an amino acid, or a peptide; X is OH, NH2, NHR2, NR2R3, an amino acid, or a peptide; R2 and R3 are selected from alkyl, alkylenearyl, or alkyleneheteroaryl; each R4 and R5 is independently H or CH3; Z is 2-amino-2,3-dihydro-1H-indene-2-carboxylic acid; 2-amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid; 6-amino-6,7,8,9-tetrahydro-5H-benzo[7]annulene 6-carboxylic acid; cyclohexylalanine; cyclohexylglycine; homophenylalanine; 1-naphthylalanine; 2-naphthylalanine; 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; or octahydro-1H-indole-2-carboxylic acid; n is 0, 1, 2, 3, or 4; with the proviso that X is not NH2 when R1 is H, R4 is H, R5 is CH3, Z is Aci, and n is 2; or a pharmaceutically acceptable salt, ester or solvate thereof. A method of treating pain and a method for treating a mu-opioid receptor mediated disorder and/or a delta-opioid receptor mediated disorder also are provided.

Abstract: The present invention relates to antibacterial peptides and analogs thereof, e.g., originating from, derived from, isolated and/or purified from mammalian milk, that reduce, inhibit and/or prevent the growth or proliferation of a bacterial organism.

Abstract: Process for the preparation of a cyclopropylamide compound which is useful as a structural unit in a process for the preparation of a viral protease inhibitor.

Abstract: Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds. The compounds of the invention have potential therapeutic activity in view of their binding and inhibitory activities towards Plk1. They are based on the amino acid sequence PLHSpT (phosphorylated Thr). The PEG moiety, when present, is covalently attached at the N-terminus.

Abstract: The subject invention provides advantageous new salts of mu-opiate receptor peptides. These salts have been found to have excellent properties in terms of their crystal structure, stability, solubility, lack of impurities and/or the ability to be produced, with these advantageous properties, in amounts sufficient for the production of therapeutic compositions.

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

Abstract: At least some embodiments of the invention relates to an implant having a coating that contains or is composed of a functionalized RGD peptidomimetic RGD-P1 having the formula (1) and/or a functionalized RGD peptidomimetic RGD-P2 having the formula (2), and an associated manufacturing method.

Abstract: Compositions comprising dendritic cells pulsed with tumor lysate and at least one toll-like receptor (TLR) ligand which may be used for eliciting a specific immune response in a mammal in need thereof for treating diseases including a tumor are disclosed. Also disclose are methods of activating dendritic cells, comprising providing at least one toll-like receptor (TLR) ligand; and pulsing a dendentic cell with the at least one TLR ligand. A method further comprises pulsing the dendritic cell with a tumor lysate.

Abstract: There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

Abstract: The invention provides a peptide or peptidomimetic that is derived from or based upon the amino acid sequence of the C-terminal ?-helix or hypervariable region (HVR) or a Ras protein, a nucleic acid encoding the peptide or peptidomimetic, and methods employing the same.

Abstract: Cosmetic composition which can be applied topically, comprising at least one compound of the general formula (I) in which R1 is H, C1-C20-alkyl, cycloalkyl or aryl-C1-C4-alkyl, n is 1-4, X is —O—, —NH— or —NR2— and R2H or C1-C20-alkyl; and at least one compound corresponding to the above formula (I) but in which XR1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid; use of these compounds and of the composition for stimulating the synthesis of the proteins of the basement membrane; and also both those compounds of the formula (I) in which X is —NR2— and both R1 and R2 are different from H, and the compounds corresponding to formula (I) but in which XR1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid, as such.

Abstract: The present application relates to novel derivatives of monomethylauristatin F, to processes for preparing these derivatives, to the use of these derivatives for treating and/or preventing diseases, and also to the use of these derivatives for preparing medicaments for treating and/or preventing diseases, more particularly hyperproliferative and/or angiogenic disorders such as, for example, cancerous disorders. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.

Abstract: A peptidic hydrolyzate enriched in bioactive peptides is disclosed that is a proteasome activator. Cosmetic and pharmaceutical compositions are disclosed that include the peptidic hydrolyzate enriched in bioactive peptides in a physiologically acceptable medium. Also disclosed are methods for depigmenting, lightening and/or whitening the skin and treating hyperpigmentation blemishes as well as cutaneous signs due to photo-aging by administering the cosmetic compositions or pharmaceutical compositions.

Abstract: A tri-podal compound according to formula (I) wherein, each Z is the same and is a substituted or unsubstituted N-heteroaromatic single-, multiple-, or fused-ring; and each A is the same, and can represent a direct bond between the cyclohexane ring and Z, or a carboxamide group (—C(O)—N(H)—). Use of the compounds in combinatorial libraries, methods of making the tripodal compounds, sensor devices for detecting carbohydrate targets, and methods of using the tripodal compounds to detect carbohydrate targets in a sample are also disclosed.

Abstract: The present invention relates to process for identifying a compound which induces the mitochondrial permeability transition (MPT) in proliferating cells, wherein said process comprises contacting a cell or cell extract with a compound, determining whether the compound binds to adenine nucleotide translocator (ANT), and determining whether the compound selectively induces the MPT in proliferating cells.

Abstract: A peptide comprising a unit of formula (I) and having a molecular weight of less than 2000 wherein each X is independently an organic group, e.g. a C1-6 alkyl or C1-6 alkenyl group, preferably —CH2—CH?CH2, or the two X groups taken together can form a covalent or non-covalent link between the two O groups, preferably a C1-10 saturated or unsaturated carbon chain optionally interrupted by one or more heteroatoms selected from O, S, N, P, or Si, especially a C3-10 carbon chain or one X represents an azido group and the other an C2-6-alkynyl group; both Z's are the same and are O or S; each Y is independently C, CH, CH2, N or NH; R1 is H or C1-6 alkyl; R2 is H or C1-6 alkyl; R5 is a C1-6 alkyl group, preferably isopropyl; or a salt, ester or prodrug thereof.

Abstract: A compound comprising a peptide moiety comprising, consisting essentially of, or consisting of, the peptide sequence of a tyrosine cluster YC of the BY-kinase of a Gram positive or Gram negative bacteria, or a fragment or an analogue thereof, and an adenine peptide analogue PNA(A), whereas the peptide moiety and the PNA are linked together. The compound is useful as an inhibitor of bacterial tyrosine kinase.

Abstract: Peptides of general formula (I): R1-Wp-Xn-AA1-AA2-AA3-AA4-Ym-R2 their stereoisomers, mixtures thereof, and/or their cosmetically or pharmaceutically acceptable salts, a method of preparation, cosmetic or pharmaceutical compositions containing them and their use for the treatment, prevention and/or care of conditions, disorders and/or diseases of the skin, mucous membranes and/or scalp.