Abstract: The present invention relates to new auristatin compounds and prodrugs thereof, compositions comprising them and uses thereof.

Abstract: Specific template-fixed ?-hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are ?-amino acid residues connected from the carbonyl (C?O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these ?-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilization of stem cells.

Abstract: Disclosed are methods and compositions for the inhibition of modulation of T cell costimulatory pathway by a pathogenic agent, particularly, the inhibition of activation of a T cell costimulatory pathway by a pyrogenic exotoxin. The direct interaction of a superantigen with a specific site within the dimer interface of a CD28 family member is inhibited using immunomodulatory peptides. Specific antagonist immunomodulatory peptides comprise amino acid sequences derived from a dimer interface of a T cell co-stimulatory pathway member, or peptides which comprise an amino acid sequence which specifically binds to an amino acid sequence within the dimer interface of a T cell co-stimulatory pathway member. Compositions comprising said peptides and methods for the treatment of immune-related disorders are also disclosed. Such molecules may be used in screening for a test substance which specifically binds to the CD28 molecule and is capable of antagonizing pyrogenic exotoxin-mediated activation of Th1 lymphocytes.

Abstract: The present invention relates to peptide ligands of the melanocortin receptors, in particular the melancortin-4 receptor, and as such, are useful in the treatment of disorders responsive to the activation of this receptor, such as obesity, diabetes mellitus and sexual dysfunction.

Abstract: Compositions that include isolated peptides that inhibit TLR-4 signaling pathways and inflammation are disclosed. Methods of producing and using the compositions to inhibit TLR-4 signaling and/or inflammation are also disclosed herein.

Abstract: This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.

Abstract: Methods for treating muscular wasting diseases such as Duchenne muscular dystrophy are disclosed. Specifically, the methods include administering to a subject in need of treatment for a muscular wasting disease, an NF-?B activation inhibitor capable of blocking the activation of NF-?B.

Abstract: Embodiments of the present disclosure provide for RGD mimetic ?-AApeptide compounds, ?-AApeptide compounds capable of binding an RGD binding site on integrin ?v?3, linear ?-AApeptide compounds, cyclic ?-AApeptide compounds and multimeric RGD mimetic ?-AApeptide compounds, methods of making each, and methods of using each, and the like. In embodiments, the RGD mimetic ?-AApeptide compounds can be used in imaging, diagnostics, and treatment of angiogenesis related conditions.

Abstract: Coating compositions having a peptidic antimicrobial additive and an antimicrobial additive of another configuration are provided. The concentrations of the antimicrobial agents within the coating composition are sufficient to synergistically inhibit microbial growth on an inanimate surface coated with the surface coating composition or within a container storing the coating composition. Methods for making and using such compositions to inhibit microbial growth in stored coatings and on susceptible surfaces are also provided.

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

Abstract: The disclosure provides a cell penetrating peptide. The cell penetrating peptide includes an amino acid sequence of Dn, in which D represents an aspartate residue and 2?n?15.

Abstract: Described is an N-terminal hexapeptide fragment of maximakinin, QUB 698.8, which exhibits potent tissue selective actions on smooth muscle. It demonstrates a high degree of selectivity for arterial smooth muscle over small intestinal smooth muscle, causing potent relaxation of arterial smooth muscle, while causing less potent contraction of ileal smooth muscle. It may be used treatment of diseases of the cardiovascular system and in promotion of angiogenesis.

Abstract: A personal care composition is disclosed comprising a di-amido gellant, wherein the di-amido gellant has a formula: wherein R1 and R2 are aminofunctional end-groups which may be the same or different, and L is a linking moiety of molecular weight from 14 to 500 g/mol. The personal care composition may take a variety of forms such as a leave-on composition or an emulsion and/or may comprise one or more actives or agents.

Abstract: The present invention relates to peptide compounds of the general formula (I) R1-(AA)n-X1-X2-Arg-Glu-Met-Asn-Trp-X3-(AA)P-R2 modulating the survivin protein. Furthermore, the present invention relates to a cosmetic or pharmaceutical composition, including at least one peptide of the general formula (I), in a physiologically acceptable medium as well as to the use thereof for preventing and/or treating the cutaneous signs of ageing and photo-ageing and for protecting the skin against external aggressions. In addition, the composition according to the invention can be used to prevent and/or limit hair loss and/or stimulate hair growth. Finally, the invention relates to a cosmetic treatment method for preventing and/or controlling the cutaneous signs of ageing or photo-ageing.

Abstract: Peptides are provided that comprise less than 24 amino acids. The peptides have an amino acid sequence selected from the group consisting of: (a) an amino acid sequence having from 4 to 6 contiguous amino acids of a reference sequence PEPTIDE 1; (b) an amino acid sequence substantially identical to the sequence defined in (a); and (c) a variant of the amino acid sequence defined in (a). Also provided is a non-myristoylated MANS peptide. Various methods of using the peptides are also provided.

Abstract: Hydrogel compositions comprise an aqueous dispersion phase and a plurality of peptides, or derivatives, or analogues thereof. Each peptide comprises at least two amino acid residues and an aromatic stacking ligand and the hydrogel is formed by self-assembly of said peptides in said aqueous dispersion medium. The aqueous dispersion phase is physiologically acceptable and may have a pH of 6 to 8, as may the hydrogel itself. The hydrogel may be used for cell culture or for treatment of medical conditions characterised by tissue loss/damage.

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

Abstract: Disclosed are peptides for inhibiting mdm2 (mouse double minute 2) and a pharmaceutical composition comprising the same.

Abstract: The present invention relates to peptides derived from human HMG-CoA reductase of general formula (I): R1-(AA)n-X1-Gly-Lys-X2-(AA)p-R2, And of sequence SEQ ID No. 1 to SEQ ID No. 10. The present invention also relates to a cosmetic or pharmaceutical composition comprising at least one peptide of general formula (I), in a physiologically suitable medium. The present invention further relates to the use of this novel peptide as an active principle that activates human HMG-CoA reductase in a cosmetic composition intended to strengthen the barrier function of the skin and to stimulate epidermal differentiation. The invention further applies to a cosmetic treatment method intended to prevent and/or combat the external stresses and signs of cutaneous aging.

Abstract: The disclosure provides aromatic-cationic peptide compositions and methods of preventing or treating disease using the same. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof.

Abstract: The present invention relates to compounds of the formula (I) and in particular medicaments comprising at least one compound of the formula (I) for use in the treatment and/or prophylaxis of physiological and/or pathophysiological states in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.

Abstract: Auristatin compounds and conjugates thereof are provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently an Auristatin compound. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.

Abstract: Peptide ligands for transporting therapeutic agents across the intestinal epithelial barrier that ordinarily are inadequately absorbed and must be delivered by alternative means, which contain an isolated amino acid sequence wherein at least one pair of amino acids are of an opposite charge and the pair members are separated by a spacer of 1-12 amino acid residues including at least one hydrophobic amino acid, and wherein the length of the amino acid sequence is greater than 5 and less than 20 amino acids. Pharmaceutical compositions for gastro-intestinal delivery and methods for the gastrointestinal delivery of poorly absorbed therapeutic agents are also disclosed.

Abstract: Embodiments of the present invention are directed to a coated cell comprising a therapeutic cell and a plurality of targeting complexes coating the therapeutic cell and each of said targeting complexes comprising a homing molecule, a lipid moiety, and a spacer having from about 1 to about 10 amino acids and covalently linking the homing molecule to the lipid moiety and wherein the lipid moiety is non-covalently attached to the therapeutic cell. In some embodiments, the therapeutic cell is a stem cell. Embodiments of the invention are directed to methods of coating a therapeutic cell. Embodiments of the invention are directed to methods of treating diseases of the vasculature.

Abstract: Embodiments described herein are directed to methods for the treatment and control of hyperlipidemia, hypercholesterolemia, dyslipidemia, and other lipid disorders, and in delaying the onset of or reducing the risk of conditions and sequelae that are associated with these diseases, including atherosclerosis and non-insulin dependent diabetes. In addition, embodiments are directed to methods of treating coronary heart disease and metabolic syndrome. Embodiments are also directed to neurotensin analogs. In embodiments, the neurotensin analogs may be capable of binding to neurotensin receptors and, upon binding, may modulate the levels of lipids in subjects.

Abstract: The present invention provides compositions for the therapeutic and/or cosmetic treatment of Elastin comprising tissues. Therapeutic and cosmetic compositions comprising an elastin digest stimulate the endogenous production of Elastin and appear to enhance the elasticity of the skin and provide an external supply of peptide precursors of Elastin that penetrate into the tissue to which it is applied. The present invention describes compositions containing an elastin digest derived from proteolytic digestion of insoluble elastin derived from mammalian ligaments with a protein digesting composition, such as proteinase K. The elastin digest is a mixture of elastin peptides wherein the elastin peptide mixture comprises peptides of the sequence GXXPG, wherein X represents one of the natural amino acids. The elastin digest of the present invention may also comprise epitopes of cytokines, growth factors and di-peptides.

Abstract: Provided herein are peptide modulators of ion channels. Specifically, the peptide modulators comprise the amino acid sequence VEDEC wherein V is valine, E is glutamate, D is aspartate, C is cysteine. In certain embodiments, the modulator is attached to the C-terminal end of Slo1 protein isoform. The present invention also claims conjugations of the first valine that make the peptide modulator more membrane permeable, such as myristoyl moieties and arginine-rich cell penetrating peptides. The present invention contemplates use of the peptide modulators in the treatment of diseases/malfunctions such as epilepsy, chronic pain, migraine, asthma, chronic obstructive pulmonary disease, urinary incontinence, hypertension, erectile dysfunction, irritable bowel syndrome, renal disorders of electrolyte imbalance, and possibly in certain kinds of cancer.

Abstract: The current invention relates to the use of a peptide comprising an amino acid sequence in the preparation of a medicament for the regeneration of tissue, preferably for the treatment of a wound. Further the invention relates to compositions comprising such peptides, and use of said peptides in both medical and nonmedical (cosmetic) applications.

Abstract: Methods and compositions for improving the delivery and/or efficacy of a therapy (e.g., a cancer therapy) are disclosed. In one embodiment, methods and compositions for treating or preventing a cancer (e.g., a solid tumor such as a desmoplastic tumor) by administering to a subject an anti-hypertensive agent, as a single agent or in combination with a microenvironment modulator and/or a therapy, e.g., a cancer therapy (for example, a therapeutic agent or therapy, including immunotherapy (e.g., antibodies, vaccine, cell-based), nanotherapeutics, radiation therapy, photodynamic therapy, low molecular weight chemotherapeutics, molecularly targeted therapeutics and/or oxygen radical) are disclosed.

Abstract: The invention provides a peptide triazole conjugate and derivatives thereof, and methods of its use. The invention also provides an antibody to the peptide triazole conjugate. The invention further provides a method of identifying an HIV-1 entry inhibitor candidate.

Abstract: Provided herein are compositions and methods for use in promoting wound healing and tissue regeneration following tissue injury in a subject.

Abstract: Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.

Abstract: The present application relates to new derivatives of monomethylauristatin F, substituted on the N terminus by a carboxyalkyl group, processes for preparing these derivatives, their use for the treatment and/or prevention of diseases and to produce medication for the treatment and/or prevention of diseases, particularly hyperproliferative and/or angiogenic disorders such as cancer disorders, for example. Such treatments can occur as monotherapies or in combination with other medication or further therapeutic measures.

Abstract: A soothing cosmetic or pharmaceutical composition that includes at least one peptide that activates human HMG-CoA reductase general formula (I): R1-(AA)n-X1-Gly-Glu-Leu-Ser-X2-X3-(AAp-R2 in a physiologically suitable medium is disclosed. The invention further applies to a cosmetic treatment method intended to combat skin irritations. Additionally, methods of treating skin irritations with such a composition are described.

Abstract: Soothing cosmetic or pharmaceutical composition that includes at least one peptide as an active principle that activates human HMG-CoA reductase of general formula (I): R1-(AA)n-X1-Gly-Lys-X2-(AA)p-R2 and is chosen from among sequences SEQ ID NO: 1 to SEQ ID NO: 10, in a physiologically suitable medium is described. This novel peptide is designed to act as a soothing active principle capable of providing a solution to skin sensitivity in a cosmetic composition. The invention further applies to a cosmetic treatment method intended to combat skin irritations.

Abstract: The invention relates to composition comprising a pharmaceutically effective amount of one or more functional vasoactive intestinal peptide (VIP) fragments, and the use of those compositions in the treatment of fibrosis, hypertension and other disorder.

Abstract: The present invention provides novel compounds that have been demonstrated to be modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, iso forms and variants thereof). These compounds are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, diabetes, central nervous system disorders, genetic disorders, and hyperproliferative disorders.

Abstract: The present invention relates to the use of leukotriene B4 to enhance the response of Toll-like receptor (TLR), RIG-I-like receptor (RLR), and NOD-like receptor (NLR) when stimulated simultaneously with respective proper ligands. The use in combination of LTB4 with those ligands is useful to potentiate immune response for the treatment of autoimmune diseases, immunosuppressive diseases, as well as immunological disorders.

Abstract: The invention relates to pharmaceutical compositions and food products containing peptides derived from the ?s1-casein in milk and having benzodiazepine-type activity and particularly, anxiolytic activity.

Abstract: The invention relates to compositions comprising of SEQ NO: 1-244, 248-249, and any homologs, analogs, and fragments thereof. Such compositions can be used to treat, prevent, and modulate pain, inflammation, and metabolic processes in various organisms including plants and animals. Such compositions can be formulated with an acceptable pharmaceutical excipient for administration to a human or a plant. The compositions can be administered topically or for systemic use.

Abstract: The use of lipopeptides as inducers of NF-?B for the protection of mammals from the effects of apoptosis is described.

Abstract: The present invention relates to a peptide capable of binding to an immunoglobulin, and to a fusion protein containing such a peptide. The present invention also relates to a pharmaceutical composition for the treatment or prevention of a disease caused by binding between C1q and an immunoglobulin, which comprises a peptide capable of binding to the immunoglobulin or a fusion protein with such a peptide, and to the like. The pharmaceutical composition provided by the present invention is effective particularly in treating arthritis and rheumatism.

Abstract: The present invention provides for novel peptides derived from human milk. In aspects of the invention, the peptides are capable, individually or in combination, of evoking an antioxidative stress response, immunomodulation, anti-inflammatory response and anti-pathogenic response. As such the peptides of the invention may be used in food supplements, milk substitutions, infant formula., mother's milk, parenteral nutrition solutions, cell/tissue/organ storage and perfusion solutions and pharmaceutical formulations.

Abstract: This invention relates in one aspect to non-natural desamino alkyl amino acid compounds, methods of making these compounds, and peptides containing these compounds. In one embodiment, the peptide is neurotensin (8-13) in which the N-terminus is an alpha-desamino, alpha-methyl-N,N-dimethyl-homolysine residue of the invention.

Abstract: The invention provides novel peptides and constructs. In addition the invention provides methods for carrying compounds across the cell membrane, for antagonizing or destroying X-protein of HBV, treatment and/or management of HBV infection, treatment and/or prevention of HCC, and degradation of a target protein.

Abstract: The present invention provides methods and materials for use in increasing HSP20 activation in a biological system, for example by increasing phosphorylation of Ser16 of HSP20. In one aspect, the invention provides a method for increasing HSP20 activation in a biological system, comprising contacting the system with an antagonist capable of inhibiting PDE4 binding to HSP20, the antagonist comprising or consisting essentially of a fragment of PDE4 or an analogue thereof. In a further aspect the invention provides a method of screening for an agent able to increase activation of HSP20. A preferred antagonist has a C-terminal lysine residue.

Abstract: The present invention relates to improvements in compositions containing peptides that are ligands of the GHS receptor, or pharmaceutically acceptable salts thereof, methods for preparing such compositions, and methods of using such compositions to treat mammals. In particular, the present invention relates to a pharmaceutical composition comprising a pamoate salt of H-Inp-D-Bal-D-Trp-Phe-Apc-NH2, which is a ligand of the GHS receptor and in which, after subcutaneous or intramuscular administration to a subject, the peptide forms an in situ depot at physiological pH that is slowly dissolved and released into the body fluid and bloodstream. The present invention may further comprise an organic component such as dimethylacetamide (DMA) or polyethylene glycol with an average molecular weight of lower than 1000.

Abstract: A method for managing withdrawal from an addictive substance is described. The method involves administering one or more peptides having specific activity for the ? and/or ? isozyme of protein kinase C (PKC). The peptide(s) can be administered prior to, concurrent with, or subsequent to administration of the addictive substance. Also described is a kit having at least one container containing a peptide having isozyme-specific activity for ?PKC or ?PKC and instructions for use.

Abstract: Topical cosmetic use as a whitening active ingredient of at least one peptide, comprising at least one blocked aromatic cycle and having the general formula (I): A-(Xa)m-Xc-(Xb)n-B. The invention also discloses a cosmetic composition comprising at least said peptide and a method of decreasing skin pigmentation, whitening or lightening human skin, comprising a topical application of said composition.