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 invention provides protein nanorings.

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 invention provides small molecule mimics of the Smac peptide that are dimer- or dimer-like compounds having two 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: It is an object of the present invention to provide a substance usable as an anticancer agent or DDS, which has intracellular stability, which is capable of evading side effects from functional disorder with respect to normal cells, or which has instantaneous effect. The inventors developed a novel chimeric peptide targeting cancer cells which overexpress EGFR or the like using a binding peptide such as a peptide sequence binding to EGFR, and a lytic peptide sequence, thereby solving such an object. Particularly, by using a chimeric peptide including an EGF receptor-binding peptide or the like and a cytotoxic peptide, this object was solved.

Abstract: We have disclosed dicephalic amphiphiles having peptide sequences as the head groups. We have also disclosed self-assembly hydrogels prepared from the dicephalic peptide amphiphiles. These hydrogels are useful for the encapsulation and delivery of bioactives to a patient.

Abstract: The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. Peptide complexes also are provided. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, and identify a TFPI-binding compound.

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

Abstract: The present invention provides novel lipoglycopeptide compounds which are Type 1 signal peptidase inhibitors (SpsB). Compounds of the present invention are useful for the treatment of various bacterial related infectious diseases, particularly when used as a potentiator of a ?-lactam antibiotic such as imipenem and ertapenem. Accordingly, the present invention provides a method for the treatment of bacterial related infections using the compounds described herein, either alone or in combination with a ?-lactam antibiotic.

Abstract: The present invention provides polypeptide inhibitors of HSP27 kinase, compositions thereof, and methods for using such polypeptides and compositions for various therapeutic uses.

Abstract: The invention provides an improved process for preparing romidepsin. The process involves producing, purifying, or storing romidepsin under conditions that prevent the formation of undesired adducts. Purifying romidepsin at an apparent pH lower than approximately 6.0 (e.g., between an apparent pH of 4.0 and 6.0) has been discovered to prevent the reduction of the disulfide bond of romidepsin and the subsequent formation of dimerized, oligomerized, or polymerized adducts. The invention also provides pharmaceutical compositions of monomeric romidepsin free of dimerized, oligomerized, or polymerized adducts.

Abstract: The application provides synthetic peptide conjugates capable of targeting and causing ablation of adipose tissue in mammal comprising at least one targeting peptide and at least one therapeutic peptide. The synthetic peptide conjugates are envisaged to have decreased physiological toxicity and/or enhanced in situ cytotoxicity compared to the peptide CKGGRAKDC-GG-D(KLAKLAKKLAKLAK) (SEQ ID NO: 2).

Abstract: Provided is a macromolecule comprising two or more functionalized bis-peptides connected by one or more linkers, and methods of making thereof. In some embodiments, the functionalized bis-peptides are covalently attached to one or more functionalized bis-peptides to form linear strings of functionalized bis-peptides, macrocycles of functionalized bis-peptides, three-dimensional networks of functionalized bis-peptides, and combinations of any of these. Also provided is a macromolecule comprising two or more bis-peptides connected by one or more linkers, and methods of making thereof. In some embodiments, the bis-peptides comprise non-functionalized bis-peptides, functionalized bis-peptides or a combination of both functionalized and non-functionalized bis-peptides. In some embodiments, the bis-peptides are covalently attached to one or more bis-peptides to form linear strings of bis-peptides, macrocycles of bis-peptides, three-dimensional networks of bis-peptides, and combinations of any of these.

Abstract: The present invention concerns glutathione-lanthionine compounds, the process of preparing such compounds, and their use. The invention also concerns methods of using the compounds and derivatives and combinations of these compounds in the treatment and/or prevention diseases, including diseases affecting the central nervous system.

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

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: The present invention provides a novel macrocyclic compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

Abstract: A Smac mimetic therapy wherein the Smac mimetic is selected and developed based at least in part on its cIAP degradation properties.

Abstract: The method for producing a surfactin or a salt thereof according to the present invention comprises the steps of adding an organic solvent containing a branched alkyl alcohol to a culture fluid containing the surfactin or the salt thereof, or to a solution obtained by removing an insoluble component from the culture fluid, and extracting the surfactin or the salt thereof with the organic solvent, wherein the surfactin or the salt thereof is represented by the formula (1): wherein * indicates an optically active center; X is an amino acid selected from leucine, isoleucine and valine; R is a C9-13 alkyl group or a C9-13 branched alkyl group; and M is an alkali metal, an alkaline earth metal, an optionally-substituted amine or the like.

Abstract: The present invention relates to novel multimeric inhibitors of viral entry into cells and their use for the prophylaxis and treatment of viral infections.

Abstract: A method for treating disorders involving deregulation of cell proliferation and/or angiogenesis comprising the administration of an effective amount of a multivalent synthetic compound comprising a support on which at least 3 pseudopeptide units are grafted, said compound being of formula (I).

Abstract: The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs.

Abstract: A melanocortin receptor agonist cyclic peptide of the formula where R, x and y are as defined in the specification, compositions and formulations including the peptide of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including sexual dysfunction such as male erectile dysfunction and female sexual dysfunction.

Abstract: [Problems] To provide a polypeptide having a novel structure and showing an activity of inhibiting angiogenesis or an activity of inhibiting osteoclastogenesis, and to provide a recombinant protein by constructing a method of purifying the above protein. To provide an ingredient useful in designing remedies for tendinitis, rheumatoid arthritis, arthritis deformans, malignant tumor, etc. [Means for Solving Problems] A novel soluble polypeptide protein.

Abstract: The present invention provides a multimeric form of a Tie 2 binding peptide monomer, wherein the multimeric form has Tie 2 agonist activity. The multimeric form, preferably a tetramer, stimulates angiogenesis and promotes wound healing. The present invention also features pharmaceutical compositions comprising the multimeric Tie 2 agonists, including those suitable for topical or systemic administration. Methods of using the multimeric Tie 2 agonists of the invention for stimulating angiogenesis and for promoting healing of wounds, such as diabetic ulcers or skin grafts, are also 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: The present application discloses a new multivalent peptide ligand specifically targeting polymorphonuclear leukocytes (PMNs) with favorable pharmacological parameters to monitor sites of inflammation for imaging. The detailed synthesis, characterization, and pharmacological evaluation of the ligands are reported here. Two separate peptide binding ligands for formyl peptide and tuftsin receptors were chosen to link together based on the high expression levels of the two receptors on activated PMNs The heterobivalency and pegylated links were incorporated in the structural design to improve the sensitivity of the detection and to improve the bioavailability along with blood clearance profile, respectively. Two chemical constructs: cFLFLF-(PEG)n-TKPPR-99mTc (n=4, 12) were evaluated in vitro with human PMNs for binding affinity and bioavailability. As a result, FLFLF-(PEG)12-TKPPR99mTc was found to have more favorable pharmacological properties and was therefore used for further in vivo studies.

Abstract: Provided are compounds and methods of making compounds containing two or three groups derived from a peptide, such as enfuvirtide or exenatide, covalently bound to a linker. The compounds may contain polyethylene glycol groups to enhance solubility and pharmacokinetic properties. The compounds are useful for the treatment of diseases or conditions subject to treatment with the parent peptide, such as HIV and AIDS in the case of enfuvirtide, or diabetes in the case of exenatide.

Abstract: The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.

Abstract: The instant invention refers to an antibacterial peptide with all aminoacids in D-configuration, possessing strong antimicrobial activity against Gram-negative and Gram-positive bacteria and Candida strains. The peptide can be in linear form or multimerised on a skeleton of polyacrylamide, of dextrane units or on a skeleton of ethylene glycol units. The peptide is resistant to proteolysis especially when synthesized in the tetra-branched form where identical peptide sequences are linked together by an appropriate molecular scaffold.

Abstract: The present invention provides compounds of formula M-L-M? (where M and M? are each independently a monomeric moiety of Formula (I) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.

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: The present invention provides peptidomimetic macrocycles capable of modulating growth hormone levels and methods of using such macrocycles for the treatment of disease.

Abstract: Provided herein are peptidomimetics and their salts having a stable, internally constrained protein secondary structure containing a thioether-, ether-, or alkylamine-linked hydrogen bond surrogate; compositions containing at least one of these, and methods of making and using these.

Abstract: An azapeptide derivative of growth hormone releasing peptide (GHRP) of Formula I: A-(Xaa)a-N(RA)—N(RB)—C(O)-(Xaa?)b-B which binds to CD 36.

Abstract: The invention relates to peptide derivatives (peptides and pseudo-peptides) and the use thereof as vectors for molecules of interest. The invention also relates to conjugates containing a peptide derivative of the invention bound to a molecule of interest. The peptides of the invention can be used, in particular, to vectorize, generally in the form of prodrug conjugates, molecules of pharmaceutical or diagnostic interest such as, for example, therapeutic molecules, imaging or diagnostic agents, or molecular probes, across cell membranes of different tissues or organs, healthy or pathologic, and in particular to enable their transport across physiological barriers of the nervous system such as the Blood brain barrier (BBB), Blood-spinal cord barrier (BSCB), or Blood-retinal barrier (BRB).

Abstract: The present invention relates generally to branched macromolecules bearing functional moieties. In particular, the invention relates to dendrimers, derived from lysine or lysine analogues, bearing a plurality of functional moieties. The invention further relates to the use of such macromolecules, particularly in therapeutic applications, and compositions comprising them.

Abstract: The present invention is directed to cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity, preferably Kitastatin 1. The present invention is further directed to methods of inhibiting cancer cell growth and/or microbial growth in a host inflicted therewith by administering cyclodepsipeptide compounds to the inflicted host.

Abstract: Methods of modulating interfacial characteristics in a self-assembled, force-transmitting peptide network at a fluid-fluid interface are disclosed. The methods involve exposing a peptide capable of participating in a self-assembled, force-transmitting peptide network, either before or after it interacts with other peptides to form the peptide network to a stimulus that alters the chemical and/or physical properties of the peptide. Use of such methods in applications such as emulsions and foams are also disclosed.

Abstract: The present invention relates to an ecPNA having the general structure: H2N—X—B—Y—COOH and uses thereof, wherein X is A or C and Y is A or C with the proviso that when X is A, Y is C, and when X is C, Y is A; A represents an oligopeptide structure, the sequence of which comprises a sequence which renders the compound able to enter the nucleus of a cell; B represents a peptide nucleic acid (PNA) structure at least 12 nucleotides in length, the sequence of which is capable of hybridizing with a DNA within the nucleus of the cell, which DNA is within a promoter region of a gene; C represents an oligopeptide structure; and each — represents a chemical linkage between the structures at each side thereof, which may be the same as or different from each other such linkage.

Abstract: The invention provides compositions useful as molecular probes. In particular, the invention provides activatable cell penetrating peptides comprising a fluorescence donor and a fluorescence acceptor. Exemplary fluorescence donors and fluorescence acceptors include compounds derived from cyanine. Also provided are ratiometric, multispectral, and excitation lifetime imaging methods for detecting the molecular probes provided herein.

Abstract: Zwitterion-containing compounds for the modification of hydrophobic molecules to improve their solubility and/or to lower their non-specific binding as provided. The zwitterion-containing compounds may be suitable for modification of detectable labels such as biotin and fluorescein to improve their solubility. The zwitterion-containing compounds may also be useful for the preparation of conjugates of proteins, peptides and other macromolecules or for crosslinking molecules and/or macromolecules.

Abstract: The invention encompasses radiopharmaceutical compounds that can be used in imaging cell death associated with either apoptosis or necrosis. Phosphatidylethanolamine (PtdE) is externalized to the surface of apoptotic cells, and also becomes accessible in necrotic cells due to compromised plasma membrane integrity. Duramycin, a 19 amino acid polypeptide, binds PtdE at a 1:1 ratio with high affinity and exclusive specificity. Novel Duramycin-based radiopharmaceuticals and non-radioactively labeled compounds are disclosed herein. Such compounds facilitate detection of cell apoptosis and/or necrosis by binding to PtdE. The location of the bound compound can then be pinpointed using standard imaging techniques.

Abstract: A composition for promoting lacrimal secretion which can be used safely and effectively in the lacrimal secretion promoting therapy, not in the conventional supplemental therapy of lacrimal fluid components is provided. The composition for promoting lacrimal secretion comprising a peptide derivative represented by the formula (I): and a contact lens which retains and/or contains the composition are provided.

Abstract: In alternative embodiments, the invention provides apratoxin F and apratoxin G compounds, which include apratoxin F and apratoxin G stereoisomers, derivatives and analogs compositions and methods. In alternative embodiments, the invention provides pharmaceutical compositions and formulations comprising apratoxin F (compound 6 of FIG. 1) and apratoxin G (compound 7 of FIG. 1) and their stereoisomers, derivatives and analogs. In alternative embodiments, pharmaceutical compositions and formulations of the invention are administered in an amount sufficient to treat, prevent and/or ameliorate a disease or condition that can be ameliorated by decreasing or inhibiting cell growth, e.g., pathological, uncontrolled or unwanted cell growth, e.g., a cancer or a metastases, or any disease or condition (e.g., allergy) or infection having a hyperproliferative cell growth component.

Abstract: The invention relates to a nucleic acid molecule selected from the group comprising a) a nucleic acid molecule having one of the nucleotide sequences presented in SEQ ID:NO 4 to SEQ ID:NO 8, b) a nucleic acid molecule that codes for a peptide having one of the amino acid sequences presented in SEQ ID:NO 12 to SEQ ID:NO 16, c) a nucleic acid molecule, the complementary strand of which hybridizes to a nucleic acid molecule according to a) or b) and which codes for a peptide having antimicrobial activity, and d) a nucleic acid molecule, the nucleotide sequence of which deviates from the nucleotide sequence of a nucleic acid molecule according to c) because of the degenerated genetic code.

Abstract: The present invention provides a metastin derivative in which the amino acids comprising metastin were modified by alternative chemical substituents resulting in metastin derivitives, having excellent blood stability and exhibiting cancer metastasis inhibiting action or cancer growth inhibiting action.

Abstract: Disclosed are ?-amino acid monomers containing cylcoalkyl, cycloalkenyl, and heterocylic substituents which encompass the ? and ? carbons of the peptide backbone and ?-polypeptides made from such monomers. Method of generating combinatorial libraries of polypeptides containing the ?-peptide residues and libraries formed thereby are disclosed.

Abstract: The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity.

Abstract: The invention provides synthetic heparin-binding growth factor analogs having two peptide chains each branched from a branch moiety, such as trifunctional amino acid residues, the branch moieties separated by a first linker of from 3 to about 20 backbone atoms, which peptide chains bind a heparin-binding growth factor receptor and are covalently bound to a non-signaling peptide that includes a heparin-binding domain, preferably by a second linker, which may be a hydrophobic second linker. The synthetic heparin-binding growth factor analogs are useful as pharmaceutical agents, soluble biologics or as surface coatings for medical devices.