Abstract: A heparin-binding growth factor (HBGF) analog having two substantially similar sequences (homodimeric sequences) branched from a single amino acid residue, where the sequences are analogs of a particular HBGF that binds to a heparin-binding growth factor receptor (HBGFR), or alternatively that bind to a HBGFR without being an analog of any particular HBGF. The homodimeric sequences may be derived from any portion of a HBGF. The synthetic HBGF analog may be an analog of a hormone, a cytokine, a lymphokine, a chemokine or an interleukin, and may bind to any HBGFR. Further provided are preparations for medical devices, pharmaceutical compositions and methods of using the same.

Abstract: The invention relates to truncated GLP-1 analogues, in particular a GLP-1 analogue which is a modified GLP-1(7-35) (SEQ ID No 1) having: i) a total of 2, 3, 4, 5 6, 7, 8, or 9 amino acid substitutions as compared to GLP-1(7-35), including a) a Glu residue at a position equivalent to position 22 of GLP-1(7-35), and b) an Arg residue at a position equivalent to position 26 of GLP-1(7-35); as well as derivatives thereof, and therapeutic uses and compositions. These analogues and derivatives are highly potent, have a good binding affinity to the GLP-1 receptor, also to the extracellular domain of the GLP-1 receptor, which is of potential relevance achieving long-acting, stable GLP-1 compounds with a potential for once weekly administration.

Abstract: The present invention features HCV NS3 protease substrates containing a europium label and a quenching group. The europium label and quenching group are located on different sides of an ester HCV NS3 protease cleavage site. The substrate can be used in a time-resolved fluorescence (TRF) assay to measure HCV protease activity.

Abstract: Disclosed is a PNA probe that includes a nucleobase sequence suitable for the detection, identification and/or quantitation of Pseudomonas (sensu stricto). In one embodiment, the PNA probe is complementary to a target sequence of 23S rRNA or rDNA from all species of the genus Pseudomonas. The invention has a wide range of important uses including detecting Pseudomonas in a sample of interest.

Abstract: The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Hemoglobin (HBF/HBG), in particular, by targeting natural antisense polynucleotides of Hemoglobin (HBF/HBG). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of HBF/HBG.

Abstract: The present invention relates generally to branched macromolecules and their use as imaging or contrast agents. In particular, the invention relates to dendrimers, derived from lysine or lysine analogues, bearing a plurality of functional moieties and their application to imaging techniques in which a disease state may be imaged with a targeted contrast agent.

Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

Abstract: The present invention relates generally to the field of immunotherapy, and more particularly to immunomedicaments in the form of lipopeptides which induce an antibody response to drugs of dependence, and uses thereof in the treatment and prevention of drug addiction.

Abstract: The present invention features a compound having the formula A-X—B, where A is peptide vector capable of enhancing transport of the compound across the blood-brain barrier or into particular cell types, X is a linker, and B is a peptide therapeutic selected from the group consisting of neurotensin, a neurotensin analog, or a neurotensin receptor agonist. The compounds of the invention can be used to treat any disease in which increased neurotensin activity is useful and can be used to induce hypothermia or analgesia.

Abstract: The disclosure relates to compounds of the formula (I): wherein R1, R2, R3, and R4 are as defined in the disclosure, or a pharmaceutically acceptable salt thereof; which is formed by the microorganism ST 201196 (DSM 18870); the use thereof for the treatment and/or prophylaxis of fungal disorders; medicaments containing a compound of formula (I); processes for production thereof; and the microorganism ST 201196 (DSM 18870).

Abstract: The present invention provides antineoplastic peptides of formula I, R1R2N—CHX—CO—A—B-D-E-(G)s-K wherein R1, R2, X, A, B, D, E, G, K and s have the meanings stated in the description. The compounds have antineoplastic activity.

Abstract: The present invention relates to a method for preparing a peptide having a stable, internally constrained alpha-helical, beta-sheet/beta-turn, 310-helical, or pi-helical region and a method of stabilizing an alpha-helical, beta-sheet/beta-turn, 310-helical, or pi-helical region within a peptide structure. The resulting peptides and methods of using them are also disclosed.

Abstract: The present invention relates to a method for preparing an protein monolayer using a peptide hybrid for protein immobilization, more precisely a peptide hybrid for protein immobilization which has improved solubility by introducing a PEG linker and a proper reaction group to the oligopeptide having specific affinity to selected types of proteins and is designed to provide enough space between solid substrates and proteins immobilized, whereby various solid substrates treated by the hybrid catch specific proteins effectively on. The peptide hybrid for protein immobilization of the present invention facilitates the control of orientation of an antibody on various solid surfaces and immobilization of various antibodies of different origins or having different isotypes with different affinity. Therefore, the surface treatment technique using the peptide hybrid of the invention can be effectively used for the production of various immunosensors and immune chips.

Abstract: Growth factor binding molecules having a plurality of peptide loops attached to a non-peptide organic scaffold, preferably having pseudo-six amino acid peptide loops with four amino acid sidechains. The growth factor binding molecules specifically bind various growth factors and are suitable for treating a subject having tumors or restinosis. In one embodiment a platelet-derived growth factor binding molecule is disclosed that is used to inhibit tumor growth and angiogenesis in solid tumors.

Abstract: The present invention relates to a polypeptide carrying a human BNP(I-32) epitope according to Formula (I): a1-R1-X1-FGRKMDR-X2-R2-a2 as well as ligands specific of the FGRKMDR epitope.

Abstract: An azapeptide derivative of growth hormone releasing peptide (GHRP) of Formula I: A-(Xaa)a-N(RA)—N(RB)—C(O)-(Xaa?)b-B which binds to CD 36.

Abstract: Provided herein are biodegradable copolymers and nanoplex delivery systems comprising the same and a cargo molecule, such as a nucleic acid, a polynucleotide or other biomolecule. The biodegradable copolymers may comprise a reducible polymer linearly modified with lysine, such as a linear lysine-modified N,N?-cystamine bisacrylamide. The biodegradable copolymers also may be conjugated to a sequestering moiety, such as dietheylamine. The biodegradable copolymers also may comprise one or both of a targeting moiety and one or more moieties to facilitate endosomal escape. Also provided are methods for treating a pathophysiological condition and for increasing biocompatibility of a polymeric delivery system upon delivery to a subject using the biodegradable copolymers and nanoplexes.

Abstract: The present invention is directed to cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity, preferably Kitastatin 1. The present invention is further directed to methods of inhibiting cancer cell growth and/or microbial growth in a host inflicted therewith by administering cyclodepsipeptide compounds to the inflicted host.

Abstract: The invention provides conjugates, comprising an organ, tissue or tumor cell homing molecule linked to a moiety. Such a moiety can be, for example, an oligonucleotide, small interfering RNA, gene, virus, protein, pharmaceutical or detectable agent. In addition the invention provides methods to diagnose or treat neuronal or neuromuscular disease, or a pathology of the brain, or a tumor of neuronal or neuroectodermal origin, by administrating to a subject having or suspected of having a pathology a molecule or conjugate that homes to, binds to and is taken up by the brain cells or neuronal cells, or by the tumor cells of neuronal or neuroectodermal origin. The invention also provides a method of identifying and measuring neurite growth in neuronal cells.

Abstract: A class of macrocyclic compounds of formula (I), wherein R1, R3, R4, Ra, Rb, A, Z, Y, X, M, W, n and m are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes 5 for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.

Abstract: The present invention relates to novel lipopeptide compounds, pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The compounds of the invention are particularly useful against a variety of bacteria, including resistant strains. The compounds are useful as antibacterial agents against Clostridium difficile.

Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

Abstract: The invention relates to cysteine containing peptides of the structure XXCCXXXXXXXCXXXCXXXXXXQXXCXXXCXCXXXXXXXCXXXXXX, of the structure XXCCXXXXXXXCXXXCXXXXXXXXXCXXXCXCXXXXTXXCXXXXXX and of the structure XXCCXXXXXXXCXXXCXXXXXXXXXXCXXXCXCXXXXXXXXCXXXXXX, wherein X, independently of one another, represents any naturally occurring amino acid, as well as to nucleic acid sequences encoding said peptides, to vectors comprising said sequences, as well as to pharmaceutical compositions containing said peptides and their use as pharmaceutics, particularly for the treatment of cancers.

Abstract: The synthesis, biological evaluation, and molecular modeling of alkoxysuccinyl-peptidyl-haloalkyl ketones for use as proteinase K inhibitors are described. Sample preparation processes for in situ RNA or DNA analysis using such inhibitors, methods and compositions therefor are provided.

Abstract: Supravalent peptide compounds depicting enhanced efficacy, and which comprise at least bivalent peptide units that bind to a receptor target and are connected to a polymeric carrier unit are disclosed herein.

Abstract: Disclosed herein are polypeptide multilayer films comprising a hybrid polypeptide comprising a first polypeptide segment and a second segment, the two segments being covalently joined by one or more non-peptidic linkages. The first segment comprises a polypeptide having a magnitude of net charge per residue of greater than or equal to 0.4, and a length of greater than or equal to about 12 amino acid residues. The second segment comprises a polypeptide or another polyelectrolyte.

Abstract: The present invention provides novel compounds and pharmaceutical compositions containing such compounds, wherein the compounds have affinity for proteoglycans. The compounds comprise an amino acid based core unit linked to positively charged moieties. The compounds further comprise at least one imaging moiety detectable in in vivo imaging making the compounds useful as diagnostic contrast agents for imaging of proteoglycans, such as heparan sulphate proteoglycans.

Abstract: This disclosure relates to compositions for delivering agents to a subject, and in particular, to compositions for delivery of therapeutic agents or diagnostic agents in the presence or absence of targeting moieties. In part, this disclosure relates to compositions comprising a hydrophobic group with a first end and a second end, a first metal binding domain linked to the hydrophobic group, a metal ion capable of being chelated to the first metal binding domain, and an agent linked to a second metal binding domain capable of chelating to the metal ion.

Abstract: The present invention relates to the composition of small molecules and their use in the field of protein isolation, purification, stabilizing and/or enhancing its activity. In particular, the present invention relates to the synthesis and optimization of compounds comprising small peptides and peptide derivatives with affinity to coagulation Factor VIII and/or Factor VIII-like polypeptides and/or domains thereof. These compounds are useful for labeling, detecting, identifying, isolating and preferably for purifying, stabilizing and enhancing the activity of Factor VIII, Factor VIII-like polypeptides or domains thereof from physiological and non-physiological solutions comprising same. Further, these compounds may be used as ligands, which bind Factor VIII, Factor VIII-like polypeptides or domains thereof in methods of the present invention.

Abstract: Compounds of the present invention include cell growth inhibitors which are peptides of Formula I, A-B-D-E-F-(G)r-(K)s-L??(I), and acid salts thereof, wherein A, B, D, E, F, G and K are ?-amino acid residues, and s and r are each, independently, 0 or 1. L is a monovalent radical, such as, for example, an amino group, an N-substituted amino group, a ?-hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, or an oximato group. The present invention also includes a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula I in a pharmaceutically acceptable composition.

Abstract: It is provided mimotope receptors and inhibitors that employ peptide mimics that mimic the shape and function of natural receptors and ligands, thus providing synthetic binding sites for ligands and receptors. Receptor mimics can be attached to carriers, such as liposomes, to act as synthetic platelets, for example, by providing multiple binding sites for binding to other (natural or synthetic) platelets or to the endothelium. Synthetic platelets would have virtually limitless shelf life and would not require disease screening prior to transfusion, thereby providing a solution to the perpetual platelet shortages, as well as the safety and storage issues associated with natural blood platelets.

Abstract: The invention relates to aplidine derivatives of the general formula: which are useful for the treatment of tumors.

Abstract: This invention relates to a peptide or polypeptide (a) which is esterified or thio-esterified (i) at the carboxylate of the C-terminus with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulthydryl group; (ii) at a side-chain carboxylate of one or more Asp or GIu residues, if present, with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulfhydryl group; (iii) at a hydroxyl group of one or more Ser, Thr or Tyr residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; (iv) at a sulthydryl group of one or more Cys residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; and/or (v) at the N-terminus with a guanidinium alkanoi

Abstract: The present invention relates to prokaryotic ubiquitin-like protein (Pup) nucleic acid sequences and Pup amino acid sequences encoded therefrom. Also encompassed are antibodies that are immunologically specific for Pup. Methods directed to isolation and identification of pupylated substrates that utilize the conjugated Pup as an affinity tag are also included. Pupylated substrates that are identified using the method and reagents of the present invention provide tools useful for the identification of additional components of prokaryotic proteasomal machinery. Modulators of Pup activity and methods for identifying such modulators are also encompassed herein.

Abstract: Compounds which are Spiruchostatin analogues of the general formula (I) or (I?), isosteres thereof and pharmaceutically acceptable salts thereof are found to inhibit HDAC wherein R1, R2, R3 and R4 are the same or different and represent an amino acid side chain moiety and each R6 is the same or different and represents hydrogen or C1-C4 alkyl.

Abstract: The present invention relates to tamandarin and didemnin analogs which have a deoxo-proline residue or a dehydro-proline residue in their structure. These analogs are useful as anti-cancer agents and for other purposes. Methods of making these analogs and methods of using them as inhibitors of protein synthesis, cell growth, and tumorigenesis and as enhancers of apoptosis are also provided.

Abstract: Disclosed herein are biocompatible and biodegradable polymers comprising one or more ECM-mimetic peptides and one or more biodegradable moieties, wherein the moieties do not comprise an amino acid or residue thereof. Further disclosed herein are methods for making and using the disclosed biocompatible polymers.

Abstract: The invention provides methods and compositions, e.g., for tumor imaging and therapy.

Abstract: The present invention relates to a new antimicrobial peptide, comprising the amino acid sequence of human galanin message associated peptide (GMAP) or a homolog, ortholog, chemically modified variant or antimicrobially active variant thereof, and respective uses thereof, particular in the topical treatment of antimicrobial diseases.

Abstract: The present invention relates to a fusion protein comprising IGF-I or an IGF-I variant N-terminally linked to the C-terminus of a propeptide. The invention relates also to a method involving the use of the aforementioned fusion protein in the production of a lysine-PEGylated IGF-I or IGF-I variant. The method comprises the steps of cultivating a prokaryotic host cell comprising an expression vector containing a nucleic acid encoding the fusion protein and causing the cell to express the fusion protein, recovering and PEGylating said fusion protein, cleaving said PEGylated fusion protein with IgA protease, and recovering lysine-PEGylated IGF-I or IGF-I variant. The invention relates also to a lysine-PEGylated IGF-I or IGF-I variant produced using the above method. In addition, the invention relates to a method for treating a neurodegenerative disorders like Alzheimer's Disease using the lysine-PEGylated IGF-I or IGF-I variant and a composition comprising the lysine-PEGylated IGF-I or IGF-I variant.

Abstract: A method of ligating two or more molecules, for example, peptides to peptides or peptides to labels is provided. The method may comprise the steps: a) providing a first oligopeptide having a reactive moiety, which is a hydrazine moiety, a hydrazide moiety or an amino-óxy moiety b) providing a second oligopeptide having an activated ester moiety, c)allowing the reactive moiety of the first oligopeptide to react with the activated ester moiety of the second oligopeptide to form an oligopeptide product, in which the first and second oligopeptides are linked via a linking moiety having Formula I, II or III. The second oligopeptide may preferably be generated by thiol reagent induced cleavage of an intein fusion protein. The invention further provides labelling and ligation methods in which protein hydrazides are ligated by reaction of the hydrazide moiety with an aldehyde functionality or a ketone functionality.

Abstract: Cyclic constructs with an N-terminus and a C-terminus which bind to a natriuretic peptide receptor and include a plurality of amino acid residues, at least one amino acid surrogate of formula I: where R, R?, Q, Y, W, Z, J, x and n are as defined in the specification, and optionally at least one prosthetic group, pharmaceutical compositions including such cyclic constructs, and methods of treating congestive heart failure or other conditions, syndromes or diseases for which induction of anti-hypertensive, cardiovascular, renal or endocrine effects are desired.

Abstract: The present invention relates to a super-antigen fusion protein, comprising: a peptide fragment whose sequence corresponds to a partial SARS E2 spike protein; and a translocating peptide fragment for transporting a protein into a cell and translocating the protein in cytosol; wherein, the amino acid sequence of the peptide fragment corresponding to the partial SARS E2 spike protein includes SEQ ID NO. 1, SEQ ID NO. 2, SEQ ID NO. 3 or SEQ ID NO. 4. The present invention further relates to DNA sequences corresponding to the partial SARS E2 spike protein includes SEQ ID NO. 5, SEQ ID NO. 6, SEQ ID NO. 7, or SEQ ID NO. 8; wherein the DNA sequences are able to express specific proteins in an E. Coli expression system.

Abstract: There is provided a temperature responsive polymer compound which comprises a repeating unit represented by the following general formula (I): —R1-Hmb-R2—??(I) where, Hmb represents a valic acid residue represented by the following formula (II); R1 represents an amino acid, a polypeptide, or a hydroxy acid being linked by ester bond; R2 represents an amino acid or a polypeptide being linked by amide bond or a hydroxy acid being linked by ester bond: and wherein said polymer compound has 18 or more of amino acids residues and hydroxy acid residues in total.

Abstract: The present invention relates to the diagnosis, evaluation, and therapeutic intervention of disorders mediated by the activity of cell surface receptor VEGFR-3, which activity often is stimulated by VEGFR-3 ligands VEGF-C and VEGF-D. More particularly, the present invention identifies novel methods and compositions for the inhibition of VEGF-C/D binding to VEGFR-3. The compositions of the present invention will be useful in the inhibition of angiogenesis and lymphangiogenesis.

Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease. The novel compounds typically include a 15-20 member macrocycle and have the general structure of structural Formula 1: wherein Z?, L?, M?, R1, X and D are defined herein.

Abstract: The present invention relates to polyamide compositions and therapies for treating cells infected with human papilloma virus (HPV).

Abstract: Compounds and methods of using such compounds in the imaging and detection of multidrug resistance cancer in a subject are provided. In particular, novel imaging agents are provided which are suitable for the detection and imaging of a multidrug resistance phenotype in cancer cells and/or tissues using non-invasive medical imaging modalities.

Abstract: A receptor ligand is conjugated to a lipid-soluble moiety, thereby allowing effective delivery of the peptide ligand to a target cell in the form of a liposome complex. The ligand brings the liposome in proximity to the target cell, facilitating the fusion of the liposome with an endosome of the cellular target to release the payload into the cytoplasm. The liposome itself packages drugs or other therapeutics that are delivered to the interior of the cell upon fusion of the liposome.

Abstract: The present invention relates to novel cyclic or constrained acyclic compounds which modulate the activity of G protein-coupled receptors and are useful in the treatment of conditions mediated by G protein-coupled receptors, for example, inflammatory conditions.