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: Methods and assays are disclosed for treating subjects with 22q13 deletion syndrome or SHANK3 deletion or duplication, mutation or reduced expression, where the methods comprise administering to the subject insulin-like growth factor 1 (IGF-1), IGF-1-derived peptide or analog, growth hormone, an AMPAkine, a compound that directly or indirectly enhances glutamate neurotransmission, including by inhibiting inhibitory (most typically GABA) transmission, or an agent that activates the growth hormone receptor or the insulin-like growth factor 1 (IGF-1) receptor, or a downstream signaling pathway thereof.

Abstract: The invention provides a cationic lipid comprising: (i) one head group, comprising one or more amino acids, in which at least one amino acid has a side chain that comprises a cationic moiety or a cationic precursor; (ii) a linking moiety of formula (5): —(HNR5)2NC(O)R3C(O)—??(5), wherein: each R5 is independently an optionally substituted C1-4 alkylene moiety; and R3 is an optionally substituted alkylene or alkenylene moiety; and (iii) two lipophilic moieties, wherein the head group and each of the lipophilic moieties are connected to the linking moiety through amide linkages.

Abstract: A method for treating a subject afflicted with an autoimmune disease with a pharmaceutical composition comprising glatiramer acetate and a pharmaceutically acceptable carrier, comprising the steps of administering a therapeutic amount of the pharmaceutical composition to the subject, determining whether the subject is a glatiramer acetate responder or a glatiramer acetate hypo-/non-responder by measuring the value of a biomarker selected from the group consisting of IL-10 concentration, IL-17 concentration, IL-18 concentration, TNF-? concentration, BDNF concentration, caspase-1 concentration, IL-10/IL-18 ratio and IL-10/IL-17 ratio in the blood of the subject, and comparing the measured value to a reference value for the biomarker to identify the subject as a glatiramer acetate responder or a glatiramer acetate hypo-/non-responder, and continuing the administration if the subject is identified as a glatiramer acetate responder, or modifying treatment of the subject if the subject is identified as a glatiramer

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: The present invention provides methods, pharmaceutical compositions, medicaments, and pharmaceutical kits that employ the use of boceprevir as a CYP3A4/5 inhibitor to improve the pharmacokinetics of therapeutic compounds metabolized by cytochrome P450 3A4/5 (CYP3A4/5) enzymes.

Abstract: The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to, the prevention and treatment of Alzheimer's disease.

Abstract: The invention provides compounds of formula (I): (I) or salts thereof, wherein R1, R2, R3 Z, and X have any of the values defined herein, as well as compositions comprising such compounds. The compounds and compositions are useful for treating neurodegenerative disorders.

Abstract: The subject invention provides advantageous new salts of mu-opiate receptor peptides. These salts have been found to have excellent properties in terms of their crystal structure, stability, solubility, lack of impurities and/or the ability to be produced, with these advantageous properties, in amounts sufficient for the production of therapeutic compositions.

Abstract: Compositions comprising dendritic cells pulsed with tumor lysate and at least one toll-like receptor (TLR) ligand which may be used for eliciting a specific immune response in a mammal in need thereof for treating diseases including a tumor are disclosed. Also disclose are methods of activating dendritic cells, comprising providing at least one toll-like receptor (TLR) ligand; and pulsing a dendentic cell with the at least one TLR ligand. A method further comprises pulsing the dendritic cell with a tumor lysate.

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

Abstract: A peptidic hydrolyzate enriched in bioactive peptides is disclosed that is a proteasome activator. Cosmetic and pharmaceutical compositions are disclosed that include the peptidic hydrolyzate enriched in bioactive peptides in a physiologically acceptable medium. Also disclosed are methods for depigmenting, lightening and/or whitening the skin and treating hyperpigmentation blemishes as well as cutaneous signs due to photo-aging by administering the cosmetic compositions or pharmaceutical compositions.

Abstract: The present invention relates to the treatment of vascular disease in a diabetic patient using a drug-eluting implantable medical device that releases everolimus from three distinctly loaded drug reservoir layers wherein at least one of the layers comprises at least 200 ?g/cm2 of everolimus and further wherein the everolimus is the only therapeutic agent in the layers or the layers or any combination thereof further comprise an anti-inflammatory agent or an RGD peptide or both.

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: A hydrogel that includes an aqueous solution or an alcohol aqueous solution, and a hydrogelator containing a lipid peptide represented by Formula (1), or a pharmaceutically usable salt thereof. In Formula (1), R1 represents an aliphatic group having 9 to 21 carbon atoms; R2, R3, and R4 independently represent a hydrogen atom, an alkyl group having 1 to 4 carbon atoms that optionally has a branched chain having 1 or 2 carbon atoms, a phenylmethyl group, or a —(CH2)n—X group, and at least one of R2, R3, and R4 represents a —(CH2)n—X group; n represents an integer from 1 to 4; and X represents an amino group, a guanidino group, a —CONH2 group, or a 5-membered ring, a 6-membered ring or a fused heterocyclic ring composed of a 5-membered ring and a 6-membered ring that optionally has 1 to 3 nitrogen atoms.

Abstract: Peptides of general formula (I): R1-Wp-Xn-AA1-AA2-AA3-AA4-Ym-R2 their stereoisomers, mixtures thereof, and/or their cosmetically or pharmaceutically acceptable salts, a method of preparation, cosmetic or pharmaceutical compositions containing them and their use for the treatment, prevention and/or care of conditions, disorders and/or diseases of the skin, mucous membranes and/or scalp.

Abstract: Mixtures are described comprising two or more compounds selected from at least two of the following groups: i) salicylic acid and/or its functional analogous products (ESA), ii) promoting compounds (PRO) and iii) modulating compounds (MOD), and their use for stimulating the natural defense systems of plants and for inducing resistance in plants. The use is also described, of two or more compounds selected from at least two of the following groups: one or more compounds belonging to the ESA group and/or one or more compounds belonging to the PRO group and/or one or more compounds belonging to the MOD group, individually adopted by means of application programs which envisage alternating application, to stimulate the natural defense systems of plants and inducing resistance in plants.

Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.

Abstract: The present invention concerns a peptide of following formula I: R being a side chain having at least one heteroatom selected from sulfur, nitrogen and oxygen in a carbonyl form (C?O); R1 being either H or a lipophilic chain; R2 being either OH or a lipophilic chain. More particularly the present invention concerns a cosmetic composition comprising a peptide as recited above and a physiologically acceptable medium. Results on the activity of the compounds are obtained and on the general state of the skin and its appendages, in particular via the stimulation of extracellular matrix components.

Abstract: This invention relates to the cosmetic use of at least one compound of formula (I) wherein A1 is the radical corresponding to D- or L-Ser A2 is the radical corresponding to D- or L-Asp or Glu, A3 is the radical corresponding to D- or L-Lys, Arg or Orn, A4 is the radical corresponding to D- or L-pro, R1, R2 and R3 are as defined in the claims as anti-aging and restructuring agents.

Abstract: The invention provides compositions and methods for preventing or treating an ischemia-reperfusion injury, such as occurs during acute myocardial infarction and organ transplant in a mammalian subject. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide or a pharmaceutically acceptable salt thereof, and one or more additional active agents such as cyclosporine.

Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.

Abstract: This disclosure features compounds that are useful as pro-drugs of epoxy ketone protease inhibitors.

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 present invention provides an amphiphilic linear peptide and/or peptoid as well as a hydrogel that includes the amphiphilic linear peptide/peptoid.

Abstract: The invention provides methods of treating stroke and related conditions exacerbated by fever and/or hyperglycemia by administering peptides or peptidomimetics that inhibit binding of NMDAR 2B to PSD-95 to a patient.

Abstract: Small molecule, peptidic hepatocyte growth factors mimics, which act as both mimetics and antagonists, have been generated. These molecules have been shown or predicted to have therapeutic potential for numerous pathologies including dementia, neurodegenerative disease, diabetes and metabolic syndrome, cancer, and defective wound healing.

Abstract: The present invention provides materials and methods useful to treat various sGC?1-expressing cancers. Materials include peptides which interfere with sGC?1's pro-survival functions, thereby resulting in apoptosis of sGC?1-expressing cells. In addition, the present invention provides screening assays, diagnostic assays, methods to prognose, methods to treat, and kits.

Abstract: The invention relates to acetates of the tetrapeptides AQGV (SEQ ID NO:2) and LQGV (SEQ ID NO:3), pharmaceutical compositions comprising the acetates of the tetrapeptides, and methods of treating using the acetates of the tetrapeptides or pharmaceutical compositions to treat acute inflammatory conditions including sepsis.

Abstract: The present application relates to new derivatives, substituted on the N terminus by a carboxyalkyl group, of monomethylauristatin E and monomethylauristatin F, to processes for preparing these derivatives, to the use of these derivatives for treating and/or preventing diseases, and to the use of these derivatives for producing medicaments for treating and/or preventing diseases, more particularly hyperproliferative and/or angiogenic disorders such as cancer disorders, for example. Such treatments may be applied as a monotherapy or else in combination with other medicaments or further therapeutic measures.

Abstract: A delivery system is provided. The delivery system includes a carrier or an active compound and a glutathione or a glutathione derivative grafted thereon. The invention also provides a compound including a moiety comprising a vitamin E derivative or a phospholipid derivative, a polyethylene glycol (PEG) or a polyethylene glycol derivative bonded thereto, and a glutathione (GSH) or a glutathione derivative bonded to the polyethylene glycol or the polyethylene glycol derivative.

Abstract: The present invention provides an agent having a suppressive action against the thickening of the heart wall, a prophylactic agent for heart failure containing the above described agent, and functional foods expected to have a prophylactic effect for heart failure. The agent for suppressing heart wall thickening comprises Xaa Pro Pro as an active ingredient.

Abstract: The present invention provides peptide-based peroxidase inhibitors having the formula AA1-AA2-AA3, wherein AA1 is a positively charged, negatively charged or neutral amino acid, AA2 is a redox active amino acid, and AA3 is an amino acid possessing a reducing potential such that AA3 is capable of undergoing a redox reaction with a radical of amino acid AA2 or a retro or retro-inverso analog thereof. The result of such a combination is a highly effective inhibitor of peroxidase activity that has potent anti-inflammatory properties in widely diverse models of vascular disease and injury. Exemplary tripeptides effectively inhibit peroxidase mediated LDL oxidation, increase vasodilation in SCD mice, inhibit eosinophil infiltration and collagen deposition in asthma mice, inhibit acute lung injury, and decrease ischemic injury of the heart.

Abstract: The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxo-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.

Abstract: Peptides useful as angiotensin converting enzyme inhibitors are provided. Also provided are compositions comprising one or more of the peptides and methods for preventing, treating and/or diminishing one or more syndromes associated with angiotensin converting enzyme by using the peptides.

Abstract: The present invention is directed to peptide compositions and methods of using the peptide compositions to treat prediabetes, diabetes, obesity, high blood pressure and metabolic syndrome.

Abstract: Nutritional compositions for maximizing muscle protein synthesis while minimizing the catabolism of muscle proteins and methods of using same are provided. In this manner, the nutritional compositions may provide for retention of lean body mass, which helps to avoid loss of independence and functionality, as well as to improve quality of life especially in the elderly at risk of sarcopenia and frailty. The nutritional compositions include ?-hydroxyisocaproic acid and ?-ketoglutarate. The composition may include other functional ingredients such as, but not limited to whey protein including whey protein micelles, prebiotic fibers, citrulline, eicosapentaenoic acid, L-carnitine, nucleotides, and amino acids. Methods of administering such nutritional products to individuals in need of same are also provided.

Abstract: Short biologically active tetrapeptides are disclosed that are comprised of the sequences GxxG and PxxP where G (glycine) and P (proline) are maintained and x is a variable amino acid. The peptides can be used singly or in combination to stimulate production of extracellular matrix proteins in skin. A rapid, low-cost method of producing heterogenous formulations of tetrapeptides is disclosed.

Abstract: The present invention relates to a control method of a wheel alignment apparatus using an MDPS, which determines whether or not to cancel center alignment control due to a trouble or error is preferentially determined prior to each control step and then performs control when wheels of a vehicle having an MDPS mounted therein are aligned, such that the trouble or error is preferentially considered in the control priority, thereby increasing driver's convenience and improving safety performance for protecting the driver.

Abstract: The invention provides tight junction protein modulators, compositions comprising the same, and uses thereof. In particular, the invention provides tight junction protein modulators that modulate the second extracellular loop of tight junction proteins, such as occludin or claudin.

Abstract: This invention relates to peptide compounds of general formula (I) R1-(AA)n-X1—X2—X3-Asp-Leu-Lys-Lys-X4—X5-(AA)p-R2. Said peptide compounds have an action on the SCF/c-Kit signaling pathway and thus make it possible to protect skin pigment structures from external stresses. In addition, this invention relates to a cosmetic or pharmaceutical composition comprising at least one peptide of general formula (I), in a physiologically acceptable medium, and its use for attenuating age-related pigmentation defects and the effects of photoaging on the skin. The invention finally relates to various cosmetic treatment methods using said peptides according to the invention.

Abstract: The invention refers to TFEB phosphorylation inhibitors. Such molecules have a therapeutic applicability in all disorders that need induction of the cell authophagic/lysosomal system, such as lysosomal storage disorders, neurodegenerative diseases, hepatic diseases, muscle diseases and metabolic diseases.

Abstract: The invention provides a peptide having an activity of inhibiting angiotensin-converting enzyme (ACE), and a food and drink and/or a pharmaceutical composition containing the peptide.

Abstract: This disclosure relates to polymer coated particles targeting cancer cells and methods related thereto. In certain embodiments, the disclosure relates to nanoparticles coated with amphiphilic polymers conjugated with molecules useful for targeting tumors, monitoring the location of the nanoparticles administered to a subject by MRI, and viewing the presence of the nanoparticles during optical image-guided surgery.

Abstract: The invention proposes a method of treatment of idiopathic pulmonary fibrosis by a liposomally formulated reduced glutathione.

Abstract: The invention provides a method for reducing oxidative damage in a mammal, a removed organ, or a cell in need thereof. The method comprises administering an effective amount of an aromatic cationic peptide. The aromatic cationic peptide has (a) at least one net positive charge; (b) a minimum of three amino acids; (c) a maximum of about twenty amino acids, (d) a relationship between the minimum number of net positive charges (pm) and the total number of amino acid residues (r) wherein 3 pm is the largest number that is less than or equal to r+1; (e) a relationship between the minimum number of aromatic groups (a) and the total number of net positive charges (pt) wherein 3a or 2a is the largest number that is less than or equal to pt+1, except that when a is 1, pt may also be 1; and (f) at least one tyrosine or tryptophan amino acid.

Abstract: Use of the tripeptide ITP and salts thereof for the preparation of a functional food angiotensin-converting enzyme inhibitor. Also provided is the use of the combination of tripeptide MAP and the tripeptide ITP and salts thereof as an angiotensin-converting enzyme inhibitor in functional foods.

Abstract: Method for identifying a modulator of Sirt6, PfSir2a, or Sirt7 deacylase activity, wherein a fatty-acylated substrate containing an acyl-lysine moiety and an indicator moiety is contacted with Sirt6, PfSir2a, or Sirt7 in the presence of a candidate compound under conditions for Sirt6, PfSir2a, or Sirt7 to deacylate the substrate, wherein the acyl is a hydrophobic fatty acyl group containing a hydrocarbon group having at least three carbon atoms connected by carbon-carbon bonds; contacting the deacylated substrate with a cleavage agent that cleaves the linkage between the lysine and indicator moiety to generate a detectable signal; and correlating a quantified Sirt6, PfSir2a, or Sirt7 deacylase activity therefrom. Modulating compounds of Sirt6, PfSir2a, or Sirt7 deacylase activity are also described, as are pharmaceutical compositions thereof, methods of treatment by administration of the modulating compounds, and kits for practicing the method.

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: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating lupus, a fibrotic condition, or inflammatory myopathies and other conditions (e.g., skin conditions).