Abstract: The invention relates to novel antimicrobial, including antibacterial and antifungal, agents and compositions based on hemin derivatives of general formula (I), and also to the production of novel hemin derivatives. The advantages of antibacterial agents based on hemin derivatives are their biocompatibility, biodegradability, high effectiveness against resistant bacteria and widespread microfungi that are harmful to humans, and freedom from toxicity and side effects.

Abstract: Provided herein are novel compounds and novel protected compounds that can be derived from polymyxin, including, e.g., polymyxin A. The novel compounds have antibacterial properties against a diverse range of Gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin A. Also provided are antibacterial pharmaceutical compositions containing the novel compounds and novel protected compounds, as well as methods for preparing the antibacterial compounds and protected compounds.

Abstract: The present invention provides compositions for preventing growth and proliferation of biofilm embedded microorganisms on devices comprising: (a) a cationic polypeptide and (b) a bis-guanide or a salt thereof. The invention further provides methods for preparing medical devices with such compositions.

Abstract: The application relates to antimicrobial agents against Gram-negative bacteria, in particular to fusion proteins composed of an enzyme having the activity of degrading the cell wall of Gram-negative bacteria and a peptide stretch fused to the enzyme at the N- or C-terminus, as well as pharmaceutical compositions thereof. Moreover, it relates to nucleic acid molecules encoding such a fusion protein, vectors carrying the nucleic acid molecules and host cells transformed with either the nucleic acid molecules or the vectors. In addition, it relates to such a fusion protein for use as a medicament, in particular for the treatment or prevention of Gram-negative bacterial infections, as diagnostic means or as cosmetic substance. The application also relates to the treatment or prevention of Gram-negative bacterial contamination of foodstuff, of food processing equipment, of food processing plants, of surfaces coming into contact with foodstuff, of medical devices, of surfaces in hospitals and surgeries.

Abstract: This invention provides novel targeted antimicrobial compositions. In various embodiments chimeric moieties are provided comprising an antimicrobial peptide attached to a peptide targeting moiety that binds a bacterial strain or species.

Abstract: Disclosed herein are novel peptides and protected peptides. These compounds can be derived from naturally occurring peptides, such as those selected from colistin, circulin A, polymyxin A, polymyxin B, polymyxin D, octapeptin B, octapeptin C, and [Ile7]polymyxin B1. Also disclosed are pharmaceutical compositions containing the new peptides, as well as methods for preparing the novel peptides and protected peptides.

Abstract: Multilayer films comprised of polypeptide epitopes and a toll-like receptor ligand are described. The multilayer films are capable of eliciting an immune response in a host upon administration to the host. The multilayer films can include at least one designed peptide that includes one or more polypeptide epitopes from a virus, bacteria, fungus or parasite.

Abstract: Disclosed are an antibiotic peptide and the like, having an amino acid sequence of Ac-Phe-Lys-Lys-Leu-Lys-Lys-Leu-Phe-Ser-Lys-Leu-Trp-Asn-Trp-Lys-NH2 (SEQ ID No:1). Also disclosed are a method of preparing the antibiotic peptide and the like, and the application thereof. The antibiotic peptide and the like synthesized by the solid phase synthetic technology according to the present invention can be used as a formulation against microbial infection and as alternate or adjuvant medicaments of antibiotics in the prior art.

Abstract: The present invention relates to monomeric and multimeric peptidic compounds which have antipathogenic, in particular antiviral or/and antibacterial activity. In a preferred aspect, the peptide compounds of the invention have an activity in respect of a broad spectrum of viruses, both DNA and RNA viruses, irrespective of whether they possess virus envelope or not. Further, the present invention refers to compositions comprising said peptidic compounds for medical use, i.e. for the treatment or prevention of pathogenic, in particular viral or/and bacterial infections.

Abstract: Compositions and methods relating to interfering with the interaction of gangliosides, such as GM1, with their ligands are provided. For example, methods are provided for treating infections by blocking the infectious agent from binding with GM1 using GM1-like peptides. Also provided are methods of inhibiting ligands from binding to GM1 on the surface of cells and for neutralizing anti-GM1 antibodies in neurological diseases.

Abstract: Provided are fragments of human p97 (melanotransferrin) polypeptides having blood-brain barrier (BBB) transport activity, including variants and combinations thereof, conjugates comprising said p97 fragments, and related methods of use thereof, for instance, to facilitate delivery of therapeutic or diagnostic agents across the BBB.

Abstract: The present invention relates to novel combined laundry detergent, bleach, and antimicrobial composition incorporating novel sulfoperoxycarboxylic acid compounds, and methods for making and using them. The sulfoperoxycarboxylic compounds used in compositions of the invention are storage stable, water soluble and have low to no odor. Compositions of the invention may be in the form of a liquid, a solid, or a gel. The sulfoperoxycarboxylic compounds useful in preparing compositions of the present invention can be formed from non-petroleum based renewable materials.

Abstract: Disclosed are novel antimicrobial peptides which can promote the regeneration of skin cells, thus healing wounds. Pharmaceutical compositions comprising the peptides as active ingredients are also provided for wound healing and skin rejuvenation. The antimicrobial peptides exhibit inhibitory activity against antibiotic-resistant strains, and their antimicrobial activity is maintained without loss of structural stability even under a high salt condition. Also, being proven to promote the migration and regeneration of skin cells in mice as well as in vitro, the antimicrobial peptides may be widely used as an agent for regenerating skin cells. Further, they can find applications in various fields including the medical industry and the cosmetic industry. Hence, the novel antimicrobial peptides are anticipated to have considerable repercussions in the market for antibiotics, wound healing agents and cosmetics.

Abstract: Described herein are compositions comprising at least one buffering agent, at least one chelating agent and at least one antimicrobial agent, which can be used for treating and/or preventing diseases or disorders in a variety of animals. In certain embodiments, in particular, the compositions can be used for treating and/or preventing ophthalmic and oral cavity diseases or disorders in dogs and cats and oropharyngeal and/or guttural pouch diseases or disorders in equines. In certain embodiments, the compositions can also be used for treating ophthalmic or oral cavity diseases or disorders in humans.

Abstract: The present invention encompasses combination comprising a plurality of amino acids, formulations thereof for use in humans and animals, as well as methods for increasing muscle protein synthesis, muscle strength, and/or muscle function.

Abstract: The present disclosure relates generally to antimicrobial peptides, methods for their use, and methods for preparing devices having surfaces which are modified to incorporate OH said peptides. In some embodiments, the antimicrobial peptides are antimicrobial OH cationic peptides modified to comprise a thiol functional group.

Abstract: The present invention relates to a plant disease control agent containing a compound represented by the following formula (1) or salt thereof as an active ingredient (in the formula, R1 and R2 represents a hydrogen atom or methyl group but excepting cases where R1 and R2 are the same), a plant disease controlling method applying the plant disease control agent on plants suffering from diseases, and a novel compound represented by formula (1) or salt thereof.

Abstract: The present invention relates to compositions and methods for treating autoimmune, microbial, metabolic, neoplastic, and posttraumatic diseases mediated by inflammation in a subject. Compositions and methods including at least one importin beta-selective nuclear transport modifier (NTM) and/or at least one importin alpha-selective NTM, and/or at least one importin alpha-specific NTM, and/or at least one inhibitor of importin alpha and importin beta complex formation may be administered to a subject to modulate the transport of transcription factors, mediated by nuclear import adaptors, into the nucleus of a cell resulting in a decrease or abrogation of inflammation.

Abstract: It is an object of the present invention to provide improved pharmacological properties to molecules which bind to a target with low affinity (hereinafter referred to as a “ligand moiety”) through linkage of such molecules to a metal binding moiety, thereby generating a combination molecule commonly referred to as a “metallodrug” or “metallotherapeutic.” The metal binding domain of metallodrugs typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, resulting in modification of proteins and nucleic acids that are in close proximity due to binding of the ligand moiety to its target.

Abstract: Anti-microbial peptides and methods of use are provided.

Abstract: A composition and method adapted for delivery of hydrophilic, biologically-active agents are disclosed. The composition can include a reverse microemulsion formed from at least one hydrophilic, biologically-active agent solubilized by a hydrophobic reverse emulsion surfactant in a non-stinging, volatile, hydrophobic solvent. The non-stinging, volatile, hydrophobic solvent is selected from the group consisting of volatile linear and cyclic siloxanes, volatile linear, branched, and cyclic alkanes, volatile fluorocarbons and chlorofluorocarbons, liquid carbon dioxide under pressure, and combinations thereof. The reverse microemulsion can be an optically clear solution.

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 to methods of preparation of this inventive polymeric carrier molecule and of the inventive polymeric carrier cargo complex. The present invention also provides methods of application and use of this inventive polymeric carrier molecule 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 of such diseases.

Abstract: The present invention relates to a polypeptide with an amino acid sequence according to SEQ ID NO: 1 and fragments or derivatives thereof. The present invention further relates to fusion proteins comprising said polypeptide and an additional peptide stretch fused to said polypeptide at the N- or C-terminus. Moreover, the present invention relates to nucleic acid molecules encoding said polypeptide or fusion protein, vectors comprising said nucleic acid molecules and host cells comprising either said nucleic acid molecules or said vectors. In addition, the present invention relates to said polypeptide or fusion protein for use as a medicament, in particular for the treatment or prevention of Gram-negative bacterial infections, as diagnostic means, as cosmetic substance or as sanitizing agent.

Abstract: The present invention relates to methods and compositions for the treatment of diseases, including cancer, infectious diseases and autoimmune diseases. The present invention also relates to methods and compositions for improving immune function. More particularly, the present invention relates to multifunctional molecules that are capable of being delivered to cells of interest for the treatment of diseases and for the improvement in immune function.

Abstract: The present disclosure serves to reduce the healing time of tissue wounds, including those formed during surgery, whether necessary or elective (including cosmetic surgery), by providing a therapeutic dose of a pancreatic enzyme inhibitor.

Abstract: The present invention provides polyphenolic compositions derived from a plant that inhibit the formation of a biofilm. Also provided are combinations that comprise at least one phenolic phytochemical and at least one antimicrobial agent that inhibit the growth of an established biofilm. Further, the present invention provides methods for inhibiting the formation and growth of biofilms.

Abstract: Provided is a bacterial strain which produces a family of mosquitocidal toxins, Xenorhabdus MT, on deposit with the American Type Culture Collection, PTA-6826, insecticidal compositions comprising the mosquitocidal toxin(s) produced by Xenorhabdus MT, a mosquitocidal toxin preparation prepared from spent culture medium, whole culture or cells or a mixture thereof, of Xenorhabdus MT and method of insect control, especially mosquito control. Also provided are microbial compounds (same as mosquitocidal toxins) compositions comprising them and use in formulating therapeutic and other antimicrobial compositions, and methods of use for inhibiting microbial growth and for treating infection.

Abstract: The present invention provides compositions for controlled release of a peptidic molecule comprising a lipid-saturated matrix comprising a biocompatible polymer and a peptidic molecule associated with PEG. The present invention also provides methods of producing the matrix compositions and methods for using the matrix compositions to provide controlled release of the peptidic molecule.

Abstract: Compositions and methods for achieving hemostasis. Hemostatic compositions comprise a phospholipid, and optionally, an anti-infective agent. The hemostatic composition can be administered to a bleeding bone to achieve hemostasis.

Abstract: The invention concerns a novel antimicrobial peptide (AMP) polymer conjugate comprising at least one AMP, typically colistin, and a dextrin polymer wherein said dextrin polymer has a molecular weight between 5,000-60,000 g/mol and is modified by the additions of pendant groups which increase the stability of the conjugate and so delays its degradation thereby slowing the rate at which the AMP is released.

Abstract: The present invention describes novel single drug entities, formed by direct linkage of an antibiotic to a steroidal drug. Upon topical application to the eye, the conjugate would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs. The antibiotic is coupled directly to the steroid drug.

Abstract: Peptide compositions are disclosed that include fragments of surfactant protein-A, or a derivative thereof, wherein the fragment binds to TLR4. Methods of producing and using the peptide compositions are also disclosed.

Abstract: Novel peptoid oligomers are disclosed that have a formula represented by the following formula I: The peptoids demonstrate antimicrobial activity and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals including humans where microbial invasion is involved. The present cyclic and linear peptoids are particularly valuable as their effect is rapid, broad in spectrum and mostly indifferent to resistance provoked by standard antibiotics.

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. The compounds provided herein can in other embodiments overcome the resistance conferred by single amino acid mutations at defined positions of bacterial Signal Peptidases (SPases) and in other embodiments provide for a broader spectrum of antibiotic bioactivity compared to the natural product. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

Abstract: The invention relates to peptide derivatives of general formula (I): R1-AA1-AA2-R3-AA4-R2??(I) their stereoisomers, mixtures thereof, and their cosmetically or pharmaceutically acceptable salts, a method for obtaining them, cosmetic or pharmaceutical compositions containing them and their use for the treatment, care and/or cleansing of those conditions, disorders and/or pathologies of the skin, mucosae, scalp and/or nails resulting from microorganism proliferation or being at risk of microorganism proliferation.

Abstract: A method and formulation for preparing spray dried vancomycin. In various embodiment, the formulation includes vancomycin HCl (10-20%) and one or more of the following PEG (0-5%), mannitol (0-5%), ethanol (0-10%), and a citrate buffer. Spray dried vancomycin has favorable reconstitution times and water content.

Abstract: The invention provides a method for preventing or treating a disease caused by an extracellular microorganism, said method comprising systemically administering to a subject in need thereof a prophylactically or therapeutically effective amount of a salicylic acid (SAL) or a SAL analogue. The extracellular microorganism can be of the bacterial genus Staphylococcus, for example, Staphylococcus aureus. The extracellular microorganism can be a strain that is resistant to at least one antibiotic. The strain can be selected from the group consisting of methycillin-resistant Staphylococcus aureus (MRSA), vancomycin-intermediate Staphylococcus aureus (VISA) and vancomycin-resistant Staphylococcus aureus (VRSA).

Abstract: The present invention relates to novel sulfoperoxycarboxylic acid compounds, and methods for making and using them. The sulfoperoxycarboxylic compounds of the invention are storage stable, water soluble and have low to no odor. Further, the compounds of the present invention can be formed from non-petroleum based renewable materials. The compounds of the present invention can be used as antimicrobials, and bleaching agents. The compounds of the present invention are also suitable for use as coupling agents.

Abstract: The invention relates to multimeric forms of antimicrobial peptides, for example, defensin peptides. The multimeric forms of defensin peptides possesses antimicrobial activity and may be formulated into antimicrobial compositions, pharmaceutical compositions, eyedrop composition, contact lens solution compositions for coating medical devices and the like. The invention also relates to the use of these multimeric forms of peptides, e.g. multimeric forms of defensin peptides for inhibiting and/or reducing the growth of microorganisms in general, including in a host. The invention further relates to a method of preparing multimers of peptides derived from defensins, for example hBD3.

Abstract: The present invention generally relates to a novel highly discriminating antibiotic, plantazolicin, a plantazolicin-like compound and to pharmaceutical compositions comprising the same. Also provided are methods for producing and using plantazolicin. Due to its bactericidal activity against Bacillus anthracis, plantazolicin and plantazolicin-like compounds can be used in methods for treating and/or preventing anthrax infections.

Abstract: The present invention relates to treatment of inflammatory bowel diseases with mammal beta defensins.

Abstract: Antimicrobial compositions including a cell penetrating peptide (CPP) having the amino acid sequence Tyr-Ala-Arg-Val-Arg-Arg-Arg-Gly-Pro-Arg-Gly-Tyr-Ala-Arg-Val-Arg-Arg-Arg-Gly-Pro-Arg-Arg (SEQ ID NO:1) or variant thereof are disclosed. The CPP, which itself has antimicrobial properties, can be advantageously combined with or conjugated to a cargo to increase the delivery, efficacy, or combinations thereof, of the cargo into cells. In preferred embodiments, the CPP is combined with or conjugated to a functional nucleic acid, such as an external guide sequence (EGS) which can target and reduce expression of essential microbial genes or genes than impart resistance to antimicrobial drugs. Methods of using the compositions alone or in combination with traditional antimicrobial drugs to treat infections are also disclosed.

Abstract: The present invention relates to gel compositions comprising at least one entrapped active component.

Abstract: The present invention relates generally to novel depsipeptides, to methods for the preparation of these novel depsipeptides, to pharmaceutical compositions comprising the novel depsipeptides; and to methods of using the novel depsipeptides to treat or inhibit various disorders.

Abstract: An anhydrous multiphase gel system consisting of an outer lipid matrix and an inner phase gelled by means of a polymer is described, which can be obtained by a) Melting the lipid phase with the formation of a liquid lipid phase, b) Mixing and homogenizing polymers or polymer blends capable of swelling with the formation of a polymer phase to be dispersed, c) Combining the polymer phase with the liquid lipid phase and homogenizing the phases, and d) Cold stirring the phase mixture until a solid gel-like mixed structure of the entire system is formed. The anhydrous multiphase gel system is particularly suitable for taking up difficulty soluble active substances in high concentration and for providing topical and transdermal applications. The described system is called an EDRS, “Entrapped Drug Reservoir System”.

Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 12 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. These ?-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 12 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. These ?-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

Abstract: Provided herein is a novel binding pocket within NEDD8 co-E3 proteins that binds NEDD8 E2 enzymes. Particularly at its M-Terminus. Methods are provided for screening for compounds that bind to the disclosed E2-binding pocket in NEDD8 co-E3 proteins. Compounds that bind to the E2-binding pocket and optionally inhibit the activity of NEDD8 co-E3 proteins and pharmaceutical compositions comprising the same are further provided. The NEDD8 co-E3 inhibitors find use, as agents preventing the NEDDylation of a target protein, in inhibiting cell growth and methods for treating cancers, inflammatory disorders, and pathogenic infections. The preferred inhibitors are peptides corresponding to a M-terminal fragment of Dnc1, e.g. MTLASKLKRDD, MLKLRQLQKKKQ, and MIKLFSLKQQKK, which are substituted at the M-Terminus with an uncharged group (e.g. acyl).

Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Abstract: Characterization of the biosynthetic gene cluster for the lantibiotic actagardine, identification of a novel variant of actagardine and its biosynthetic cluster, and methods of production and use of actagardine are described.