Abstract: Peptide ligands for transporting therapeutic agents across the intestinal epithelial barrier that ordinarily are inadequately absorbed and must be delivered by alternative means, which contain an isolated amino acid sequence wherein at least one pair of amino acids are of an opposite charge and the pair members are separated by a spacer of 1-12 amino acid residues including at least one hydrophobic amino acid, and wherein the length of the amino acid sequence is greater than 5 and less than 20 amino acids. Pharmaceutical compositions for gastro-intestinal delivery and methods for the gastrointestinal delivery of poorly absorbed therapeutic agents are also disclosed.

Abstract: Methods of using halogenated peptides as internal standards for liquid chromatography-mass spectrometry, and novel halogenated peptides useful for the same, are disclosed. In particular, methods of using halogenated peptides as internal standards in proteomic analyzes, as well as methods of using halogenated peptides to conduct quality control assessments of and/or to calibrate liquid chromatography-mass spectrometry systems are disclosed.

Abstract: The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18 (SEQ ID NO: 93), wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15, A16, A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —(O)C1-C20alky or a diaminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.

Abstract: The present invention provides branched amphipathic peptides and vesicles formed thereof. The peptides comprise a polar/positively charged C-terminal segment, a branch point, and two hydrophobic N-terminal segments extending from the branch point. The vesicles are formed using a plurality of first and second peptides, wherein the first peptide has a different chain length from the second peptide. When a plurality of the first and second peptides are mixed together, they self-assemble to form small spheres defined by a membrane consisting of an interlocking peptide network bilayer and having a liquid-receiving interior space (i.e., hollow core). In the bi-layer, the respective hydrophobic segments of the peptides form beta-sheet structures having a hydrogen bond-stabilized, anti-parallel orientation in which the opposed sequences interlock to form a zipper-like structure in three dimensions. Thus, the peptide assembly (i.e.

Abstract: The method for producing a surfactin or a salt thereof according to the present invention comprises the steps of adding an organic solvent containing a branched alkyl alcohol to a culture fluid containing the surfactin or the salt thereof, or to a solution obtained by removing an insoluble component from the culture fluid, and extracting the surfactin or the salt thereof with the organic solvent, wherein the surfactin or the salt thereof is represented by the formula (1): wherein * indicates an optically active center; X is an amino acid selected from leucine, isoleucine and valine; R is a C9-13 alkyl group or a C9-13 branched alkyl group; and M is an alkali metal, an alkaline earth metal, an optionally-substituted amine or the like.

Abstract: Disclosed herein are compositions and methods for generating ribo-nucleic neutral (RNN) or deoxyribo-nucleic-neutral (DNN) polynucleotides with reduced anionic charge, for improved intracellular delivery. Also disclosed herein are methods of using RNN and DNN compositions.

Abstract: Methods of restoring the circadian rhythm and resynchronizing the biological clock of cells are described. The methods include topically applying a topical composition comprising a cosmetically acceptable medium and an effective quantity of a peptide compound of general formula (I), R1-(AA)n-X1-Ser-Thr-Pro-X2-(AA)p-R2, to skin or skin appendages to be treated.

Abstract: Provided are fragments of human p97 (melanotransferrin) polypeptides having blood-brain barrier (BBB) transport activity, including variants and combinations thereof, conjugates comprising said p97 fragments, and related methods of use thereof, for instance, to facilitate delivery of therapeutic or diagnostic agents across the BBB.

Abstract: Compositions and methods are provided for eliciting antigen-specific T-cell responses against human cyclin A1 (CCNA1), which is herein identified as a leukemia-associated antigen based on its overexpression in acute myeloid leukemia (AML) including leukemia stem cells (LSC) and in immunologically privileged testis cells, but not in other normal cell types. CCNA1-derived peptide epitopes that are immunogenic for T-cells including CTL are disclosed, as are immunotherapeutic approaches using such peptides for vaccines and generation of adoptive transfer therapeutic cells.

Abstract: The present invention refers to a peptide of general formula (I) R1-Wn-Xm-AA1-AA2-AA3-AA4-AA5-AA6-Yp-Zq-R2, cosmetic compositions which comprises said peptide, method of preparation of said peptides and its use in the treatment and/or prevention of itching, inflammation, pain, diseases and/or disorders of the respiratory airways.

Abstract: A peptide composition is provi'deo!which specifically inhibits the ability of ? protein kinase C (?PKC) to phosphor/late pyruvate dehydrogenase kinase (PDK) under ischemic conditions. The peptide composition is useful for treating or reducing tissue damage resulting from ischemia and/or reperfusion.

Abstract: The present invention relates to compounds which bind to Beta Trans-ducin repeat-containing protein (PTrCP), and modulate the activity of 13TrCP. In particular, the invention relates to compounds which demonstrate optimised binding to PTrCP. The invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds as medicaments, specifically for the treatment of disorders associated with aberrant protein degradation, such as cancer. The preferred binding inhibitors are peptides derived from the motive DSGXXS, e.g. DEGFWE, DDGFWD and Succinyl-EGFWE.

Abstract: A series of integrin blockers that present strong angiogenesis inhibiting performance, high integrin affinity and integrin-bonding capacity is provided. This series of integrin blockers can be adopted in treatment of solid tumors and rheumatoid arthritis. Specifically, said series of integrin blockers include polypeptide I, polypeptide II and polypeptide III (see SEQ ID NO. 1, SEQ ID NO. 2 and SEQ ID NO. 3) that can be adopted in treatment of solid tumors and rheumatoid arthritis. This invention also relates to application of these three integrin-blocking polypeptides in preparation of anti-tumor drugs, wherein the tumors that can be treated include those primary or secondary cancers originated from head and neck region or other organs such as brain, thyroid, esophagus, pancreas, lung, liver, stomach, breast, kidney, gallbladder, colon, rectum, ovary, cervix, uterus, prostate, bladder and testicle, as well as melanoma and sarcomas.

Abstract: The subject of the present invention are peptide preparations obtained via the enzymatic digestion of hair, wool, bristles, animal fur and individual peptides with sequences corresponding to individual components of a peptide preparation with antitumour activity, for use in the treatment of tumours or oncological prophylaxis as basal components or components of compositions of substances for treating tumours or components of substances used in oncological prophylaxis.

Abstract: The present invention relates to an antibacterial and fungicidal peptide in which a lysine and tryptophan dipeptide is repeated. More specifically, the antibacterial and fungicidal peptide of the present invention, in which lysine and tryptophan dipeptide is repeated four times, shows excellent antibacterial activities with respect to gram-positive bacteria, gram-negative bacteria and antibiotic-resistant strains by affecting the inner membrane of harmful microorganisms, has remarkable fungicidal activities with respect to pathogenic fungi and antibiotic-resistant fungi, and shows little cytotoxicity, and thus can be useful for a pharmaceutical composition, a cosmetic composition, agricultural chemicals, a food preservative, a cosmetic preservative, and a pharmaceutical preservative.

Abstract: A DPP-4 inhibitor comprising a peptide represented by the formula (1): Xe-Pro/Ala/Hyp-Xa-Xb-Xc-Xd (wherein Xe is an amino acid residue with an isoelectric point of 5.9 to 6.3; Pro/Ala/Hyp represents Pro, Ala, or Hyp; Xa is an amino acid residue other than Hyp, Pro, and Arg, or deletion; Xb is Gly, Pro, or deletion; Xc is Pro, Ala, or deletion; and Xd is an amino acid residue or deletion) as an active component. The inhibitor can be expected to bring out an effect of lowering blood glucose levels by enhancing effects of incretins; and the inhibitor may be used as a therapeutic agent for diabetes and, in addition, can act on the immune system or the like to be thus used in treatment for skin diseases or the like.

Abstract: The present invention concerns methods and compositions that employ peptides that target dorsal root ganglion (DRG) neurons. In particular, the peptides are used to target therapeutic agents, such as proteins, liposomes, or viral particles comprising therapeutic polynucleotides, to one or more peripheral neuropathies or neuropathic pain, for example. In particular cases, the peripheral neuropathies or neuropathic pain is caused directly or indirectly by DRG neuronopathy.

Abstract: It is an object of the present invention to provide improved pharmacological properties to molecules which bind to a target with low affinity (hereinafter referred to as a “ligand moiety”) through linkage of such molecules to a metal binding moiety, thereby generating a combination molecule commonly referred to as a “metallodrug” or “metallotherapeutic.” The metal binding domain of metallodrugs typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, resulting in modification of proteins and nucleic acids that are in close proximity due to binding of the ligand moiety to its target.

Abstract: The present disclosure relates generally to epitopes of an antibody known as PAT-LM1, and methods for using said epitopes.

Abstract: The present application provides stable peptide-based Akt capture agents and the use thereof as detection, diagnosis, and treatment agents. The application further provides novel methods of developing stable peptide-based capture agents, including Akt capture agents, using iterative on-bead in situ click chemistry.

Abstract: Substrates for detecting microorganisms are provided, wherein the substrate comprises a set of molecular markers linked, optionally with linker molecules or moieties, to a di-, or tripeptide consisting of amino acids X1 and X2, or X1, X2 and X3, in which one of them, for example, X1, is a D-amino acid and the others, for example, X2 and X3, may be any D- or L-amino acid. The substrate preferably is used for the detection of Bacillus anthracis. Also provided are substrates for detecting Pseudomonas aeruginosa, wherein the substrate comprises a set of molecular markers linked, optionally with linker molecules or moieties to a tri-, tetra-, or pentapeptide consisting of glycine amino acids. The invention further comprises methods for detecting microorganisms, specifically B. anthracis and P. aeruginosa, with the substrates of the invention and use of the substrate(s) in such a method.

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: The present invention relates to compounds which bind to the hydrophobic pocket of the ? clamp, i.e., to the surface of the ? ring with which said protein interacts with other proteins of the bacterial replication complex during DNA replication. These compounds are derived from the acetylated peptide AcQLDLF (P6) to improve their affinity to their target.

Abstract: The present disclosure is directed to peptide-based compounds, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present disclosure may inhibit neurotransmitter release and muscle contraction as a treatment for wrinkles. The compounds of the disclosure may be used for pathological neuronal exocytosis-mediated cosmetic and/or therapeutic purposes.

Abstract: A non-radioactive, ultrasensitive methodology for the quantification of protein kinase catalytic activity of any protein kinase in, for example, biological/clinical samples or recombinant/purified proteins, based on using near-infrared-fluorescence (NIRF)-labeled peptide substrates that are selective for individual protein kinases and using a combination of kinase-selective inhibitors to define the catalytic activity of individual protein kinases, including but not limited to, a substrate for phosphorylation by a protein kinase comprising a core peptide having the formula: (N-terminus)-Arginine-Lysine-Arginine-Serine-Arginine-Lysine-Glutamic-acid-(C-terminus); and an indicator component covalently bonded to the core peptide.

Abstract: The present invention relates to adjuvant compositions, vaccine compositions, and methods of enhancing an immune response to an antigen.

Abstract: Polymeric conjugates comprising a polymeric backbone having attached thereto a bone targeting moiety and a therapeutically active agent, wherein the bone targeting moiety is attached to one end of the polymeric backbone via a branching unit such that a molar ratio of the bone targeting moiety to the polymer is at least 2:1, are disclosed. Pharmaceutical compositions containing these conjugates and uses thereof in the treatment of bone related disorders are also disclosed.

Abstract: The invention is based in part on identifying a core region of ND2 responsible for interacting with Src to within residues 289-321 of ND2 and more particularly residues 307-321 or 310-321 of ND2. Peptides including, overlapping or from within this region can be used to inhibit ND2 interaction with Src Inhibition of this interaction is useful for treatment or prophylaxis of neurological diseases and disorders, pain and cancer.

Abstract: The present disclosure provides peptides and constructs that inhibit mitochondrial fission, and compositions comprising the peptides or constructs. The present disclosure provides methods of reducing abnormal mitochondrial fission in a cell. Also provided are methods for designing and validating mitochondrial fission inhibitor constructs and peptides, including but not limited to, evaluating the effects of the constructs and peptides on Drp1 GTPase activity, binding of Drp1 to Fis1, reduction of mitochondrial damage, reduction in cell death, inhibition of mitochondrial fragmentation in a cell under pathological conditions, and reduced loss of neurites in primary dopaminergic neurons in a Parkinsonism cell culture.

Abstract: The present invention concerns antibodies recognizing Mycobacterium avium paratuberculosis epitopes able to cross-reacting with the beta-cell antigen ZnT8 to be used as early biomarkers of type 1 diabetes, epitopes for in vitro prognostic and diagnostic methods suitable to reveal a risk to develop type 1 diabetes, therapies for the prevention of T1D by avoiding, controlling or monitoring Mycobacterium paratuberculosis infection.

Abstract: Novel peptoid oligomers are disclosed that have a formula represented by the following formula I: wherein R1 and n are as described herein. The peptoids demonstrate antimicrobial and antimalarial activity and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals including humans where microbial or malarial infection is involved. The present cyclic peptoids are particularly valuable as their effect is rapid, broad in spectrum and mostly indifferent to resistance provoked by standard antibiotics.

Abstract: The disclosure provides for one or more peptoids, methods of manufacture thereof, and methods of use thereof, including the use of one more peptoids in neutralizing the anticoagulant activity of heparin.

Abstract: The disclosure provides for one or more peptoids, methods of manufacture thereof, and methods of use thereof, including the use of one more peptoids in neutralizing the anticoagulant activity of heparin.

Abstract: Isolated peptides, compositions and methods of use for treating tumors infiltrated with macrophages, such as glioblastomas.

Abstract: An isolated antibody that has a specific binding affinity to a polypeptide comprising the amino acid sequence HTEGKP (SEQ ID NO: 2) phosphorylated at threonine is provided. The antibody may be used as biomarker for mitotic cells. A method for using the antibody in accordance with the invention comprises contacting a cell with the antibody and detecting antibody bound to the cell as an indicator of the cell being in the mitotic state. A reagent kit comprising the antibody is also provided.

Abstract: Described herein are compositions and methods for cancer cell biomarkers, such as pancreatic ductal adenocarcinoma (PDAC) cell biomarkers, and binding molecules for diagnosis and treatment of cancer, e.g., PDAC. Methods of identifying “accessible” proteomes are disclosed for identifying cancer biomarkers, such as plectin-1, a PDAC biomarker. Additionally, imaging compositions are provided comprising magnetofluorescent nanoparticles conjugated to peptide ligands for identifying PDACs.

Abstract: The present invention is directed to C-type lectin-like molecule-1 (CLL1) specific ligand peptides, comprising the amino acid motif LR(S/T), and methods of their use, e.g., for imaging detection for diagnosis of leukemia and the presence of leukemic stem cells (LSCs) and targeted therapy against leukemia mediated at least in part by CLL1-expressing LSCs.

Abstract: The present invention concerns methods and compositions that employ peptides that target dorsal root ganglion (DRG) neurons. In particular, the peptides are used to target therapeutic agents, such as proteins, liposomes, or viral particles comprising therapeutic polynucleotides, to one or more peripheral neuropathies or neuropathic pain, for example. In particular cases, the peripheral neuropathies or neuropathic pain is caused directly or indirectly by DRG neuronopathy.

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. The compounds provided herein can in other embodiments overcome the resistance conferred by single amino acid mutations at defined positions of bacterial Signal Peptidases (SPases) and in other embodiments provide for a broader spectrum of antibiotic bioactivity compared to the natural product. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

Abstract: A process for chemically converting a peptide chain into a peptide thioester includes, when a —C(?X)—R1 group is introduced to the thiol group of the cysteine residue and then the resulting peptide is reacted with a compound having a leaving group represented by the formula: —NH—C(?Y)NHR3 in an organic solvent, the —NH—C(?Y)NHR3 group binds via addition reaction to the carboxyl group of the N-terminal-side peptide bond of the cysteine residue, whereby the peptide bond is cleaved and the C-terminal-side peptide fragment is cut off. Further, when the resulting peptide chain having the —NH—C(?Y)NHR3 group is reacted with a thiol in a buffer solution, a thiol exchange reaction occurs, namely, the thiol group of the thiol binds to the carbonyl carbon to which the —NH—C(?Y)NHR3 group has bound, whereby the —NH—C(?Y)NHR3 group is eliminated.

Abstract: The invention provides methods and mass-labeled peptides for use in said methods for quantifying the presence of a one or more viral proteins in a sample of a preparation containing agents which bind to said viral protein, using mass-spectroscopic analyses of the sample and standards containing known amounts of labeled and unlabeled signature peptides, in particular wherein said viral proteins are antigens in a vaccine for porcine circovirus.

Abstract: The invention provides cyclo[{4-(NH2—C2H4—NH—CO—O-)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.

Abstract: A conjugated compound of Formula I: Q-Z—R4 wherein Q is a TLR7 and/or TLR8 agonist and Z—R4 is a TLR2 agonist, the conjugated compound being chosen among compounds of Formula II:

Abstract: The present invention relates to means and methods to protect against disease caused by bacteria belonging to the genus Chlamydia. In particular, the present invention relates to isolated B- and T-cell epitopes derived from the major outer membrane protein of Chlamydia psittaci which can be used against an infection with a species of the genus Chlamydia. More in particular, the invention provides a vaccine which can be used against chlamydiosis caused by Chlamydia psittaci in birds and man. In addition, the invention relates to a diagnostic method to diagnose the latter infections.

Abstract: An immunoglobulin binding peptide having the general formula, from amino terminus to carboxy terminus, of Z—R1—R2—R3—R4—R5—R6—X, is described, wherein: R1 is H or Y; R2 is a hydrophobic, preferentially aromatic, amino acid (for example W, F, Y, V); R3 is a positively charged or aromatic amino acid (for example R, H, F, W); R4 is a hydrophobic or positively charged amino acid (for example G, Y, R, K, L); R5 is a positively charged or aromatic amino acid (for example W, F, R, H, Y); R6 a random amino acid but preferably hydrophobic or negatively charged (for example V, W, L, D, H); X is present or absent and when present is a linking group; and Z is present or absent and when present is a capping group bonded to the N terminus of R1; and wherein the amino acids of said peptide are in D form, L form, or a combination thereof.

Abstract: The invention is directed to peptides. Specifically, the invention is directed to peptides which bind skin and do not bind hair. Alternatively, the invention is drawn to peptides which bind hair and do not bind skin.

Abstract: Provided is a family of intramolecularly quenched imaging agents for use in both in vivo and in vitro imaging that contain at least one enzymatically cleavable oligopeptide and two fluorophores or a fluorophore and a quencher. When subjected to proteolytic cleavage, at least one fluorophore is unquenched and becomes capable of producing a fluorescent signal upon excitation with light of an appropriate wavelength. Also provided are in vivo and in vitro imaging methods using such imaging agents.

Abstract: The instant invention relates to peptides obtained from the enzymatic hydrolysis of yellow pea seed proteins that are capable of lowering the blood pressure and reducing the effects of kidney disease in a subject by inhibiting or reducing the affinity of the enzymes in the renin-angiotensin system for their substrates, specifically renin, to compositions comprising said peptides and to uses thereof.

Abstract: The invention provides methods and compositions for modulating the Wnt signaling pathway, in particular by interfering with binding of Dkk1 or SOST with LRP5 and/or LRP6.

Abstract: The present invention provides the use of hepatitis C virus immunogenic peptides or derivative thereof in the manufacture of a pharmaceutical for preventing or treating arthritis, wherein the peptide or derivative thereof is a peptide represented by formula I or pharmaceutically acceptable salt or ester thereof. The present invention further provides a method for treating arthritis, including administering a pharmaceutical containing therapeutically effective amount of said peptide or derivative thereof to a patient. Xaa1-Gln-Xaa2-Xaa3-Thr-Ser-Gly-Xaa4 (formula I), wherein, Xaa1 is deleted, or Xaa1 is Ala, Gly, Val, Leu or Ile, Xaa2 is Thr or Ser, Xaa3 is Tyr, Phe or Trp, and Xaa4 is deleted, or Xaa4 is Ala, Gly, Val, Leu, Ile or Pro.