Abstract: Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.

Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.

Abstract: The present invention relates to peptides comprising amino acids according to Formula I ((X)l(Y)m)n ??(I) wherein l, m and n are integers from 0 to 10; X and Y, which may be the same or different, are an amino acid selected from the group consisting of hydrophobic amino acids and/or cationic amino acids, together with methods for the use of the peptides in the treatment of microbial infections.

Abstract: Compounds represented by general Formula I may form photo-responsive hydrogels that can be modulated between a non-viscous liquid state and a hydrogel. Formula I is: where a stereochemical conformation of double bond “a” is cis- or trans-, Ak is an alkylene group; and R represents a series of two or more naturally occurring or synthetic amino acid residues.

Abstract: Scaffold comprises a polymer defining macropores and comprising hydroxypropylcellulose partially substituted by a substituent comprising a self-crosslinkable group, which is crosslinked through the self-crosslinkable group. The macropores have an average pore size larger than 50 microns and are at least partially interconnected. In one method, bicontinuous emulsion comprising a continuous aqueous phase and a continuous polymer phase is formed. The polymer phase comprises hydroxypropylcellulose partially substituted by a substituent comprising a self-crosslinkable group, and is crosslinked through the self-crosslinkable group to form a polymer defining at least partially interconnected pores. In another method, phase separation is induced in a solution comprising a polymer precursor and water to form a bicontinuous emulsion comprising a continuous polymer phase and a continuous aqueous phase.

Abstract: The invention relates to pharmaceutical compositions comprised of a chemical moiety attached to an active agent in a manner that substantially decreases the potential of the active agent to cause overdose or to be abused. When delivered at the proper dosage the pharmaceutical composition provides therapeutic activity similar to that of the parent active agent.

Abstract: The present invention relates to new molecularly imprinted polymers which are suitable for the selective recognition of glutathione GSH and/or of an analog thereof, and in particular which are of use for the treatment of media comprising in particular a mixture of glutathione GSH, and/or of an analog thereof, with GSH adducts.

Abstract: Compositions comprising a tripeptide having the sequence XC1C2; wherein X is any amino acid such that XC1C2 is capable of binding a metal in a square planar orientation or square pyramidal orientation or both; and wherein C1 and C2 are the same or different; and wherein C1 and C2 individually are chosen from a cysteine and a cysteine-like nonnatural amino acid, as well as metal-XC1C2 complexes and methods for forming such complexes.

Abstract: The instant invention relates to peptides obtained from the enzymatic hydrolysis of yellow pea seed proteins that are capable of lowering the blood pressure and reducing the effects of kidney disease in a subject b\ inhibiting or reducing the affinity of the enzymes in the renin-angiotensin system for their substrates, specifically renin, to compositions comprising said peptides and to uses thereof.

Abstract: This present invention discloses a method for preparing a lipolysis-stimulating soy protein hydrolysate, proceeding a hydrolysis reaction, which is a predetermined concentration of soy protein mediated by Flavourzyme in a predetermined hydrolysis conditions, wherein Flavourzyme versus the soy protein is 1:100, and the optimal hydrolysis conditions including reaction pH value 7˜7.5, reaction temperature 40˜50° C. and hydrolysis time 100˜150 minutes. This invention further discloses nine recombinations of isolated peptide sequences from the soy protein hydrolysate including Val-His-Val-Val, Leu-Leu-Leu, Leu-Leu-Ile, Leu-Ile-Leu, Leu-Ile-Ile, Ile-Leu-Leu, Ile-Leu-Ile, Ile-Ile-Leu and Ile-Ile-Ile.

Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Abstract: Disclosed are peptides which inhibit the enzymatic activity of tyrosinase as well as formulations and methods for their use in the reduction of skin pigmentation, and methods of administering the inhibitory peptides in a topical formulation. Methods of skin treatment are also provided, the methods further including use of a peptide characterized by the amino acid sequence SFLLRN (SEQ ID NO: 1).

Abstract: The present invention provides novel peptides that facilitate the opening of mammalian tight junctions. i.e. tight junction agonists. The present invention also provides methods for the treatment of disease by administering to a subject suffering from the disease a composition comprising a peptide tight junction agonist of the invention in combination with a therapeutically effective amount of an active agent.

Abstract: The present invention pertains generally to the field of therapeutic compounds and more specifically to certain pyruvamide compounds of the formula (X) (for convenience, collectively referred to herein as “PVA compounds”), which, inter alia, inhibit a dust mite Group 1 peptidase allergen (e.g., Der p 1, Der f 1, Eur m 1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit a dust mite Group 1 peptidase allergen, and in the treatment of diseases and disorders that are mediated by a dust mite Group 1 peptidase allergen; that are ameliorated by the inhibition of a dust mite Group 1 peptidase allergen; asthma; rhinitis; allergic conjunctivitis; atopic dermatitis; an allergic condition which is triggered by dust mites; an allergic condition which is triggered by a dust mite Group 1 peptidase allergen; and canine atopy.

Abstract: Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical compositions containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.

Abstract: The storage stability of a serine hydrolase acting on ester bonds in a formulation without a protease can be improved by incorporating a serine protease inhibitor.

Abstract: A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.

Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.

Abstract: The invention relates to compounds, in particular MMP inhibitors. The compounds of the invention have formula (1). The invention can be used in particular in the pharmaceutical field. The present invention also relates to labeled compounds of formula (2), and to the use thereof as contrast agents for detecting extracellular matrix metalloproteinases.

Abstract: The invention relates to growth hormone compounds with a protracted profile. The effect is obtained by linking an albumin binding residue via a hydrophilic spacer to growth hormone variants. Further described are methods of preparing and using such compounds. These growth hormone compounds are based on there altered profile considered particular useful in therapy.

Abstract: The invention provides novel peptide prodrugs that contain cleavage sites specifically cleaved by human kallikrein 2 (hK2). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. Upon cleavage of the prodrug by hK2, the therapeutic drugs are activated and exert their toxicity. Methods for treating cell proliferative disorders are also featured in the invention.

Abstract: The present invention provides vaccine compositions comprising OmpA, or antigenic fragments thereof, and related methods of active immunization against A. baumannii infection. The invention also provides antibodies and antigen-binding parts thereof that specifically bind to OmpA, and related methods of passive immunization against A. baumannii infection. The compositions and methods of the invention are useful for preventing or treating A. baumannii infections, including those caused by strains resistant to carbapenems and all other antibiotics except colistin or tigecycline, also referred to as extreme drug resistant (XDR) A. baumannii infections, and those resistant to every FDA approved antibiotic, also referred to as pan-drug resistant (PDR) A. baumannii infections.

Abstract: An immunoconjugate in which a phosphate-prodrugged DNA minor groove binding agent of formula (I), where X is a nucleophilically displaceable leaving group, is conjugated to an antibody or an antigen binding fragment of an antibody, and compounds that can be used for making such immunoconjugates, and uses of such immunoconjugates.

Abstract: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.

Abstract: The embodiments provide prodrug compounds of Formulae I-XV. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XV that provides controlled release of an opioid. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of an opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, of formula I: X—W wherein X is a caspase-selective structure and W has the structure of —NH—CH(Y)(Z) wherein Y is a structure that can form a reversible covalent bond with a caspase; and Z is selected from a carboxyl moiety or a carboxylic acid mimetic.

Abstract: A protein synthesis promoter that exhibits a protein synthesis-promoting effect includes a whey protein hydrolyzate having a molecular weight distribution that is within a range of 10 kDa or less and has a main peak of 200 Da to 3 kDa, an average peptide length (APL) of 2 to 8, a free amino acid content of 20% or less, a branched-chain amino acid content of 20% or more, and an antigenicity equal to or less than 1/100,000th of that of ?-lactoglobulin.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: A peptide of formula: R1-X1-X2-X3-X4-X5-R2, wherein X1 is T; S2 is L; X3 is K; X4 is T, S, K, R or no amino acid; X5 is V, A, Y, M or no amino acid; R1 represents a primary amine function of the N-terminal amino acid; and R2 represents a hydroxyl function of the C-terminal amino acid, is capable of activating cytochrome C. The peptide can be included in cosmetic and pharmaceutical compositions intended to stimulate the functions of the mitochondria and increase intracellular ATP levels. Such compositions are useful to help protect the skin from external aggression, reduce and treat skin damage caused by UV radiation and combat cutaneous signs of aging.

Abstract: The present invention relates to compounds of Formula I, II, III or IV, 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 a compound of the present invention.

Abstract: Compounds based around tetrapeptide, tripeptide and dipeptide moeties and corresponding peptiod moeties. Related methods and pharmaceutical compositions for use in treatment of cancer, inflammatory diseases, and other disorders.

Abstract: The present invention provides a carrier capable of highly efficiently introducing a compound into cells with low cytotoxicity, which contains peptide lipids represented by the following formula, and a method for introducing a compound into cells using the carrier: wherein R1 is an amino acid or peptide having 1-10 amino acid residues, R2 is a side chain of any amino acid, provided that R2 has a carboxyl group, the carboxyl group may be an ester with a hydrocarbon group having 1-30 carbon atoms, R3 is a hydrocarbon group having 1-30 carbon atoms.

Abstract: Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.

Abstract: This invention relates to novel crystalline forms of the following Compound (1), and the sodium salt thereof, and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:

Abstract: Disclosed are methods for identifying high affinity adaptor molecules that bind to both a circulating antibody and a target molecule and redirect the specificity of the circulating antibody to the target molecule. Exemplary high affinity adaptor molecules are also provided.

Abstract: A process for producing a peptide product having cholecystokinin secretion promoting effect, said process comprising hydrolyzing soybean residues with one or more proteases so that the peptide product having cholecystokinin secretion promoting effect is obtained. Also disclosed is the composition containing the peptide product and the use thereof.

Abstract: A series of peptides with divergent confirmations including structures of formula (1A), (1B), (2) and (3) are provided. In the formula, wherein U, G, A, B, R1, R2 and T are as defined in the specification. The divergent peptides disclosed in the present invention are characterized in a mineral binding affinity function.

Abstract: The present invention relates to the field of protein misfolding diseases and thus to diseases which are associated with or induced by abnormal or pathogenic three-dimensional folding of proteins and/or peptides or which are linked to pathogenic conformational changes of proteins and/or peptides, such as Alzheimer's disease. Particularly, the present invention provides novel trimeric pyrazole compounds, which exhibit a therapeutic effectiveness in regard to the aforementioned protein misfolding diseases, and refers to their use for the treatment of such protein misfolding diseases, especially neurodegenerative diseases as well as to medicaments or pharmaceutical compositions comprising these compounds.

Abstract: Embodiments of the invention include methods for selecting in parallel (i.e., synchronously or simultaneously) peptides that target a number of organs, in which each peptide targets distinct tissues or organs. Typically, the methods of the invention provide for peptide selection in a Minimal number of subjects and still provides a selectively binding peptide. In certain aspects, methods of identifying peptides that bind to multiple selected tissues or organs of an organism may comprise the steps of administering a phage display library to a first subject; obtaining a sample of two or more selected tissues; obtaining phage displaying peptides that bind to the samples from the first subject; enriching for peptides by administering phage isolated from the samples of the first subject to a second subject; obtaining a sample of two or more selected tissues from the second subject; and identifying the peptides displayed.

Abstract: Proteasome inhibitors (PI) are used for inhibiting the maturation of dendritic cells (DZ) and thus in the treatment or the prophylaxis of allergies, asthma, tissue or transplant rejection or autoimmune diseases. The concentration of the proteasome inhibitors lies preferably in the range of 10 nM to 10 ?M, based on the peripheral blood or the cytoplasm.

Abstract: Preventing skin aging by targeting multiple causes by a single bullet is of primal scientific and consumer interest.

Abstract: The present invention relates to novel tubulin binding molecules of formula (I) and their use for the treatment of cancer and other diseases.

Abstract: There is provided inter alia a compound of formula (I): for use in treatment of viral infection or as an immunosuppressant.

Abstract: Compositions comprising a tripeptide having the sequence XC1C2; wherein X is any amino acid such that XC1C2 is capable of binding a metal in a square planar orientation or square pyramidal orientation or both; and wherein C1 and C2 are the same or different; and wherein C1 and C2 individually are chosen from a cysteine and a cysteine-like nonnatural amino acid, as well as metal-XC1C2 complexes and methods for forming such complexes.

Abstract: The invention is directed to methods of treatment of Alzheimer's disease and other tauopathies, via the administration of antibodies having specificity to abnormal forms of tau protein, the antibodies showing no binding and/or reactivity to a normal tau protein and being administered under conditions and in amounts effective to prevent or treat Alzheimer's disease or other tauopathies. In certain embodiments, the antibodies are selective for soluble truncated tau protein truncated at (i) its C-terminus after the glutamic acid residue Glu391, or (ii) at the aspartic acid residue Asp421, or (iii) at its N-terminus at the aspartic acid residue Asp13, or (iv) a combination of (i)-(iii). Further aspects of the invention are directed to the administration of an immunogen comprising an abnormal tau, preferably a soluble truncated tau.

Abstract: This invention relates to novel compounds that are peptides derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel peptides that are deuterated derivatives of boceprevir. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating HCV infection.

Abstract: The present invention relates to a polypeptide derived from a highly conserved region (HCR) I-III of an extracellular region of a CD99 and CD99 family such as CD99L2 and PBDX (or XG), which are a kind of transmembrane protein, or a fused protein thereof. The polypeptide or the fused protein thereof has an activating function of inhibiting the extravasation of white blood cells, or inhibiting the growth and/or metastasis of cancer cells. The present invention also provides a polynucleotide coding the polypeptide, a vector including same, and a transformant transformed by the vector. In addition, the present invention provides a pharmaceutical composition including the polypeptide or the fused protein thereof for preventing or treating inflammatory diseases. Further, the present invention provides a pharmaceutical composition including the polypeptide or the fused protein thereof inhibiting the growth and/or metastasis of cancer cells, i.e., a pharmaceutical composition for preventing or treating cancer.

Abstract: The invention relates to methods of treatment or prophylaxis of physiological and/or pathological conditions with at least one LHRH antagonist, in particular at least one peptidomimetic LHRH antagonist such that the at least one LHRH antagonist is administered in a dose, which does not cause chemical (hormonal) castration.

Abstract: Neurotrophin binding to its specific receptors Trk A and p75 leads to the activation of multiple signalling cascades, culminating in neuroprotective and regenerative effects, including neuronal survival and neurite outgrowth. Neurotrophic factors have been used for the treatment of several neurodegenerative diseases. However, their use is limited by their inability to cross the blood-brain barrier, their short half life and their side effects. Small molecule neurotrophin mimetics may be beneficial in treating a number of neurodegenerative disorders. The present invention shows the capacity of nerve growth factor agonist molecules of Formulae I-IV, as defined in the specification, to induce differentiation in PC 12 cells, promote survival in RN22 cells and activate Trk A, IkBa and SAPK/JNK phosphorylation to various extents in both cell lines.

Abstract: The present invention relates to human laminin ?2 chain LG3 domain and active peptides promoting cell adhesion, spreading, migration, and neurite outgrowth. More particularly, it was found that when nerve cells are incubated using human laminin ?2 chain LG3 domain and active peptides in the LG3 domain, cell adhesion, spreading, migration, and neurite outgrowth of nerve cells promote and the promotion of cell adhesion, spreading, migration, and neurite outgrowth of nerve cells are integrin-mediated and achieved by the activation of PKC? and FAK phosphorylation. Thus, the present invention can be very useful for researches on cell adhesion, spreading, migration, and neurite outgrowth activities of cells which are focused on nerve cells and mediated by various extracellular matrix proteins including laminin, manufacture of artificial nerve conduits, burns treatment, wounds treatment, and tissue regeneration.