Abstract: The present invention discloses a method of assaying Fc-function in an immunoglobulin containing sample by contacting the sample, in the presence of a complement, with red blood cells modified to incorporate a F-S-L peptide-lipid construct. The F-S-L peptide construct comprises a functional group (F) that is a target antigen for a complement activating immunoglobulin, a spacer group (S) covalently linking F to L and a lipid group (L). The present invention further discloses a specific construct, DOPE-Ad-CMG(2)-hCMV2 where the F group is an antigen of cytomegalovirus, that is used in assaying the Fc function of an intravenous immunoglobulin (IVIG) product.

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: A method of inhibiting a binding event between a target protein and a binding protein, comprising administering to a cell in vitro an effective amount of a non-naturally occurring bifunctional inhibitor molecule including (a) protein binding moiety, and (b) an effector region, wherein the protein binding moiety binds to a blocking protein, and wherein the effector region binds to the target protein in order to bind the target protein and the blocking protein and prevent access of the binding protein to the target protein. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: The present invention provides Immunosuppressive compounds capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The present invention further provides peptide based compositions for treatment of cancer or treatment of infections via immunopotentiation caused by inhibition of immunosuppressive signalling induced by PD-1, PD-L1, or PD-L2 and therapies using them, immunopotentiative substrates included as the active ingredient. Further, the invention provides pharmaceutical compositions comprising the Immunosuppressive peptide compounds or modified peptide moieties for preventive and/or therapeutic agents for cancer, cancer metastasis, immunodeficiency, an infectious disease or the like and an application of PD-1 or PD-L1 as a testing or diagnostic agent or a research agent for such a disease.

Abstract: The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The invention relates to a compound of the general structure (I), where R is a hydrogen atom (II) or an unsubstituted, monosubstituted or polysubstituted C1-C20-alkyl, wherein the alkyl is straight, branched, cyclic and/or partially unsaturated, or an unsubstituted, monosubstituted or polysubstituted phenyl group.

Abstract: Embodiments of the invention are directed to a one-bead-two-compound method for the creation of encoded cyclic peptoid libraries. This scheme is useful for the creation of cyclic peptoid microarrays since only the cyclic peptoid, not the linear encoding molecule, contains an attachment residue and thus can be spotted onto an activated substrate.

Abstract: A cyclic organic compound which comprises 16 amino acids or 17 amino acids and has no carboxyl group C-terminally and/or no amino group N-terminally. Optionally, one of the amino acids is a nonnatural amino acid. The ring closure is formed between a side chain of one amino acid and the C-terminus of another amino acid, or the ring closure is effected with the aid of a nonnatural amino acid. A process for producing and using the compound for regulating vectorial ion channels, for treating diseases associated with the lung function and for treating oedemas is provided.

Abstract: The disclosure relates to the field of candidate drug testing and drug development. Described are methods for providing a compound composed of at least one molecule attached via at least two linkages to a molecular scaffold, the method comprising providing a scaffold comprising at least a first and a second reactive group; providing at least one molecule able to react with the at least first and second reactive group; and contacting the scaffold with at least one molecule to form at least two linkages between the scaffold and the molecule in a coupling reaction, wherein the formation of a linkage accelerates the formation of a consecutive linkage. The coupling reaction may be performed in solution, such as an aqueous solution. Furthermore, described is a method for selecting a candidate drug compound comprising providing a library of the compounds and determining the binding of a target molecule to the compounds.

Abstract: Methods for use of a melanocortin receptor agonist cyclic peptide of the formula where R, x and y are as defined in the specification, and compositions and formulations including the peptide of the foregoing formula, for preventing, ameliorating or treating female sexual dysfunction.

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: 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: A zinc finger-like peptide for treating cancer, a pharmaceutical composition containing the zinc finger-like peptide and a method for treating cancer are disclosed. In the present invention, the zinc finger-like peptide for treating cancer comprises: at least seven amino acids, wherein the sequence of the at least seven amino acids has 85-100% similarity to a sequence represented by SEQ ID NO: 1.

Abstract: The invention provides small molecule mimics of the Smac peptide that are dimer-like or trimer-like compounds having two or three amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.

Abstract: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract: The present invention aims at providing motilin-like peptide compounds that maintain the gastrointestinal motility stimulating activity of native motilin and which are adapted to have higher absorbability upon transmucosal administration. Motilin derivatives were designed and synthesized in consideration of the pathway for the degradation of motilin at a site of its transmucosal absorption and the maintenance of motilin's physiological activity and compounds characterized by substitutions for the amino acid at position 21 of native motilin have been found to show higher absorbability upon transmucosal administration and yet maintain the same activity as motilin.

Abstract: Compounds comprising peptides capable of binding C3 protein and inhibiting complement activation are disclosed. These cyclic compounds are modified to improve stability while maintaining substantially equivalent complement activation-inhibitory activity as compared with currently available compounds. The compounds comprise compstatin analogs in which the disulfide bond between C2 and C12 is modified via a thioether bond to form a cystathionine.

Abstract: The present invention provides extracts of material fermented with Paenibacillus sp., preferably the one called here Paenibacillus elgii ourofinensis with antimicrobial activity and/or growth promoter in animals intended for slaughter for human consumption. The invention provides new peptides derived from the fractions of the fermentation of Paenibacillus elgii ourofinensis extract, said new peptides having antimicrobial activity and promoting the growth of organisms, for example, plants and animals. The invention is also related to the use of the extract of this new strain, Paenibacillus elgii ourofinensis, as a growth promoter and as an antimicrobial agent in the treatment and prophylaxis of animals intended for human consumption.

Abstract: The invention relates to compositions that comprise dendrimers useful in medical and veterinary applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the dendrimer through a linkage that releases the drug or a prodrug through controlled beta elimination.

Abstract: A fusion protein of the invention comprises an immunoglobulin Fc region and a first target protein linked to the immunoglobulin Fc region. The first target protein comprises a collagen XVIII fragment, preferably endostatin. The immunoglobulin Fc region preferably comprises a hinge region, a CH2 region, and a CH3 region.

Abstract: This invention relates to a conjugated molecule comprising a peptide derived from the CD4 receptor coupled to an organic molecule by means of a linker as well as a process for its preparation. Said organic molecule comprises a 5 to 21 amino acid anionic polypeptide. Such a conjugated molecule can be used in antiviral treatment, namely in the treatment of AIDS.

Abstract: Novel peptoids are disclosed that have a formula represented by the following formulae Ia and Ib: wherein X, Y, R, and n are as described herein. The peptoids demonstrate catalytic activity and are useful in substrate-selective catalytic transformations, including asymmetric catalytic transformations.

Abstract: The invention relates to a method or process for solution phase 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 invention relates to a peptide compound with biological activity, which in particular possesses antimicrobial properties, its preparation and its applications.

Abstract: Provided herein are inventive enopeptin compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Further provided are methods of preparation, use, and treatment.

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: The instant invention describes macrocyclic compounds having therapeutic activity, and the mechanism and methods of treating disorders such as autoimmune diseases, inflammation, and cancer, tumors and cell proliferation related disorders.

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 invention described herein pertains to processes for preparing tubulysin derivatives, conjugates of tubulysins, and intermediates therefore.

Abstract: Multiligand constructs and intermediate multivalent constructs for use in their preparation. The multiligand constructs have utility in diagnostic and therapeutic applications.

Abstract: Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.

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 invention relates to methods for effecting qualitative and quantitative changes in the functional moieties expressed at the surface of cells and multi-cellular structures, and functional lipid constructs for use in such methods. In particular, the invention relates to functional lipid constructs and their use in diagnostic and therapeutic applications, including serodiagnosis, where the functional moiety is a carbohydrate, peptide, chemically reactive group, conjugator or fluorophore.

Abstract: The present invention relates to oligomer compounds, including dimers and trimers, formed by a disulfide, sulfinyl thio, olefin or hydrocarbon bond, or a hydrazone exchange bond between two or more monomers. Methods of making the monomers and the oligomers is also disclosed. Use of the compounds for inhibiting the activity of target RNA molecules, particularly those having a secondary structure that include a stem or stem-loop formation. Dimer compounds capable of inhibiting the activity of an HIV-1 RNA frameshifting stem-loop and a (CUG)n expanded repeat stem-loop are disclosed, as are methods of treating diseases associated with these target RNA molecules.

Abstract: The present invention relates to novel polypeptides, methods for their synthesis, pharmaceutical compositions comprising the novel polypeptides as well as their use in medicaments for therapeutic applications.

Abstract: The present invention relates to novel peptides and methods for inducing an immune response in a subject against an antigen and for treatment, diagnosis and prognosis of infections or autoimmune diseases including infections with HCV, HIV, CMV and Flu. The invention further relates to methods for identifying and providing peptides useful for the treatment and diagnosis.

Abstract: The present invention relates to methods of treating or preventing retinal ganglion cell (RGC) death and/or glaucoma using modulators of neurotrophic receptors that comprise ?-turn peptidomimetic cyclic compounds or derivatives thereof. The neurotrophic receptor modulators can be used alone, in combination and/or in conjunction with one or more other compounds, molecules or drugs that treat or prevent ocular hypertension, RGC death and/or glaucoma.

Abstract: The invention provides a nucleic acid encoding the 37-kDa pneumococcal surface adhesion A protein (PsaA) from Streptococcus pneumoniae. The invention also provides purified polypeptides encoded by the nucleic acid encoding the 37-kDa protein from and the nucleic acids comprising unique fragment of at least 10 nucleotides of the 37-kDa protein. Additionally, multiple antigenic peptides that provide protection against S. pneumoniae challenge are provided. These multiple antigen peptides comprise the peptides that immunospecifically bind to the monoclonal antibodies. Also provided are vaccines comprising such immunogenic peptides, and methods of conferring protective immunity against Streptococcus pneumoniae infection by administering therapeutic composition comprising the immunogenic peptides of the invention.

Abstract: Provided are methods of making carrier polypeptide that include incorporating a first unnatural amino acid into a carrier polypeptide variant, incorporating a second unnatural amino acid into a target polypeptide variant, and reacting the first and second unnatural amino acids to produce the conjugate. Conjugates produced using the provided methods are also provided. In addition, orthogonal translation systems in methylotrophic yeast and methods of using these systems to produce carrier and target polypeptide variants comprising unnatural amino acids are provided.

Abstract: In general, the invention relates to methods of synthesizing AbA derivatives that are useful for treating infection and amenable to further chemical elaboration. These novel methods are scalable for industrial production and employ safer, simpler, and more efficient process conditions. Furthermore, the invention also provides novel compounds and intermediates useful for implementing the methods described herein and/or for the treatment of infection.

Abstract: The present invention relates to crystalline and crystal-like forms of lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention relates to methods of purifying lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention also relates to pharmaceutical compositions comprising the purified form of the lipopeptide and methods of using these compositions.

Abstract: The present invention discloses a process for the preparation of Caspofungin and its intermediates from Pneumocandin B0.

Abstract: The invention relates to methods of localizing biofunctional moieties (F) to surfaces and synthetic constructs of the general structure F-S-S? for use in such methods. F is the biofunctional moiety, S is a spacer covalently linking F to S?, and S? is sterol. In particular, the invention relates to the preparation of biofunctional surfaces and surface modified biological structures including cells (kodecytes), enveloped viruses (kodevirions) and liposomes or virosomes (kodesomes).

Abstract: The invention provides small molecule mimics of the Smac peptide that are dimers or dimer-like compounds having two binding domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.

Abstract: The subject application pertains to a compound of structure IX or X: or a pharmaceutically acceptable salt thereof, wherein: X is —C(?O)N(R10)— or —CH(OPr3) —; R7, R9 and R10 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid; Pr1 and Pr2 are the same or different and represent hydrogen or a thiol protecting group; Pr3 is hydrogen or an alcohol protecting group; R1, R2, R5 and R6 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid, or R1 and R2 and/or R5 and R6, taken together with the carbon atom to which they are attached, form a spirocyclic moiety, with the proviso that: each of R1 and R2 is not hydrogen, or each of R5 and R6 is not hydrogen.

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: There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

Abstract: Drug Linker compounds and Drug Linker Ligand conjugates are provided that have auristatins linked via the C-terminus. The conjugates show efficacy without the need for a self-immolative group to release the drug.

Abstract: The present invention relates to linker molecules that readily conjugate cellular recognition ligand at one end and drug payload at the other, and are useful in treating or preventing cancer, an autoimmune disease, an inflammatory condition, a central nervous system disorder or an infection.

Abstract: The present invention provides Ligand-Drug Conjugates, Drug-Linkers, Linkers, and Ligand-Linker Conjugates comprising a self-stabilizing linker assembly component.