Abstract: The present invention relates firstly to the discovery of the previously unknown 24-membered cyclooctadepsipeptides PF1022-V, PF1022-W, XRB-C894, XRB-C942, XRB-C976, XRB-C1010, XRB-C1044, XRB-E922, XRB-E956, XRB-E990, XRB-E1024, XRB-S958, XRB-S992, XRB-S1026, XRB-S1060 (in various isomeric forms) and to the processes for the preparation of the abovementioned cyclooctadepsipeptides by means of the fungal strains from the family Xylariaceae, in particular the genera Rosellinia and Coniolariella, and by means of the mitosporic fungal strains from the groups Fusarium, Beauveria and Verticillium (orders Hypocreales and Phyllachorales), and by means of the enzymatic preparations isolated from these fungal strains, and secondly to the use of these strains for the preparation of the abovementioned novel cyclooctadepsipeptides and to the use of bassianolide and of the abovementioned novel cyclooctadepsipeptides individually or as a mixture, as anthelmintics or endoparasiticides.

Abstract: In order to provide an effective vaccine against infection with Propionibacterium acnes, the present invention provides a peptide which is a peptide consisting of a specific amino acid sequence or a peptide consisting of an amino acid sequence derived from the specific amino acid sequence by deletion, substitution, insertion, or addition of one or more amino acids, the peptide suppressing, by immune response, inflammation caused by infection with Propionibacterium acnes.

Abstract: Embodiments of the present invention provide for novel peptides of use for detection and/or inhibition of anti-?1-adrenergic receptor antibodies. Certain embodiments concern uses of cyclic and/or linear peptides. In other embodiments, the present invention relates to novel peptides of use in diagnostic and/or pharmaceutical compositions. Some embodiments concern diagnosing and/or treating cardiac conditions. Cardiac conditions of the instant invention can concern infectious heart disease, non-infectious heart disease, ischemic heart disease, non-ischemic heart disease, inflammatory heart disease, myocarditis, cardiac dilatation, idiopathic cardiomyopathy, idiopathic dilated cardiomyopathy, immune-cardiomyopathy, heart failure, and any cardiac arrhythmia condition.

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

Abstract: The present invention relates to amino acid sequences that are capable of binding to serum proteins; to compounds, proteins, polypeptides, fusion proteins or constructs comprising or essentially consisting of such amino acid sequences; to nucleic acids that encode such amino acid sequences, compounds, proteins, polypeptides, fusion proteins or constructs; to compositions, and in particular pharmaceutical compositions, that comprise such amino acid sequences, compounds, proteins, polypeptides, fusion proteins or constructs; and to uses of such amino acid sequences, compounds, proteins, polypeptides, fusion proteins or constructs.

Abstract: Disclosed is a polypeptide comprising at least two microproteins, which preferably comprise an amino acid sequence having a specific binding activity to a target protein. Furthermore, disclosed are polynucleotides encoding such a polypeptide as well as pharmaceutical compositions and kits comprising said polypeptide or polynucleotide. Also disclosed herein are methods of treatments and second medical uses applying the disclosed polypeptide or polynucleotide. Additionally, the disclosure of the present application relates to a method for forming a covalent bond in a microprotein which can be used for producing the disclosed polypeptides.

Abstract: The present invention relates to combinations of aplidine or aplidine analogues with other titumoral agents, and the use of these combinations in the treatment of cancer, in particular in the treatment of lung cancer, breast cancer, colon cancer, prostate cancer, renal cancer, melanoma, multiple myeloma, leukemia and lymphoma.

Abstract: The following invention is directed to macromolecules having controlled stoichiometry and topology, processes for their production, and applications for their use. The macromolecules have a controlled functional moiety stoichiometry and include at least one dendritic motif having a surface layer formed from at least one surface building unit and at least one subsurface layer formed from at least one building unit, the surface building unit and building units having a hydrocarbon backbone bearing a carbonyl group and at least one amine group; and at least two different functional moieties on the building unit and/or surface building unit; where functional moiety stoichiometry refers to the number and type of functional moieties.

Abstract: The present application provides synbodies against AKT1 differing in amino acid sequence, conjugation chemistry, linker/scaffold, or adjunct moiety. The synbodies are useful for diagnosis and treatment of cancer and as research reagents.

Abstract: The present invention relates to crystalline forms of linaclotide, as well as to various methods and processes for the preparation and use of the crystalline forms.

Abstract: Novel oligopeptides, combinations thereof and fusion proteins composed of the above-mentioned oligopeptides are disclosed. Oligopeptides are homologous in amino acid sequence to the selected parts of the amino acid sequence of human myelin basic protein (MBP) and are capable to ameliorate the progression of multiple sclerosis by means of binding to and inactivation of epitope-specific anti MBP catalytic auto antibodies (ESAMBPCAA) involved into binding and catalytic degradation of MBP in course of progression of Multiple Sclerosis.

Abstract: The invention provides protein nanorings.

Abstract: The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.

Abstract: Chemically reactive dyes that are intramolecularly crosslinked with a water-soluble bridge, their bioconjugates and their uses are described. Reactive fluorescent dyes that have a water-soluble bridge are superior to those of conjugates of spectrally non-crosslinked dyes or the dyes that are crosslinked with a hydrophobic bridge. The invention includes reactive fluorescent dyes, their biological conjugates and uses.

Abstract: The instant invention relates to polyethylene glycol-based dendrons, otherwise known as PEGtide dendrons, compositions thereof and methods of use.

Abstract: This invention relates to grassystatins A, B and C, and their isolated or purified forms. The compounds of the invention are useful as aspartic protease, gamma secretase, or metalloprotease inhibitors. Methods of using the compounds and compositions thereof are also disclosed.

Abstract: The present invention provides peptides and pharmaceutical compositions thereof for appetite suppression and weight control. Preferred peptides are calcitonin analogs, preferably with specific amino acid changes to make the peptide more amylin-like.

Abstract: The present invention relates to novel fluorinated macrocyclic compounds and methods of treating a hepatitis C infection in a subject in need of such therapy with said macrocyclic compounds. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.

Abstract: Provided are constrained peptides that inhibit HIV assembly. Pharmaceutical compositions comprising the above peptides are also provided. Additionally provided are methods of inhibiting replication of a capsid-containing virus.

Abstract: Purified compounds of formula I are described. Compounds include all stereoisomeric forms and all tautomeric forms of the compounds of formula I and pharmaceutically acceptable salts and derivatives. Processes for the production of the antibacterial compounds by fermentation of the microorganism belonging to Streptomyces species (PM0626271/MTCC 5447) and to pharmaceutical compositions containing one or more of the novel compounds as active ingredient and their use in medicines for treatment and prevention of diseases caused by bacterial infections are described.

Abstract: This invention relates to methods, compositions, and apparatuses for producing macrocyclic compounds. First, one or more reactants are provided in a reaction medium, which are capable of forming the macrocyclic compound through a desired reaction pathway that includes at least cyclization, and which are further capable of forming undesired oligomers through a undesired reaction pathway that includes undesirable oligomerization. Oligomerization of such reactions in the reaction medium is modulated to reduce formation of undesired oligomers and/or to reduce separation of the undesired oligomers from the reaction medium, relative to a corresponding unmodulated oligomerization reaction, thereby maximizing yields of the macrocyclic compound. The macrocyclic compound so formed is then recovered from the reaction medium. Preferably, the macrocyclic compound spontaneously separates from the reaction medium via phase separation.

Abstract: The present invention provides methods for guiding preservation of neurons or nerves during surgery by administering a fluorescently-labeled peptide or aptamer that specifically binds to the neurons or nerves. The invention further provides targeting molecules of fluorescently-labeled peptides or aptamers that specifically bind to neurons or nerves and for compositions thereof.

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: The present invention relates to multimeric (e.g., dimeric, trimeric) forms of peptide vectors that are capable of crossing the blood-brain barrier (BBB) or efficiently entering particular cell types. These multimeric peptide vectors, when conjugated to agents (e.g., therapeutic agents) are capable of transporting the agents across the BBB or into particular cell types. These compounds are therefore particularly useful in the treatment of neurological diseases.

Abstract: The present invention, according to several embodiments, comprises a compound represented by Formula I: in which the substituents BG, B, B1, R1, R100, R2, R200, A, A1, Q and Q1 are defined herein; or a prodrug, or a salt thereof, and which bind to IAP BIR domains. In particular, the compounds of certain embodiments are useful in treating proliferative disorders such as cancer.

Abstract: The invention provides structurally constrained viral peptides for use as therapeutic and vaccination agents, and for the production of antibodies for use in a number of applications including as therapeutic agents. The invention further provides methods and kits for use of the structurally constrained peptides and antibodies of the instant invention. The invention is based, at least in part, on the result provided herein demonstrating that viral hydrocarbon stapled helical peptides display excellent proteolytic, acid, and thermal stability, restore the native helical structure of the peptide, are highly effective in interfering with the viral fusogenic process, and possess superior pharmacokinetic properties compared to the corresponding unmodified peptides.

Abstract: Disclosed herein, in certain embodiments, is a selective transport molecule with increased in vivo circulation. In some embodiments, a selective transport molecule disclosed herein has the formula (A—X—B—C)n—M, wherein C is a cargo moiety; A is a peptide with a sequence comprising 5 to 9 consecutive acidic amino acids, wherein the amino acids are selected from: aspartates and glutamates; B is a peptide with a sequence comprising 5 to 20 consecutive basic amino acids; X is a linker; and M is a macromolecular carrier.

Abstract: A library of macrocyclic compounds of the formula (I) where part (A) is a bivalent radical, a —(CH2)y— bivalent radical or a covalent bond; where part (B) is a bivalent radical, a —(CH2)z— bivalent radical, or a covalent bond; where part (C) is a bivalent radical, a —(CH2)t- bivalent radical, or a covalent bond; and where part (T) is a -Y-L-Z- radical wherein Y is CH2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for their preparation of these compounds in a combinatorial manner, is also disclosed.

Abstract: At least some embodiments of the invention relates to an implant having a coating that contains or is composed of a functionalized RGD peptidomimetic RGD-P1 having the formula (1) and/or a functionalized RGD peptidomimetic RGD-P2 having the formula (2), and an associated manufacturing method.

Abstract: At least some embodiments of the invention relates to an implant having a coating that contains or is composed of a functionalized RGD peptidomimetic RGD-P1 having the formula (1) and/or a functionalized RGD peptidomimetic RGD-P2 having the formula (2), and an associated manufacturing method.

Abstract: A polymer conjugate of a physiologically active substance, which enables drug release independent of a biological enzyme and can be expected to have a high therapeutic effect, is demanded.

Abstract: Provided are bioactive compounds and metabolites derived from Chromobacterium species culture responsible for controlling pests, compositions containing these compounds, methods for obtaining these compounds and methods of using these compounds and compositions for controlling pests.

Abstract: The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.

Abstract: The aqueous self-assembly of oligopeptide-flanked ?-conjugated molecules into discrete one-dimensional nanostructures is described. Unique to these molecules is the fact that the ?-conjugated unit has been directly embedded within the peptide backbone by way of a synthetic amino acid with ?-functionality that is compatible with standard Fmoc-based peptide synthesis or by way of a diacid or other bis(electrophile) that can covalently cross-link peptide chains presented on a synthesis support. The peptide-based molecular designs enforce intimate ?-? communication within the aggregates after charge-screening and self-assembly, making these nanostructures attractive for optical or electronic applications in biological environments. In other embodiments, a convenient method to incorporate ?-electron units into peptides that assemble into amyloid-like supramolecular polymers is disclosed.

Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.

Abstract: Disclosed are a compound represented by the general formula (I) below and a polymer compound obtained by polymerizing such a compound. R1-Gly-Lac-Pro-R2 ??(I): where -Gly-Lac-Pro- represents a structure represented by the following formula (II), R1 represents a hydrogen atom, or an amino acid, a polypeptide or a hydroxycarboxylic acid which are linked through an amide bond, R2 represents a hydroxyl group, or an amino acid or a polypeptide which are linked through an amide bond, or a hydroxycarboxylic acid which is linked through an ester bond.

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: Provided is a composition comprising a peptide comprising amino acids and/or amino acid analogs comprising a continuous sequence of a sclerostin fragment comprising Tyr43 or Tyr213. Also provided is a composition comprising a peptide comprising less than about 75 amino acids and/or amino acid analogs including an amino acid or amino acid analog capable of being sulfated, where the composition is capable of inhibiting sclerostin binding to an LRP. Further provided is a composition comprising a peptide comprising less than about 75 amino acids and/or amino acid analogs including an amino acid or amino acid analog capable of being post-translationally sulfated, where the composition is capable of inhibiting binding of a protein ligand comprising a sulfation site to its binding partner.

Abstract: This invention relates to enfuvirtide peptide derivatives that are inhibitors of viral infection and/or exhibit antifusogenic properties. In particular, this invention relates to enfuvirtide derivatives having inhibiting activity against human immunodeficiency virus (HIV), respiratory syncytial virus (RSV), human parainfluenza virus (HPV), measles virus (MeV), and simian immunodeficiency virus (SIV) with long duration of action for the treatment of the respective viral infections.

Abstract: Disclosed are compounds that include two or more haptens conjugated by a spacer or a carrier. The haptens may include diethylenetriaminepentaacetate (DTPA), histimine-succinyl-glutamine (HSG), or combinations of DTPA and HSG. The compound also includes an effector molecule which may be conjugated to one or more of the haptens, the spacer/carrier, or both. The effector molecule may be conjugated by a number of linkages including an ester linkage, an imino linkage, an amino linkage, a sulfide linkage, a thiosemicarbazone linkage, a semicarbazone linkage, an oxime linkage, an ether linkage, or combinations of these linkages. Also disclosed are methods of synthesizing the compounds and/or precursors of the compounds.

Abstract: An antisense compound for use in treating myotonic dystrophy DM1 or DM2, a method of enhancing antisense targeting to heart and quadricep muscles, and a method for treating DM1 or DM2 in a mammalian subject are disclosed. The oligonucleotide has 8-30 bases, with at least 8 contiguous bases being complementary to the polyCUG or polyCCUG repeats in the 3?UTR region of dystrophia myotonica protein kinase (DMPK) mRNA in DM1 or DM2, respectively. Conjugated to the oligonucleotide is a cell-penetrating peptide having the sequence (RXRR(B/X)R)2XB, where R is arginine; B is ?-alanine; and each X is —C(O)—(CH2)n—NH—, where n is 4-6. The antisense compound is effective to selectively block the sequestration of muscleblind-like 1 protein (MBNL1) and/or CUGBP, in heart and quadricep muscle in a myotonic dystrophy animal model.

Abstract: The present invention relates to novel amide derivatives of the lantibiotic 97518 and their uses. In particular, the present invention describes novel compounds having general formula (II) and their use as antibiotic.

Abstract: The present disclosure provides solid forms of a compound of formula I. In some embodiments, the present disclosure provides crystalline forms of Compound I. In some embodiments, the present disclosure provides solvate forms of Compound I. In some embodiments, the present disclosure provides amorphous Compound I.

Abstract: Modified relaxin polypeptides and their uses thereof are provided

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

Abstract: The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of viral disease.

Abstract: The present disclosures provides isolated or purified compounds, each of which bind to a metal atom. Generally, the compounds are small in size (e.g, molecular weight of less than about 1 kDa) and peptidic in nature, inasmuch as the compounds comprise amino acids. In some embodiments, the compound comprises a structure of Formula I: M1-P1-M2-P2 wherein each of P1 and P2 is a peptide comprising at least two amino acids, M1 is a first metal binding moiety comprising a substituted imidazolone ring, M2 is a second metal binding moiety comprising a substituted oxazolone ring, and wherein M1 and M2 bind to a single metal atom. Also provided are related complexes, conjugates, cells which synthesize the compounds of the present disclosures, substantially homogenous cultures thereof, kits and compositions, and methods of making or using the materials of the present disclosures.

Abstract: The present invention provides nucleic acid delivery polyplex complexes and anionic open polyplexes comprising a nucleic acid molecule reversibly bound to one or more of nucleic acid delivery polyplex complexes.

Abstract: Methods, systems and compositions comprising novel peptidomimetics are disclosed that can be used to inhibit calpain and, more specifically, to treat tissue damage caused by pathologic activation of calpains.

Abstract: A drug using the magnetic properties of a metal salen complex as represented by the following general formula in order to magnetize the intended drug by chemically binding the drug to a metal salen complex so that the drug can be delivered to the target diseased site. The drug can be delivered to the diseased site using the magnetic properties of the drug per se without using a carrier made of a magnetic substance as in the conventional methods.