Abstract: Peptide compounds of the following general formula (I): R1-(AA)n-X1-X2-X3-Lys-Lys-Gln-Lys-Trp-X4-(AA)p-R2 are disclosed herein. The peptide compounds can be used as Telomeric repeat-binding factor 2 (TRF2) protein-modulating compounds and have a preventive action on deoxyribonucleic acid (DNA) double-strand breaks. In addition, cosmetic compositions that include at least one peptide of general formula (I) in a physiologically acceptable medium are disclosed along with methods for preventing and/or treating cutaneous signs of aging and photoaging.

Abstract: A new and strong transcriptional activation domain was identified from the Arabidopsis protein Ethylene Response Factor 98 (AtERF98). This domain has been designated as the “EDLL domain” and has a number of highly conserved amino acid residues that are found throughout the members of the AtERF98 family from plants, including in monocot and eudicot orthologs. The EDLL domain was shown to be highly active when it was fused to transcription factors from plant and yeast, and was also shown to have activation potential comparable to the widely-used VP16 activation domain derived from Herpes simplex. The EDLL domain was also active when it was targeted to a gene promoter by a sequence-specific DNA binding protein or by protein-protein interactions. Unlike other known activation domains such as VP16 and GAL4, the EDLL domain is relatively small in size, and being of plant origin, it is favored as a strong transcriptional activation tool for application in transgenic food crops.

Abstract: The invention described herein pertains to an improved process for preparing the folate-targeted conjugate EC145 and to the conjugate EC145 prepared using the improved process, as well as to a pharmaceutical composition comprising the conjugate EC145 prepared using the improved process.

Abstract: This invention relates to fluorescent probes for screening and characterization of compounds binding to protein kinase CK2, measurement of concentration of the catalytically active form of CK2 and imaging of CK2 activity in cells and tissues. The CK2-selective probe of the present invention interacts with binding sites of both substrates of the catalytic subunit of CK2 and therefore can be used for characterization of all inhibitors binding to the active site of CK2 in the binding/displacement assay. The high affinity of the probe affords the detection of the enzyme at low concentration and characterization of inhibitors in a wide affinity range. The invention also relates to the application of the probes for mapping and monitoring of CK2 activity in cells, tissues and live organisms.

Abstract: The invention provides antibodies that inhibit activation of complement, which may be used to treat various inflammatory diseases or disorders.

Abstract: The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.

Abstract: Described herein are compounds, pharmaceutical compositions and methods for treating pathogenic cell populations in a patient. The compounds described herein include conjugates of a plurality of cytotoxic drugs and vitamin receptor binding ligands. The plurality of drugs may be the same or different. Similarly, the vitamin receptor binding ligands may be the same or different. The conjugates also include a linker that is formed from one or more spacer linkers, heteroatom linkers, and releasable linkers.

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: The invention relates to compositions and methods for monitoring phagocytic activity (e.g., diseases and conditions relating to phagocytic activity). In particular, the invention relates to compositions and methods for diagnosing, monitoring, and/or assessing risk of neurodegenerative diseases (e.g., AD).

Abstract: We describe preparation of compounds of an AT1 receptor antagonist(s) and Angiotensin (1-7), for example, Angiotensin-(1-7) losartanate and analogues thereof, and/or mixtures of these systems, pharmaceutical compositions thereof and use of their derivative products. Cyclodextrins and derivatives thereof may be used for the micro-encapsulation of compounds, for example, Angiotensin (1-7) losartanate, liposomes and biodegradable polymers and/or mixtures of these systems and/or derivative products for the obtainment of nano- or microparticles as controlled or sustained release devices of Ang-(1-7) losartanate and analogues and/or mixtures thereof. The compounds may be used as agents for treating or preventing hypertension, cardiovascular diseases, heart hypertrophy, heart failure, coronary diseases, such as angina pectoris, endothelial disorder or endothelial lesions, as a consequence, for example, of atherosclerosis processes or in association with diabetes mellitus.

Abstract: The present disclosure is directed to interleukin-10 (IL-10) peptides and isolated antibodies that specifically bind to the IL-10 peptides. The IL-10 peptides and the isolated antibodies may be administered alone or as an animal feed additive to treat gastrointestinal protozoan infection in animals.

Abstract: Conjugates of a cargo molecule with a transporter molecule are disclosed, where the cargo molecule and the transporter molecule are linked covalently by a releasable linker. The cargo of the conjugate can be a biologically active agent or a reporter molecule. The transporter modulates the transport of the cargo across a biological barrier (e.g., a cell membrane) compared to the transport of the unconjugated cargo. Releasable linkers suitable for rapid and facile conjugation to various types of cargo and transporters are also disclosed, along with methods for using the linkers in the synthesis of conjugates.

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: The present invention is directed to novel compounds of formula I and pharmaceutically acceptable salts, enantiomers thereof having inhibiting properties of dipeptidyl peptidase IV enzyme (DP-IV inhibitors). The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds along with its composition in the prevention or treatment of diseases associated with DP-IV enzyme.

Abstract: The present invention discloses compositions of peptide inhibitors of protein synthesis, and methods of identifying peptide inhibitors that are capable of inhibiting protein synthesis through an interaction at a stem-loop H18 in 16S rRNA of a 30S ribosomal subunit. Screening methods for peptides are disclosed, in addition to methods of determining the affinity of a test compound for a ribosomal subunit.

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 provides methods, compositions and kits for treating and or preventing an HIV infection. For example, HIV envelope-like polypeptides (wild-type HIV polypeptides and mimotopes) may be administered to an individual so as to induce a protective immune response to HIV. Alternatively, antibodies directed to the HIV envelope-like polypeptides may be administered to an individual to treat or prevent an HIV infection and/or one or more symptoms associated with the infection (e.g., AIDS).

Abstract: The invention relates provides a novel crystal structure of the fibrillogenic part of amyloid ?-peptide (A?). More specifically the crystal structure is A?-IgNAR and, accordingly the present invention also relates to selecting and/or designing compounds that modulate amyloid ?-peptide (A?) activity using techniques such as in silico screening and crystal soaking experiments. The invention further relates to compounds and methods for inhibiting interaction between amyloid ?-peptide (A?) monomers, more particularly, inhibiting or disrupting amyloid ?-peptide (A?) oligomer formation and toxic activity.

Abstract: The present invention relates to a prodrug comprising at least one cytostatic agent, wherein said prodrug is cleavable by prostate-specific antigen (PSA), a process for preparing said prodrug and a pharmaceutical composition containing said prodrug in a pharmaceutically effective amount, for use in the treatment of cancer.

Abstract: The present invention relates to the use of peptides that are capable of binding to, and modulating the activity of NCAM. The peptides are peptide fragments of FGFRs. They are derived from two distinct binding sites for binding of the immunoglobulin-like module 2 of FGFR to NCAM F3 modules 1-2. The invention further relates to use of said peptides for the production of a medicament for the treatment of different pathological conditions, wherein NCAM and/or FGFRs play a prominent role.

Abstract: At least one peptide molecule selected from EGDGHLGKPGROGE (SEQ ID NO:1), EKDGHPGKPGROGE (SEQ ID NO:2), G(POG)4, (POG)3, G(POG)2, (POG)2, (POG)4, (POG)5 and G(POG)3, and pharmaceutically acceptable salts thereof is effective for inhibiting various diseases such as osteoporosis, osteoarthritis and pressure ulcer. The peptide molecule is easily absorbed into a body and migrates into cells in an intestinal tract, and strongly binds to a nucleic acid compound or the like to form a complex, and thus functions well as a carrier component for delivering the nucleic acid compound or the like without causing the problems associated with conventional DDS techniques.

Abstract: Novel peptidomimetics comprising N-amino cyclic urea residues are disclosed.

Abstract: The present invention provides compounds and methods for assaying activities of enzymes such as histone deacetylases and histone acetyltransferases. In some embodiments, the methods may be performed in one step. The compounds described herein features peptide-based compounds having at least one blocked lysine or arginine residue which are coupled to reporter moieties. The methods described herein involve reacting a compound described herein with an enzyme, such as a histone deacetylase enzyme or a histone acetyltransferase enzyme, and an endopeptidase that recognizes basic amino acids to release the reporter moiety which may be subsequently detected.

Abstract: The present disclosure is directed to interleukin-10 (IL-10) peptides and isolated antibodies that specifically bind to the IL-10 peptides. The IL-10 peptides and the isolated antibodies may be administered alone or as an animal feed additive to treat gastrointestinal protozoan infection in animals.

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: 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: The present invention relates to phosphopeptide compositions and anti-phosphopeptide antibody compositions. Also provided are methods of identifying phosphorylation sites in phosphorylated peptides and phosphorylation site motifs.

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 present invention provides a peptide-phospholipid conjugate of Formula 1: wherein: X is selected from the group consisting of —CR1R2—, —R3—, —O—, —S—, and S+(R3)—; Y is selected from the group consisting of a bond, alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, amino, ether, cycloamino, cycloether, aryl heteroaryl, arylalkyl, heteroarylalkyl, hydroxyaryl, arylether, cycloalkyl, to heterocycloalkyl, hydroxycycloalkyl, halocycloalkyl, and aminocycloalkyl; Z is a peptide comprising 1 to 50 amino acids; R1 and R2 each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, amino, ether, cycloamino, cycloether, aryl, heteroaryl, arylalkyl, heteroarylalkyl, hydroxyaryl, arylether, cycloalkyl, heterocycloalkyl, hydroxycycloalkyl, halocycloalkyl, and aminocycloalkyl; and R3 is selected from the group consisting of alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, amino, ether, cycloamino, cycloether,

Abstract: The purpose of the present invention is to provide a cross-linked peptide containing a novel non-peptide cross-linked structure, and a method for synthesizing the same. A cross-linked peptide having a novel non-peptide cross-linked structure, a useful intermediate for synthesizing the cross-linked peptide, and a method for synthesizing the novel cross-linked peptide and the intermediate are provided. The cross-linked peptide is characterized by having an —NR— bond in the cross-linked structure. By using the method for synthesizing the cross-linked peptide, a cross-link can be freely designed and an change can be freely made to a cross-link.

Abstract: The present invention relates to methods of preparing ?-turn cyclic peptidomimetic compounds and intermediates thereof. Particularly, the present invention relates to a process for the synthesis of ?-turn cyclic peptidomimetic compounds of formula I: where R1, R2, R3, R4, R5, R6, R7, L2, X, Y and n are as defined in the specification. The present invention provides a more efficient route for preparing ?-turn cyclic peptidomimetic compounds and intermediates thereof.

Abstract: The invention provides an agent comprising an amino acid sequence for use in a method of diagnosis of a synucleinopathic disease.

Abstract: The present invention relates to the use of mimotopes in the treatment of diseases associated with ?-amyloid formation and/or aggregation (?-Amyloidoses) including Alzheimer's disease, whereby said mimotopes are able to induce the in vivo formation of antibodies directed to A?1-40/42, A?pE3-40/42, A?3-40/42 and A?11-40/42.

Abstract: The present invention refers to the use of protein kinase inhibitors and more specifically to the use of inhibitors of the protein kinase c-Jun amino terminal kinase, JNK inhibitor (poly-)peptides, chimeric peptides, or of nucleic acids encoding same as well as pharmaceutical compositions containing same, for the treatment of non-chronic or chronic inflammatory eye diseases, such as inflammatory diseases of the blephara, conjunctiva, cornea, sclera, the vitreous body, uvea, ciliary body, choroid, orbital bone, lacrimal gland, or iris, in particular wherein the inflammatory disease is selected from hordeolum, chalazion, conjunktivitis, keratitis, scleritis, episcleritis, endophthalmitis, panophtalmitis, irititis, uveitis, cyclitis, chorioiditis, orbital phlegmon, and myositis of the eye muscle etc.

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: The present invention generally relates to methods and compositions for preventing or treating axonal and/or neuronal degeneration in a subject by administering a composition comprising a peptide that comprises the amino acid sequence Arginine-Glycine-Aspartate (RGD).

Abstract: A peptide, wherein the peptide comprises an amino acid sequence expressed by the following SEQ ID NO: 1, an amino acid sequence expressed by the following SEQ ID NO: 2, an amino acid sequence expressed by the following SEQ ID NO: 3, an amino acid sequence expressed by the following SEQ ID NO: 4, or any combination thereof: (SEQ?ID?NO:?1) ALGDSLYGAASLN; (SEQ?ID?NO:?2) MTVDNPASTTNKDKLFSVWK; (SEQ?ID?NO;?3) PGAVPEK; and (SEQ?ID?NO:?4) STKDLTTY.

Abstract: Novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production are provided.

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: The present invention concerns isolated PAR1 cytoplasmic tail (c-tail) peptides and isolated PAR2 cytoplasmic tail (c-tail) peptides, as well as compositions comprising these peptides, uses thereof and methods of treating various diseases, in particular cancer.

Abstract: The present invention describes material and methods related to synthetic peptides which block the secretion of neurotransmitters and induce muscle relaxation, and use of said peptides as inhibitors of neurotransmitter secretion and muscle contraction, and as inducers of muscle relaxation.

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 present invention relates to novel compounds having a function of a peptide in the amylin family, related nucleic acids, expression constructs, host cells, and processes production of the compounds. The compounds of the invention include one or more amino acid sequence modifications. In addition, methods and compositions are disclosed to treat and prevent metabolic disorders such as obesity, diabetes, and increased cardiovascular risk.

Abstract: The present invention provides a conjugate that contains a therapeutic moiety linked to a homing peptide or peptidomimetic which selectively homes to vasculature of pre-malignant dysplastic skin and which includes the amino acid sequence SRPRR (SEQ ID NO: 1) or a conservative variant or peptidomimetic thereof. The present invention further provides a conjugate containing a therapeutic moiety linked to a homing peptide or peptidomimetic which selectively homes to vasculature of malignant skin and which includes the amino acid sequence CGKRK (SEQ ID NO: 6) or the amino acid sequence CDTRL (SEQ ID NO: 7), or a conservative variant or peptidomimetic of one of these sequences.

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: A method of diagnosing coeliac disease, or susceptibility to coeliac disease, in an individual comprising: (a) contacting a sample from the host with an agent selected from (i) the epitope comprising sequence which is: SEQ ID NO: 1 or 2, or an equivalent sequence from a naturally occurring homologue of the gliadin represented by SEQ ID NO: 3, (ii) an epitope comprising sequence comprising: SEQ ID NO: 1, or an equivalent sequence from a naturally occurring homologue of the gliadin represented by SEQ ID NO: 3, which epitope is an isolated oligopeptide derived from a gliadin protein, (iii) an analogue of (i) or (ii) which is capable of being recognised by a T cell receptor that recognises (i) or (ii), which in the case of a peptide analogue is not more than 50 amino acids in length, or (iv) a product comprising two or more agents as defined in (i), (ii) or (iii), and (b) determining in vitro whether T cells in the sample recognise the agent; recognition by the T cells indicating that the individual has, or is su

Abstract: The present application discloses compositions and methods of synthesis and use of 18F- or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may then be directly or indirectly attached to the targeting molecule. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the bifunctional chelating agent bound to 18F- or 19F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.

Abstract: This invention is intended to discover a peptide that induces production of an antibody specific for an abnormal amyloid ? peptide from mimic peptides of the amyloid ? peptide and to utilize the same as a vaccine or immunogen. This invention relates to a pharmaceutical composition containing a peptide consisting of 8 to 30 amino acid residues, wherein the peptide comprises at least one of an amino acid sequence represented by formula (I): Tyr-Gly-Thr-Lys-Pro-Trp-Met (SEQ ID NO: 28) (I), and an amino acid sequence represented by formula (II): Leu-Asp-Ile-Phe-Ala-Pro-Ile (SEQ ID NO: 29) (II); or a conjugate of such peptide and a carrier.

Abstract: A method for preparing stapled peptides. The stapled peptides, including helical stapled peptides, are prepared according to a photochemically-based method, a [3+2] cycloaddition reaction. The helical stapled peptides exhibit increased helicity, thermal stability and cell permeability.