Abstract: Disclosed herein are peptides which include an isoDGR motif and which selectively inhibit ?v?3 integrin. In some embodiments, the isoDGR motif results from the deamidation of an NGR motif.

Abstract: The invention relates to relatively short peptides (termed J-Superfamily conotoxin peptides, J-conotoxins or J-conotoxin peptides herein), about 25 residues in length, which are naturally available in minute amounts in the venom of the cone snails or analogous to the naturally available peptides, and which preferably include two disulfide bonds. The J-conotoxins are useful for treating disorders involving voltage gated ion channels and/or receptors.

Abstract: A method is provided for the synthesis of glycopeptides using a sugar assisted ligation strategy, wherein an N-terminal peptide portion in the form of a thioester is coupled with a C-terminal peptide portion bearing a carbohydrate moiety comprising a thiol group.

Abstract: Disclosed are processes for preparing glycopeptide phosphonate derivatives having an amino-containing side chain. Several of the process steps are conducted in a single reaction vessel without isolation of intermediate reaction products, thereby generating less waste and improving the overall efficiency and yield of the process.

Abstract: Disclosed is a polymer composite (polyplex) that contains nucleic acid, a cationic polymer, and an anionic polymer. The anionic polymer covers the surface of the composite comprising the cationic polymer and nucleic acid, has a negative charge at neutral pH, and can change so as to have a positive charge at mildly acidic pH.

Abstract: This invention relates to compounds, compositions, and methods useful for reducing a target RNA and protein levels via use of Dicer substrate siRNA (DsiRNA)-peptide conjugates.

Abstract: The present invention is directed to an inventive polymeric carrier molecule according to generic formula (I) and variations thereof, which allows for efficient transfection of nucleic acids into cells in vivo and in vitro, a polymeric carrier cargo complex formed by a nucleic acid and the inventive polymeric carrier molecule, but also methods of preparation of this inventive polymeric carrier molecule and of the inventive polymeric carrier complex. The present invention also provides methods of application and use of this inventive polymeric carrier and the inventive polymeric carrier cargo complex as a medicament, for the treatment of various diseases, and in the preparation of a pharmaceutical composition for the treatment such diseases.

Abstract: The present invention provides compositions and methods for treating or preventing antibody mediated graft rejection and blood typing.

Abstract: The present invention is directed to sulphated compounds comprising at least one glycosidic amine group, and polysaccharide, oligosaccharide, peptide and protein derivatives comprising such compounds, and mixtures thereof. The present invention is also directed to methods of synthesising such compounds. Such compounds may bind to a range of proteins, find application in methods of modifying, or testing for a modification in the level of a cytokine in vivo, ex vivo or in vitro, and find application in the treatment and/or prevention of inflammation, an inflammatory disorder, a proliferative disorder, an immune disorder, an angiogenesis-dependent disorder, a sensitivity disorder, an adverse endocrine reaction, a degenerative disorder, wound healing, depression, and other diseases and disorders.

Abstract: In one embodiment, the invention provides glycopeptides (or carbohydrate-peptide conjugates) comprising TACAs that direct against (e.g., bind specifically to) cytotoxic T lymphocytes (CTLs) or helper T cells for, e.g., CTL- or T-helper-based immunotherapy of carcinomas, and methods for making and using the glycopeptides of the invention. In one embodiment, the invention provides novel glycopeptides comprising tumor-derived carbohydrate or tumor-derived epitopes that specifically bind to major histocompatibility (MHC) class I molecules on cytotoxic T lymphocytes (CTLs) or MHC molecules on helper T cells, and methods for using same, e.g., as a vaccine, including a pan-cancer vaccine.

Abstract: Provided are methods and nucleic acids for detecting, differentiating or distinguishing between colon cell proliferative disorders by analysis of one or more of the genes Versican, TPEF, H-Cadherin, Calcitonin, and EYA4. Further provided are novel nucleic acid sequences useful for the cell proliferative disorder specific analysis of said genes as well as methods, assays and kits thereof.

Abstract: The present invention is directed to polypeptide-nucleic acid conjugates. These conjugates can allow for targeted application of a therapeutic RNAi agent across the blood-brain barrier to treat, for example, a cancer, neurodegenerative disease, or lysosomal storage disorder.

Abstract: The present invention provides compounds, methods and systems for sequencing nucleic acid using single molecule detection. Using labeled NPs that exhibit charge-switching behavior, single-molecule DNA sequencing in a microchannel sorting system is realized. In operation, sequencing products are detected enabling real-time sequencing as successive detectable moieties flow through a detection channel. By electrically sorting charged molecules, the cleaved product molecules are detected in isolation without interference from unincorporated NPs and without illuminating the polymerase-DNA complex.

Abstract: It has been discovered that facile glycation of proteins can be achieved by colyophilization of a protein with a reducing sugar, subjecting the lyophilized mixture to a vacuum (10 to 50 millitor) and incubating at an elevated temperature (50 to 100° C.) for 1 to 24 h. A stable ketoamine derivative is formed with amino groups in the protein and no advanced glycation end products (browning reaction) are observed, as is the case with aqueous glycation procedures. Another novel feature is that the in vacuo glycation reaction takes place with the protonated amine and not the deprotonated amine as is believed to be the case for aqueous glycation reactions. Advantage can be taken of the in vacuo glycation reaction to achieve facile covalent cross-linking of proteins by lyophilizing protein or proteins with compounds containing two or more reducing sugars separated by a linker.

Abstract: A bisubstrate inhibitor of Src kinases, having a nucleotide or N-heteroaromatic moiety; and a peptide/phosphopeptide, peptidomimetic, or phosphopeptide mimic moiety. The moieties are linked by a rigid or a flexible linker. The nucleotide or N-heteroaromatic moiety is ATP, ATP-mimics, N-heteroaromatics including purine-based derivatives, pyrimidine-based derivatives such as 2,4-diamino-5-substituted pyrimidine derivatives, pyrazole[3,4-d]pyrimidine derivatives, pyrrolo[2,3-d]pyrimidine derivatives, pyrido[2,3-d]pyrimidine derivatives, amino-substituted dihydropyrimido[4,5-d]pyrimidinone derivatives, thieno- and furo-substituted derivatives, quinazoline derivatives, and quinoline derivatives, and several natural products such as aminogenistein.

Abstract: The present invention provides modified nucleobase compounds, modified nucleic acid mimetic compounds and various uses thereof. In addition, the invention provides methods for nucleobase characterisation, SNP characterisation and nucleic acid sequencing.

Abstract: The present invention provides novel n-alkenyl glycosides and glycoconjugates, n-alkyl glycoamino acids, and methods for the synthesis thereof. In another aspect, the present invention provides novel clustered glycopeptides and methods for the synthesis thereof. In still another aspect, the present invention provides methods for the treatment of cancer, preferably for the prevention of recurrence of cancer, and methods for inducing antibodies in a subject, comprising administering to a subject in need, an effective amount of any of the inventive glycoconjugates as disclosed herein.

Abstract: A novel target recognition molecule is provided which has a electrostatic property whereby such target recognition molecules can be densely brought together in a self-assembly manner in a predetermined region of an analytical chip and, in addition, can be reversibly or irreversibly stably immobilized there. This target recognition molecule has a target recognition peptide segment as a specific binding site for a target substance, an electrostatically-charged segment which is provided with three or more electrostatically-charged functional groups capable of being electrically charged with charges of the same polarity in the same solution and which has no functional groups that become electrically charged to different polarities in the same solution, and a connecting segment which chemically links with the target recognition peptide segment and with the electrostatically-charged segment for establishing a connection between both the segments.

Abstract: A method of making ultra-small chitosan nanoparticles having a size range of approximately 10-20 nm, includes preparing a first microemulsion containing effective amounts of cyclohexane, n-hexanol, chitosan polymer and a nonionic surfactant. A second microemulsion is prepared containing effective amounts of cyclohexane, n-hexanol, tartaric acid, EDC, n-hydroxysuccinimide, and a nonionic surfactant. The method continues by reacting the first and second microemulsions for a time sufficient to form the ultra-small chitosan nanoparticles and recovering the nanoparticles from the reacted microemulsion. The chitosan polymer may be crosslinked and may also be tagged with a fluorescent compound, a radio-opaque compound, a paramagnetic ion, a ligand specific for a predetermined biologic target, a drug, and combinations thereof.

Abstract: This invention relates to a peptide nucleic acid (PNA) oligomer which is conjugated with one or more linear-type amino acid containing a plurality of alkyleneglycols and to a synthesis method thereof. In addition, this invention related to a linear amino acid spacer in a device for detection for detecting a target gene using the PNA oligomers which is fixed on a surface of a functionalized solid support. The linear amino acid spacer contains a plurality of alkyleneglycols and maintains enough space between the solid support and PNA oligomer in the device in order to prevent the interference of the interaction between the PNA oligomer and a target gene. Furthermore, this invention relates to a PNA array, a PNA chip and a gene diagnosis kit whereof sensitivity and specificity are improved by being manufactured with the PNA conjugated with the amino acid spacer.

Abstract: Compounds useful in the preparation of telavancin, for example, were prepared. These compounds include decylaminoethanal dialkyl acetals and N-protected decylaminoethanal dialkyl acetals, imidazolidine derivatives, and N-protected-decylaminoethanal.

Abstract: Conjugates for the efficient delivery of sequence-specific antisense to cells of a selected type for the inhibition of a target protein have the general formula: peptide-HBL-antisense in which the peptide is a homing peptide which directs the conjugate to cells of a particular type, antisense is an antisense oligonucleotide having a sequence selected to provide sequence-specific inhibition of the target protein, and HBL is a heterobifunctional linker having reactivity towards amino and sulfhydryl groups.

Abstract: The present invention relates to new radiolabelled peptide-based compounds and their use for diagnostic imaging using positron emission tomography (PET). Such compounds may thus be used for diagnosis or therapy of, for example, malignant diseases, heart diseases, endometriosis, inflammation-related diseases, rheumatoid arthritis and Kaposi's sarcoma.

Abstract: Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and/or treating diseases and disease states caused by pathogenic cell populations.

Abstract: The present invention provides novel glycosides and glycoconjugates, glycoamino acids, and methods for the synthesis thereof. In another aspect, the present invention provides novel clustered glycopeptides and methods for the synthesis thereof. In still another aspect, the present invention provides methods for the treatment of cancer, preferably for the prevention of recurrence of cancer, and methods for inducing antibodies in a subject, comprising administering to a subject in need, an effective amount of any of the inventive glycopeptides as disclosed herein, either in conjugated form or unconjugated and in combination with a suitable immunogenic carrier.

Abstract: A delivery-enhancing peptide comprising the amino acid sequence of SEQ ID NO:11 or salt thereof. This invention is directed towards methods and compositions to administer a double-stranded ribonucleic acid to a mammal so as to effectuate transfection of the double-stranded RNA into a desired tissue of the mammal.

Abstract: One aspect of the present invention relates to the surprising discovery that modification of a glycan structure on a human SAP polypeptide can increase the biological activity of the SAP polypeptide relative to a corresponding sample of wild-type SAP isolated from human serum. The disclosure provides both variant human SAP polypeptides and methods for making the same. In particular, the present invention provides methods and compositions for in vitro and in vivo addition, deletion, or modification of sugar residues to produce SAP polypeptides, such as a human SAP polypeptide, having a desired glycosylation pattern.

Abstract: An aminated complex-type oligosaccharide derivative of the formula (1) wherein R1 is H—(CO)—CH2X, —NH—(CO)—(CH2)b—CH2X, isothiocyanate group, —NH—(CO)a—(CH2)b—CO2H or —NH—(CO)a—(CH2)b—CHO, X being a halogen atom, a being 0 or 1, b being an integer of 1 to 4, R2 and R3 are a hydrogen atom or a group of the formulae (2) to (5) and may be the same or different, except for the case where both R2 and R3 are hydrogen or the formula (5), and the case where one of R2 and R3 is a hydrogen atom, with the formula (5) serving as the other thereof.

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

Abstract: A process for the preparation of cyclodextrin oligomers or polymers, whereby the cyclodextrin molecules are coupled to one another covalently via a spacer arm, based on a coupling reaction between an alkyne and an azide producing the formation of an aromatic heterocyclic bridge between the coupled units. Also described are the cyclodextrin oligomers or polymers that are obtained and their uses.

Abstract: a highly efficient antiangiogenesis agent, which is a polypeptide for inhibition of angiogenesis Ile-Val-Arg-Arg-Ala-Asp-Arg-Ala-Ala-Val-Pro, connected with a polypeptide containing Arg-Gly-Asp on its one end or two ends is provided. The inhibiting agent can be synthesized or gene engineered. It also relates to a physiochemical method for modifying the antiangiogenesis agent. Polypeptides with weight percentage of 1-70% preferably about 20-50% are mixed with 20%-95% polyethylene glycol, or heparin, or dextran, or polyvinylpyrrolidone, or polyethylene glycol-poly-amino acid copolymer, or palmitic acid or poly-sialic acid or liposomes solutions; preferably about 50-93% of the above modified substances are fully mixed even and shaken at a shaker at 4° C.-40° C., preferably 25° C.-37° C. for more than 10 min, and the modified substances are separated through appropriate methods.

Abstract: Modified Thomsen-Friedenreich disaccharide (TFD) immunogen, preparation procedure, compositions containing it, uses, and treatment methods. More specifically, the present invention refers to a immunogen obtained by modifying TFD, and comprising the general formula D-TFD-Lys(n)-C, wherein D is a hydrophobic terminal residue, TFD is disaccharide Gal?3GalNAc?; Lys(n) is a lysine connector, and n is an integer between 1 and 5, and C is a carrier. In a preferred embodiment, the modified invention immunogen comprises the general formula Bzl?TFD-Lys5-KLHs, wherein Bzl is benzyl, TFD is disaccharide Gal?3GalNAc?; Lys5 is penta-lysine, and KLHs is succinilated Keyhole limpets hemocyanin.

Abstract: The present invention is directed to novel methods for in vitro and in vivo detection of target nucleic acid molecules, including DNA and RNA targets, as well as nucleic acid analogues. The present invention is based on protein complementation, in which two individual polypeptides are inactive. When the two inactive polypeptide fragment are brought in close proximity during hybridization to a target nucleic acid, they re-associate into an active, detectable protein.

Abstract: The invention relates to a bonding product suitable as a carrier for medicinal substances and to the compound derived therefrom that carries medicinal substances. The invention further relates to a process and device for preparing such bonding products and compounds. Further, the invention relates to a pharmaceutical composition containing such bonding products and compounds, and to the use thereof for preparing an infusible medicament for treating a disease.

Abstract: To provide a photocrosslinkable compound and a photocrosslinking agent which are capable of ligation of nucleic acids within a short period of time compared to the conventional cases, and to which modifications depending on the intended use can easily be made, and a method of producing the photocrosslinking agent. Nucleic acids including a group represented by the formulae I, III, IV, or V as a nucleobase; a photocrosslinking agent including the nucleic acids, a method of producing nucleic acids by reacting nucleic acids including a group represented by the formulae VI, VII, VIII, or IX as a nucleobase with an aromatic azidated product represented by the formula X.

Abstract: The present invention provides novel compounds, compositions, methods and uses for treating microvascular disorders, eye diseases and respiratory conditions based upon inhibition of a target gene. More specifically, the present invention relates to positional motifs of modified ribonucleotides useful in the design of siRNA compounds. In particular, the ribonucleotides include modified internucleotide linkages and/or modified sugar moieties. These novel siRNA compounds may be used therapeutically to treat a variety of diseases and indications.

Abstract: The present invention provides recombinant antigen-binding regions and antibodies and functional fragments containing such antigen-binding regions that are specific for CD38, which plays an integral role in various disorders or conditions. These antibodies, accordingly, can be used to treat, for example, hematological malignancies such as multiple myeloma. Antibodies of the invention also can be used in the diagnostics field, as well as for investigating the role of CD38 in the progression of disorders associated with malignancies. The invention also provides nucleic acid sequences encoding the foregoing antibodies, vectors containing the same, pharmaceutical compositions and kits with instructions for use.

Abstract: There is presently provided a triblock peptide comprising a hydrophobic amino acid block, a histidine block and a cationic amino acid block. The triblock peptide may be used to form a nanoparticle for delivery of an agent into a cell.

Abstract: The present invention provides novel glycopeptides antibiotic derivatives. These glycopeptide antibiotic derivatives are characterized in that a sugar residue (I) represented by the formula: (wherein n is an integer of 1 to 5; Sugs are each independently a monosaccharide, (Sug)n is a divalent sugar residue formed by binding of same or different 1 to 5 monosaccharides; RA1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, or optionally substituted cycloalkyl; and RE is OH or NHAc (Ac is acetyl)) is bound to an aromatic ring of the fourth amino acid residue in the glycopeptide skeleton. These derivatives have antibacterial activity against vancomycin-resistant bacteria.

Abstract: The present invention is directed to pharmaceutical agents and compositions useful for the treatment and prevention of amyloid disease in a subject. The invention further relates to isolated antibodies that recognize a common conformational epitope of amyloidogenic proteins or peptides that are useful for the diagnosis, treatment, and prevention of amyloid disease.

Abstract: The current invention provides polypeptides and polypeptide conjugates that include an exogenous N-linked glycosylation sequence. The N-linked glycosylation sequence is preferably a substrate for an oligosaccharyltransferase (e.g., bacterial PgIB), which can catalyze the transfer of a glycosyl moiety from a lipid-bound glycosyl donor molecule (e.g., a lipid-pyrophosphate-linked glycosyl moiety) to an asparagine (N) residue of the glycosylation sequence. In one example, the asparagine residue is part of an exogenous N-linked glycosylation sequence of the invention. The invention further provides methods of making the polypeptide conjugates that include contacting a polypeptide having an N-linked glycosylation sequence of the invention and a lipid-pyrophosphate-linked glycosyl moiety (or phospholipid-linked glycosyl moiety) in the presence of an oligosaccharyltransferase under conditions sufficient for the enzyme to transfer the glycosyl moiety to an asparagine residue of the N-linked glycosylation sequence.

Abstract: An aqueous or powder composition includes anti-gram-negative antibiotic or salt thereof being present at an amount ranging from about 100 mg/ml to about 200 mg/ml. Another aqueous or powder composition includes anti-gram-positive antibiotic or salt thereof being present at a concentration ranging from about 0.6 to about 0.9 of the water solubility limit, at 25° C. and 1.0 atmosphere, of the anti-gram-positive antibiotic or salt thereof. Other embodiments include unit doses, kits, and methods.

Abstract: A novel class of antimicrobial polymeric agents which are designed to exert antimicrobial activity while being stable, non-toxic and avoiding development of resistance thereto and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and a method of treating medical conditions associated with pathological microorganisms, a medical device, an imaging probe and a food preservative utilizing same. Further disclosed are conjugates of an amino acid residue and a hydrophobic moiety residue and a process of preparing same.

Abstract: The present invention provides novel clustered multi-antigenic constructs having the structure: and methods for the synthesis thereof. In still another aspect, the present invention provides methods for the treatment of cancer, preferably for the prevention of recurrence of cancer, and methods for inducing antibodies in a subject, comprising administering to a subject in need, an effective amount of any of the inventive constructs as disclosed herein, either in conjugated form or unconjugated and in combination with a suitable immunogenic carrier.

Abstract: The present invention relates generally to peptides derived from the natural cytotoxicity receptors on natural killer (NK) cells and to antibodies against peptide epitopes on these receptors. In particular, the present invention identifies an essential epitope in the proximal domain of NKp46 and NKp44 receptors present on NK cells, as a crucial element for the binding to viral-infected cells. The present invention provides peptides that are derived from the amino acid sequence of NKp46 receptor, capable of specific targeting of viral-infected cells and tumor cells and monoclonal antibodies which recognize a specific domain of NKp46. The present invention further provides hyperglycosylated peptides that are derived from the NKp44 receptor, capable of specific targeting of viral-infected cells.

Abstract: The invention provides compositions and methods of identifying, modifying and producing modified target molecules, including therapeutic molecules by modification with non-natural amino acids. Certain aspects of the invention include methods of adding a chemical moiety to a target molecule, and the compositions resulting therefrom. Certain aspects of the invention also relate to kits for identifying, modifying and producing modified target molecules described herein.

Abstract: A polypeptide, with an amino acid sequence different from that of knottin protein, having a scaffold moiety with a helix moiety inserted in the scaffold moiety is described. The scaffold moiety comprises a knottin protein, or a fragment of knottin protein.

Abstract: The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide.

Abstract: A new approach in the field of plant gums is described which presents a new solution to the production of hydroxyproline(Hyp)-rich glycoproteins (HRGPs), repetitive proline-rich proteins (RPRPs) and arabino-galactan proteins (AGPs). The expression of synthetic genes designed from repetitive peptide sequences of such glycoproteins, including the peptide sequences of gum arabic glycoprotein (GAUP), is taught in host cells, including plant host cells.

Abstract: The invention relates to the use of a granulin or a granulin-like compound for producing a pharmaceutical composition for the therapy or prophylaxis of chronic pain, in particular for neuropathic pain.