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: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.

Abstract: Disclosed are peptide and peptidomimetic compounds generally according to formula (I) that are useful as GHRP analogs: R1-A1-A2-A3-A4-A5-R2??(I) wherein: A1 is Aib, Apc or Inp; A2 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp; A3 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp; A4 is 2Fua, Orn, 2Pal, 3Pal, 4Pal, Pff, Phe, Pim, Taz, 2Thi, 3Thi, Thr(Bzl); A5 is Apc, Dab, Dap, Lys, Orn, or deleted; R1 is hydrogen, (C1-6)alkyl, (C5-14)aryl, (C1-6)alkyl(C5-14)aryl, (C3-8)cycloakyl, or (C2-10)acyl; and R2 is OH or NH2; and pharmaceutical compositions and methods of use thereof.

Abstract: The present invention provides compositions and methods for imaging, for example, tumor resections.

Abstract: Novel peptidomimetics exhibiting affinity for opioid receptors, possessing general formula show on FIG. 1, for gastrointestinal or peripheral administration in the form of a pill, infusion, injection or implant in the treatment of peripheral opioids side effects, particularly constipation or/and respiratory depression.

Abstract: The present invention is directed to implants and the modification of the surface of implants using amino acid or polypeptide functionalized rosette nanotubes.

Abstract: An immunoconjugate in which a phosphate-prodrugged DNA minor groove binding agent of formula (I), where X is a nucleophilically displaceable leaving group, is conjugated to an antibody or an antigen binding fragment of an antibody, and compounds that can be used for making such immunoconjugates, and uses of such immunoconjugates.

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 disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof. For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant.

Abstract: Structural and functional analysis of peptide inhibitor binding to the cyclin D and cyclin A groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.

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 peptide clearing agent is provided for clearance of a conjugate of an enzyme and a binding molecule which binds specifically at a target location from a non-target location in a subject. The peptide clearing agent binds the active site of the enzyme. The peptide also binds to the asialoglycoprotein receptor expressed by hepatic cells to facilitate clearance through the liver. The peptide may be glycosylated to facilitate clearance through the liver by binding to hepatic cells expressing an asialoglycoprotein receptor. Typically, the peptide prevents or inhibits enzyme activity upon binding to the enzyme and is not substantially modified by the enzyme activity. The peptide may be based upon the dipeptide amino-naphthoic acid (ANA)-glutamate (GIu) and may comprise the amino acid sequence serine (Ser)-Alanine (Ala)-amino-naphthoic acid (ANA)-glutamate (GIu). In such cases, the enzyme of interest is typically CPG2.

Abstract: The present invention relates to novel Motoneuronotrophic Factors (MNTF) peptides and analogs thereof, including compositions capable of promoting the growth and viability of neurons. MNTF peptides between two and six amino acids in length are provided, as well as analogs of these MNTF peptides that are modified by covalent attachment to another moiety. Other embodiments are described herein.

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 invention features methods for identifying compounds that inhibit cell death, and methods for identifying compounds that promote cell death, by blocking or accelerating, respectively, the translocation of the catalytic domain of toxins or transcription factors through the endosomal membrane into the cytosol of a cell. Also featured are methods for inhibiting cell death that include the administration of polypeptides that include a toxin consensus sequence recognized by one or more components of the cytosolic translocation factor complex.

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: 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: This invention relates generally to neuropeptide Y (“NPY”) Y4 receptor agonists including pancreatic polypeptide (PP), analogs thereof, and peptide fragments of PP, e.g. PP(32-36), and analogs thereof, to pharmaceutical compositions containing such Y4 receptor agonists, and to methods for treatment of mammals using the same. The NPY Y4 receptor agonists may be administered to mammals either alone or in combination with NPY Y2 receptor agonists including peptide YY (PYY) (3-36), analogs thereof, and to peptide fragments of PYY(3-36), e.g. PYY(22-36) and PYY(25-36), and analogs thereof, such as to control food intake in mammals, blood pressure, cardiovascular response, libido, circadian rhythm, hyperlipidimia, chronic pancreatitis, and nonalcoholic fatty liver disease including nonalcoholic steatohepatitis.

Abstract: Compositions and/or mixtures comprising peptide amphiphile compounds comprising one or more contrast agents, as can be used in a range of magnetic resonance imaging applications.

Abstract: The present invention describes new compounds (e.g.

Abstract: Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.

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: The present invention relates to a stabilized vitamin C derivative with a peptide molecule linked to vitamin C or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a composition containing the same.

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 present invention relates to methods for searching and identifying absent and rare peptide sequences from public databases and their uses in the treatment of pathological diseases. One embodiment of the present invention provides a method that includes: a) storing, in a memory or storage of a computing device, a set of at least one peptide sequence of fixed length; b) searching, by the computing device, for a peptide sequence from the set within at least one database having naturally-occurring amino acid sequences; and c) classifying, by the number of appearance in the database, the peptide sequence.

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 instant invention provides compositions comprising a prodrug, the prodrug comprising a therapeutically active drug; and a peptide selected from the group consisting of the sequences: Ser-Ser-Lys-Tyr-Gln (SEQ ID NO:1); Gly-Lys-Ser-Gln-Tyr-Gln (SEQ ID NO:2); and Gly-Ser-Ala-Lys-Tyr-Gln (SEQ ID NO:3) wherein the peptide is linked to the therapeutically active drug to inhibit the therapeutic activity of the drug, and wherein the therapeutically active drug is cleaved from the peptide upon proteolysis by an enzyme having a proteolytic activity of prostate specific antigen (PSA). The invention further provides methods of making and using the claimed compositions.

Abstract: A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently a therapeutic agent having a molecular weight ?5 kDa. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

Abstract: The present invention relates to a probe for iFRET and use thereof. Specifically, the present invention relates to a novel probe for iFRET, a method for preparing the probe for iFRET, a method for searching a target protein-specific binding site or a molecule having the binding site using the probe for iFRET, and a method for imaging the target protein using the probe for iFRET. The probe for iFRET according to the present invention utilizes an amino acid in a protein as a fluorescent donor, unlike the conventional FRET method. Therefore, only one fluorescent material is used, and its emission wavelength is distinct from the intrinsic fluorescence of the protein. Thus, high specificity and sensitivity are ensured, and the quantity, activity and mechanism of various proteins can be analyzed in an easy and accurate manner.

Abstract: Disclosed are specific binding agents such as antibodies and chimera that bind to JAM-like protein. Also disclosed are heavy chain fragments, light chain fragments, and CDRs of the antibodies, as well as methods related thereto.

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 invention is directed to the cosmetic use of tetrapeptides according to formula (I) R1-Val-Leu-Leu-Lys-R2 (I) wherein R1 is linked to the NH2-terminal group of the peptide and is chosen from the group consisting of —H, a linear saturated or unsaturated or branched saturated or unsaturated acyl group having 1 to 24 carbon atoms, which may be functionalized by a —OH, —SH, —COOH or —CONH2 group wherein R2 is the terminal carboxylic group of the peptide either as —COOR3 or —CO—NH2, and wherein R3 is chosen from the group consisting of —H, a linear saturated or unsaturated or branched saturated or unsaturated alkyl group having 1 to 24 carbon atoms, which may be functionalized by a —OH, —SH, —COOH or —CONH2 group. The invention is also directed to the respective tetrapeptides and cosmetic compositions containing these.

Abstract: The invention relates to peptide derivatives of general formula (I): R1-AA1-AA2-R3-AA4-R2??(I) their stereoisomers, mixtures thereof, and their cosmetically or pharmaceutically acceptable salts, a method for obtaining them, cosmetic or pharmaceutical compositions containing them and their use for the treatment, care and/or cleansing of those conditions, disorders and/or pathologies of the skin, mucosae, scalp and/or nails resulting from microorganism proliferation or being at risk of microorganism proliferation.

Abstract: There is provided a lipid peptide that is capable of forming a hydrogel with an extremely small amount thereof over a liquid property range from acidic to alkaline, and a hydrogel having high environmental suitability, biocompatibility and biodegradability. A lipid peptide represented by Formula (1): where R1 represents an aliphatic group having 9 to 23 carbon atoms; R2, R3, R4 and R5 independently represent a hydrogen atom, an alkyl group having 1 to 7 carbon atom(s) which optionally has a branched chain having 1 to 3 carbon atom(s), a phenylmethyl group, a phenylethyl group or a —(CH2)n—X group, and at least one of R2, R3, R4 and R5 represents a —(CH2)n—X group; n represents the number of 1 to 4; X represents a guanidino group, a —CONH2 group or a 5-membered ring, a 6-membered ring or a fused heterocyclic ring composed of a 5-membered ring and a 6-membered ring which optionally have 1 to 3 nitrogen atom(s); and m represents 1 or 2, and a hydrogel comprising the lipid peptide.

Abstract: A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently a therapeutic agent having a molecular weight ?5 kDa. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

Abstract: The present invention provides a method for producing a peptide, characterized in that it comprises converting an —SH group of a peptide comprising an amino acid residue having the —SH group to an —OH group, wherein said method comprises the following steps (a) to (c): (a) allowing an —SH group in a peptide to react with a methylating agent to convert the —SH group to an -SMe group; (b) allowing the -SMe group obtained in the step (a) to react with a cyanizing agent to produce a reaction intermediate; and (c) converting the reaction intermediate obtained in the step (b) to a peptide comprising an amino acid residue having an —OH group under more basic conditions than the conditions in the step (b).

Abstract: Disclosed is a general methodology to create nanofibers of therapeutic molecules that have a dual role, as both the delivery vehicle and the drug itself. It is shown that with proper molecular design, the integration of enzymatic reaction and self-assembly provides a powerful method to create molecular hydrogels of clinically-used therapeutics without compromising their bioactivities. In addition, the results disclosed herein demonstrate enzyme-instructed self-assembly as a facile strategy for generating the supramolecular hydrogels of molecules that inherently have poor solubility in water. For example, by covalently connecting paclitaxel with a motif that is prone to self-assemble, a hydrogel of paclitaxel can be formed without compromising the activity of the paclitaxel.

Abstract: The invention relates to novel peptidase substrates of formula (I): wherein R0, R1, R2, R3, R4, R5 and n are as defined in claim 1, and a method for detecting the presence of a catalytically active peptidase, by means of one of these substrates.

Abstract: Peptide compounds of the following general formula (I): R1-(AA)n-X1-X2-X3-Lys-Lys-Gln-Lys-Trp-X4-(AA)p-R2 are disclosed herein. The peptide compounds can be used as Telomeric repeat-binding factor 2 (TRF2) protein-modulating compounds and have a preventive action on deoxyribonucleic acid (DNA) double-strand breaks. In addition, cosmetic compositions that include at least one peptide of general formula (I) in a physiologically acceptable medium are disclosed along with methods for preventing and/or treating cutaneous signs of aging and photoaging.

Abstract: The invention relates to a compound having a structure according to the general formula P3-P2-P1-P1?-P2? (I), wherein residues P3, P2, P1, P1? and P2? are specifically defined and may be, e.g., certain amino acid residues. The invention further relates to the use of said compound and to a method for synthesizing a peptide.

Abstract: The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted ? amino acid, each of the substituting groups in the ? amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.

Abstract: Auristatin compounds and conjugates thereof are provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently an Auristatin compound. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

Abstract: New peptides activating extracellular matrix protein synthesis in the skin, a cosmetic composition that includes such peptides as an active agent, and cosmetic care methods intended to delay or treat cutaneous signs of aging and photoaging by applying such peptides and/or cosmetic compositions are described.

Abstract: Tubulysin compounds of the formula (I) where R1, R2, R3a, R3b, R4, R5, W, and n are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.

Abstract: Tubulysin compounds of the formula (I) where R1, R2R3a, R3b, R4, R5, W, and n are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.

Abstract: Provided herein are compositions and kits comprising a therapeutic agent linked to a cleavable substrate, wherein the cleavable substrate is capable of being cleaved by cathepsin E. Also provided are methods of treating one or more symptoms of a disease or disorder characterized by expression of cathepsin E in a subject and methods of eliminating a cancer cell characterized by expression of cathepsin E using the provided compositions and kits. Further provided herein are methods of detecting the presence of a cancer cell or detecting a cathepsin E expressing cell using a photosensitizer linked to a cleavable substrate, wherein the cleavable substrate is capable of being cleaved by cathepsin E.

Abstract: Provided herein are compounds that inhibit a binding interaction between a ? integrin and a G protein subunit, as well as compositions, e.g., pharmaceutical compositions, comprising the same, and related kits. In some embodiments, the compound is an antibody or antibody analog, and, in other embodiments, the compound is a peptide or peptide analog. Also provided are methods of using the compounds, including methods of treating or preventing a medical condition, such as stroke, heart attack, cancer, or inflammation.

Abstract: The present invention relates to a proteinaceous extract derived from tortoise spleen and to a tetrapeptide FTGN, which have stimulatory activity on hematopoietic cells. In particular, this tetrapeptide enhances hemopoietic reconstruction, and bone marrow re-population, reduced as a consequence of a high dose of radiation or chemotherapy exposure. The invention further provides pharmaceutical compositions comprising as an effective ingredient the proteinaceous extract or the FTGN tetrapeptide and ex vivo and in vivo methods of treatment employing them.

Abstract: Potent compounds having combined antioxidant, anti-inflammatory, anti-radiation and metal chelating properties are described. Short peptides having these properties, and methods and uses of such short peptides in clinical and cosmetic applications are described.

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.