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: Structural and functional analysis of peptide inhibitor binding to the cyclin D1 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 relates to an intermediate, as represented by formula (I), for synthesizing caspofungin, and a preparation method thereof. The intermediate enables efficient preparation of caspofungin.

Abstract: A compound as represented by Formula (I) is provided, wherein groups are defined in the description. The compound is used as HCV protease inhibitor for treating HCV infection.

Abstract: The present invention is related to new peptide antagonists of ?v?3 receptor, designed on the basis of the crystal structure of integrin ?v?3 in complex with c(RGDf[NMe]V) and the NMR structure of echistatin. These peptides are potent and selective antagonists of the ?v?3 receptor and can be used as novel anticancer drugs and/or new class of diagnostic non-invasive tracers as suitable tools for ?v?3-targeted therapy and imaging.

Abstract: Lactam-bridged melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including obesity, modulation of feeding behavior, related metabolic syndrome, sexual dysfunction, male erectile dysfunction and female sexual dysfunction.

Abstract: Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death.

Abstract: A purification method of the compound represented by formula 1 is provided, which includes the following steps: (1) loading crude compound 1 on macroporous adsorbent resin, (2) washing the macroporous adsorbent resin with an aqueous solution, an organic solvent or a mixture solution of organic solvent and water, (3) eluting with an aqueous solution, an organic solvent or a mixture solution of organic solvent and water. The purified compound represented by formula 1 is obtained.

Abstract: A liquid pharmaceutical composition comprising a biodegradable polymer, polyethylene glycol having a molecular weight of less than 600 Daltons, a pharmaceutically active agent and less than 0.5% of an biologically acceptable organic solvent.

Abstract: A non-aqueous single pot synthesis of [18F]SFB is set forth. The [18F]SFB produced with this method is then used, for example, to label a peptide or an engineered antibody fragment (diabody) targeting human epidermal growth factor receptor 2 (HER2) as representative examples of labeled compounds for use as an injectable composition to locate abnormal tissue, specifically tumors within an animal or human using a PET scan.

Abstract: Disclosed is an antimicrobial peptide having an amino acid sequence of formula presented as (P1)M(nA1X1X2)N(P2)X, wherein P1 is selected from the group consisting of basic amino acids including Arg and Lys; A1 is selected from the group consisting of aromatic amino acids including Trp, Phe and Ala; X1 is selected from the group consisting of basic amino acids or nonpolar amino acids, including Arg, Lys, Val, Leu, Ala and Ile; X2 is selected from the group consisting of basic amino acids or nonpolar amino acids, including Arg, Lys, Val, Leu, Ala and Ile; P2 is selected from the group consisting of basic amino acids including Arg and Lys; and the numbers of M and X are respectively 0˜2; when N>2, A1 is Ala and the Ala residues are less than N?2.

Abstract: The invention relates to compositions which are useful for inhibiting prostaglandin F2? receptor. The compositions include, but are not limited to, linear peptides, peptide analogs, and peptidomimetics. Methods of using the compositions of the invention to treat preterm labor and dysmenorrhea are disclosed.

Abstract: The invention provides tight junction protein modulators, compositions comprising the same, and uses thereof. In particular, the invention provides tight junction protein modulators that modulate the second extracellular loop of tight junction proteins, such as occludin or claudin.

Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

Abstract: The present invention relates to a cyclosporine emulsion containing: i) a cyclosporine ii) a natural oil (long chain triglyceride) iii) a phosphatidylcholine, iv) glycerol, v) a pharmaceutically tolerable alkali salt of a free fatty acid, vi) a medium chain triglyceride-oil vii) optionally, hydrochloric acid or sodium hydroxide for pH adjustment viii) water.

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: The present invention is directed to methods, for example phage display assays, for bioengineering peptides that bind to individual distinct nucleotides. Also provided are peptides engineered by such methods. Specifically, cyclic peptides that bind individual distinct nucleotides are provided herein.

Abstract: The present invention relates generally to tissue differentiation factor (TDF) analogs. More specifically, the invention relates to structure-based methods and compositions useful in designing, identifying, and producing molecules which act as functional modulators of TDF-like receptors. The invention further relates to methods of detecting, preventing, and treating TDF-associated disorders.

Abstract: A modified release composition comprising cyclosporin A for oral administration. The composition may comprise a core and a modified release coating, wherein the core comprises a hydrogel-forming polymer matrix and cyclosporin A. The composition may be in the form of a minibead. The compositions provide a pharmacokinetic profile and dissolution profile which provides release of cyclosporin A in the lower GI tract whilst minimising systemic exposure. Also disclosed are uses of the composition in the treatment of conditions affecting the lower GI tract, particularly the colon.

Abstract: Disclosed are surprising discoveries concerning the role of anionic phospholipids and aminophospholipids in tumor vasculature and in viral entry and spread, and compositions and methods for utilizing these findings in the treatment of cancer and viral infections. Also disclosed are advantageous antibody, immunoconjugate and duramycin-based compositions and combinations that bind and inhibit anionic phospholipids and aminophospholipids, for use in the safe and effective treatment of cancer, viral infections and related diseases.

Abstract: An object of the present invention is to provide molecules that bind to a target molecule in a pH dependent manner and a screening method for selecting such molecules. Provided is a screening method for selecting peptides that bind to a target molecule at a first pH and do not bind thereto at a second pH, including a step of preparing a peptide library in which each mRNA contains at least one special amino acid that undergoes a pH-dependent change in the charge of the side chain thereof, a step of bringing the peptide library into contact with the target molecule and incubating them under the first pH condition and selecting peptides that bind to the target molecule, and a step of selecting, from the peptides which have bound to the target molecule, peptides that do not bind to the target molecule under the second pH condition.

Abstract: Disclosed embodiments concern a method for making substantial quantities of desired macrocycles. Disclosed ring closing reactions make the macrocycle with desired olefin geometry in excellent yield and E/Z ratio. Particular embodiments of the current method concern intermediates that are obtained from commercially available starting materials in a small number of steps, thereby illustrating the commercial importance and applicability of the disclosed method. The macrocycle produced by the ring closing reaction can be further derivatized to provide analogs of the macrocyclic compounds.

Abstract: The present invention provides novel peptide immunogens comprising influenza virus matrix 2 protein epitopes and related compositions and methods. The present invention relates to a composition comprising a peptide immunogen useful for the prevention and treatment of an influenza virus-mediated disease. The invention also relates to vaccines, immunogenic products and immunogenic compositions containing the peptide immunogens.

Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein the dashed line, X, R1, R2, R3, R4, R5, R6, and R7 have defined meanings; the preparation thereof; compositions containing compounds of formula (I), including bioavailable combinations with ritonavir; and the pharmaceutical uses thereof.

Abstract: The present invention provides an isolated peptide having an amino acid residue sequence that comprises at least one human cytomegalovirus glycoprotein B (HCMV-gB) sequence segment, each HCMV-gB sequence segment consisting of at least 8 and not more than 60 consecutive amino acid residues from residues 146 to 315, residues 476 to 494 of SEQ ID NO: 1, or from a sequence variant of residues 146 to 315 or 476 to 494 of SEQ ID NO: 1 that has at least 70% sequence identity thereto. The peptides of the invention are useful for treating, preventing, or inhibiting a herpesvirus (e.g., Herpes Simplex Virus-1, Human Cytomegalovirus, and the like) infection in a subject.

Abstract: The present invention relates to a novel process for preparing the aza cyclohexapeptide compound 1-[(4R,5S)-5-[(2-aminoethyl)amino]-N2-(10,12-dimethyl-1-oxotetradecyl)-4-hydroxy-L-ornithine]-5-[(3R)-3-hydroxy-L-ornithine]-pneumocandin B0 (caspofungin) represented by the following formula 1, which can improve the problem due to a pungent odor and toxicity during the process and can prepare caspofungin as a final product at high yield compared to conventional processes, and to novel intermediates which are used in the preparation process:

Abstract: The present invention concerns a chimeric polypeptide, capable of detecting the antibodies generated in rheumatoid arthritis, comprising at least two citrulinated peptide subunits: (i) one derived from the ? or ? chain of the fibrin and (ii) a second derived from the filaggrin. In addition, the invention comprises an antigenic composition, a method and a kit for the diagnosis of rheumatoid arthritis, from the detection of the autoantibodies generated during the course of said disease.

Abstract: The invention relates to peptides which bind to human FcRn and inhibit binding of the Fc portion of an IgG to an FcRn, thereby modulating serum IgG levels. The disclosed compositions and methods may be used for example, in treating autoimmune diseases and inflammatory disorders. The invention also relates to methods of using and methods of making the peptides of the invention.

Abstract: The invention concerns peptoid-peptide hybrids that may act as protein interaction inhibitors (PPIIs). Another aspect of the invention concerns a method for treating a disorder (e.g., an oncologic disorder) in a human or animal subject, comprising administering an effective amount of a peptoid-peptide hybrid (a peptoid body) of the invention, or a composition comprising a peptoid-peptide hybrid, to the subject in need thereof. Another aspect of the subject invention concerns a method for killing or inhibiting the growth of cells (e.g., cancer cells or malaria-infected cells), comprising contacting a cancer cell in vitro or in vivo with an effective amount of a peptoid-peptide hybrid, or a composition comprising the peptoid-peptide hybrid. Another aspect of the invention concerns a method for producing a peptoid-peptide hybrid.

Abstract: A high purity cyclopeptide crystal has a structure shown by Formula I. R represents H or a cation forming a pharmaceutically acceptable salt. Also disclosed are a preparation method and a use of the high-purity cyclopeptide crystal.

Abstract: This invention relates to the use of microcystins as agents for treatment of cancer. Also provided are methods of screening for microcystins with improved cytotoxicity.

Abstract: The present invention relates to a method for preparing cyclopeptides by means of protection with a substituted boronic acid. The present invention also discloses novel boronate esters of cyclopeptides of general formula (8).

Abstract: Described are lantibiotic-based compounds, pharmaceutical compositions comprising the same and use of the compounds and said compositions, for the treatment of microbial infection, for example Clostridium difficile or Micrococcus luteus infection. The lantibiotic-based compounds have antimicrobial activity and in comparison to one or more of actagardine, actagardine B, deoxyactagardine B and deoxyactagardine have retained activity or improved activity.

Abstract: The present invention relates to targeting agents and methods: of using the targeting agents to detect a fungal cell in a subject.

Abstract: The present application provides stable peptide-based anti-gp41 antibody capture agents and methods of use as detection and diagnosis agents. The application further provides methods of manufacturing anti-gp41 antibody capture agents using iterative on-bead in situ click chemistry.

Abstract: A Nisin derivative or variant, comprising an amino acid substitution at amino acid position 29 in the amino acid sequence. The Nisin derivative exhibits enhanced antimicrobial activity when compared to wild type Nisin. The Nisin derivative has an application as a natural food additive and as a therapeutic agent.

Abstract: Provided herein are peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.

Abstract: The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I employing an aldehyde acetal intermediate, wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.

Abstract: This invention relates to an isolated, compound of Formula (1) or derivatives or pharmaceutically acceptable salts thereof. The invention also includes all isomeric and tautomeric forms of the compound of Formula (1) or the derivatives thereof. The present invention further relates to processes for the production of the compound of Formula (1) by fermentation of the fungal strain of Actinomycetes (PM0895172/MTCC 684), pharmaceutical compositions comprising the compound of Formula (1) as the active ingredient; and use of the compounds or composition containing them in the treatment of cancer.

Abstract: Peptides having activity as protein binding agents are disclosed. The peptides have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R, R1, L1, L2, G, M, Y1 Y2 and SEQ are as defined herein. Methods associated with preparation and use of such peptides, as well as pharmaceutical compositions comprising such peptides, are also disclosed.

Abstract: Disclosed are a caspofungin analog, and a preparation method and applications thereof. The caspofungin analog has a structure as represented in Formula 3.

Abstract: Low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations for modifying biomolecules is provided. Compositions, methods, and kits relating to low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations are also provided.

Abstract: Peptide nanotube polymers and methods of making such are disclosed. The peptide nanotube polymers are comprised of alternating monomers of the first peptide ring and monomers of the second peptide ring covalently bonded to one another via a linker, and can be functionalized. The described peptide nanotube polymers can enjoy the combined properties of healing and toughness, self-reporting, and tunability and actuation.

Abstract: The present invention provides macrocyclic compounds of Formula (I): pharmaceutically acceptable salts thereof; and pharmaceutical compositions thereof, wherein R1, R2, R3, R4, RE, RF, RG, RH, RI, f, g, h, n, and m are as defined herein. The present invention further provides methods of synthesizing these macrocyclic compounds, and methods of their use and treatment. Certain aspects of the present invention relate to modulation of kinase activity, and in the treatment of kinase-associated diseases or disorders.

Abstract: Disclosed is a high purity cyclopeptide compound, the chemical structure of which is represented by formula (I). R represents H or a cation capable of forming a pharmaceutically acceptable salt, the purity being greater than or equal to 99.0%. Further disclosed are preparation method and use of the high purity cyclopeptide compound.

Abstract: Disclosed are a caspofungin analog and applications thereof. The caspofungin analog is a compound having a structure as indicated in Formula (4), or pharmaceutically acceptable salts thereof. R1 can be chosen from hydroxyl, benzyloxy, phenoxy, substituted phenoxy, or substituted benzyloxy. R2, R3, R4, R5 can be chosen from hydrogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxyl, benzyloxyphenyl, substituted benzyloxyphenyl, nitro, fluorine, chlorine, bromine, or iodine. Also disclosed are a preparation method for and applications of the compound.

Abstract: Compositions and methods for targeting therapeutic agents to neuromuscular junctions are disclosed. Also disclosed are methods for treating diseases and conditions affecting the neuromuscular junction. Compositions include a neuromuscular junction targeting peptide coupled to a therapeutic agent. Compositions may further include a linker peptide. Methods for targeting therapeutic agents to neuromuscular junctions and treating diseases and conditions affecting the neuromuscular junction include administering a composition including a neuromuscular junction targeting peptide coupled to a therapeutic agent.

Abstract: Factor H-binding peptides that binds to a region of factor H that does not impede the complement-inhibitory activity of factor H are disclosed. When immobilized onto the surface of a biomaterial, these peptides recruit factor H, resulting in a substantial inhibition of biomaterial-induced complement activation in a biological substance exposed to the biomaterial.

Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

Abstract: The present application provides synthetic modified peptides of five to seven natural or non-natural amino acids as well as pharmaceutical compositions comprising them, for use in the treatment a disease or disorder presenting behavioral abnormalities associated with impairment of sensory gating function, depression or cognitive impairment, particularly schizophrenia and Alzheimer's disease.