Abstract: Aspects of the invention include compositions and methods for inhibiting the interaction between scaffold proteins and kinases. These compositions and methods find a number of uses including, for example, suppressing tumor growth and metastasis and reducing tumor size and number in a mammal with cancer.

Abstract: Antitumoral compounds of Formula I, and pharmaceutically acceptable salts, derivatives, tautomers, prodrugs or stereoisomers thereof useful as antitumour agents.

Abstract: The invention provides RGD-containing cyclic peptidomimetics; conjugates of said peptidomimetics and a moiety of a payload selected from fluorescent probes, photosensitizers, chelating agents, or cytotoxic agents; and pharmaceutical compositions comprising these conjugates. The conjugates of the invention are useful both for diagnostic purposes and treatment of various diseases, disorders and conditions. More specifically, conjugates comprising fluorescent probes can be used for diagnostic purposes, e.g., visualization of organs and tissues, and diagnosis of tumors; conjugates comprising photosensitizers can be used for photodynamic therapy of both tumors and nonneoplastic tissues; conjugates comprising chelating agents can be used in radioimaging or radiotherapy; and conjugates comprising cytotoxic agents can be used for targeted chemotherapy.

Abstract: Methods to treat certain types of cancer with cyclophilin inhibitors.

Abstract: The present invention relates to kinase inhibiting compositions and uses thereof. The invention further provides isolated kinase inhibiting peptides and uses thereof for inhibiting hyperplasia, for inhibiting the growth of neoplasms, and for inducing programmed cell death in a cell population.

Abstract: The present invention provides the use of a peptide comprising an amino acid sequence of SEQ ID NO:3, or the encoding nucleic acid thereof, for manufacturing medicament for treatment of diseases associated with increased NF-?B activity. The peptide can interact with IKB and influence phosphorylation of IKB in the tyrosine at position 42, thereby inhibiting the signal pathway of NF-?B.

Abstract: Analogues of cyclosporin-A are disclosed comprising modifications of the substituents as the positions of amino acids 1 and 3, according to the following Formula. The disclosed compounds include compounds having affinity for cyclophilin, including cyclophilin-A, and reduced immunosuppressivity in comparison with cyclosporin-A and analogs thereof modified solely at position 1.

Abstract: Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds. The compounds of the invention have potential therapeutic activity in view of their binding and inhibitory activities towards Plk1. They are based on the amino acid sequence PLHSpT (phosphorylated Thr). The PEG moiety, when present, is covalently attached at the N-terminus.

Abstract: Methods, compositions and articles of manufacture for contributing to the treatment of cancers, including solid tumors, are disclosed. The methods, compositions and articles of manufacture can utilize an endothelin B agonist (ETB) to enhance the delivery and resulting efficacy of a chemotherapeutic agent.

Abstract: Methods and compositions are provided for inhibiting metastasis of a tumor in a subject, or of inhibiting progression of a primary tumor in a subject which requires macrophages for progression.

Abstract: A method of treatment of inflamed, pre-cancerous or cancerous tissue or polyps in a mammalian subject is disclosed. The treatment involves administration of a composition of at least one peptide agonist of a guanylate cyclase receptor and/or other small molecules that enhance intracellular production of cGMP. The at least one peptide agonist of a guanylate cyclase receptor may be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The inhibitor may be a small molecule, peptide, protein or other compound that inhibits the degradation of cGMP. Without requiring a particular mechanism of action, this treatment may restore a healthy balance between proliferation and apoptosis in the subject's population of epithelial cells, and also suppress carcinogenesis.

Abstract: The invention features targeted cytotoxic compounds and methods relating to their therapeutic use for the treatment of neoplasia and other conditions.

Abstract: The present invention provides a drug delivery system for targeted delivery of therapeutic agent-containing particles to tissues, cells, and intracellular compartments. The invention provides targeted particles comprising a particle, one or more targeting moieties, and one or more therapeutic agents to be delivered and pharmaceutical compositions comprising inventive targeted particles. The present invention provides methods of designing, manufacturing, and using inventive targeted particles and pharmaceutical compositions thereof.

Abstract: The invention provides structurally-constrained peptides by hydrocarbon stapling of a BCL9 HD2 helix for use as a therapeutic agent. The invention further provides methods and kits for use of the structurally-constrained peptide of the instant invention. The invention is based, at least in part, on the results provided herein demonstrating that hydrocarbon stapled helical peptides display excellent proteolytic, acid, and thermal stability, restore the native helical structure of the peptide, possess superior pharmacokinetic properties compared to the corresponding unmodified peptides, and are highly effective in binding to ?-catenin in vitro, in cellulo, and in vivo, disrupting the BCL-9/?-catenin interaction, and thereby interfering with deregulated Wnt/?-catenin signaling for therapeutic benefit in a variety of human diseases including human cancer.

Abstract: The invention provides methods and dosing regimens for safely and effectively treating androgen-dependent prostate cancer with a gonadotrophin releasing hormone (GnRH) antagonist without causing a testosterone spike and/or other side effect of GnRH agonist therapy such as a urinary tract infection, or an arthralgia-related or cardiovascular side effect.

Abstract: Methods of treating a disease in a subject are provided comprising administering to the subject an amount of an agent which reduces, or prevents, interaction of a G?? with a pi 110? effective to treat the disease. Methods are also provided for identifying an inhibitor of interaction between a G?? and a ?110?. Compositions are provided comprising a peptide comprising amino acid residues having the KAAEIASSDSANVSSRGGKKFLPV (SEQ ID NO:6).

Abstract: Methods are provided for inhibiting growth of prolactin-responsive cancer cells and treating prolactin-responsive malignancies via administration of an agent such as cyclosporine A which directly inhibits an enzymatic activity of a cyclophilin.

Abstract: The present invention provides compositions, compounds, and methods relating to recombinant adenoviral-based polypeptides for treating disorders associated with epithelial tissues.

Abstract: The invention provides methods for reducing growth and/or metastasis of androgen-independent (castration resistant) prostate cancer in a tissue in an animal. In one embodiment the method comprises administering to the animal a therapeutically effective amount of a compound that reduces the number of B cells, and/or the function of B cells, in the tissue. In yet another embodiment, the invention provides methods for reducing androgen-induced growth of prostate epithelial cells in prostate tissue in an animal. In one embodiment, the method comprises administering to the animal a therapeutically effective amount of a compound that reduces the number of B cells, and/or the function of B cells, in the tissue.

Abstract: Disclosed here is the rational design and use of potent and specific GPCR antagonist pepducins based on GPCR regions such as the third intracellular loop and adjacent regions.

Abstract: The present invention provides a self assembly molecule having an affinity for one or more target molecules, for use in formation of a heptameric complex, comprising: a) a monomer comprising a multimerization domain of Archaeal Sm1 (AF-Sm1) protein or SM-like ribonucleoprotein from other organisms, able to interact with other molecules of the same monomer comprising a multimerization domain of AF-Sm1 protein or SM-like ribonucleoprotein to self-assemble into a heptamer; and b) a target binding domain or peptide attached directly or via a linker to the monomer of (a). Also provided are heptamers comprising these self assembly molecules and methods for their use in therapy, imaging and diagnostics.

Abstract: The instant invention relates to novel solid materials of {[(2S,5R,8S,11S)-5-benzyl-11-(3-guanidino-propyl)-8-isopropyl-7-methyl-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaaza-cyclopentadec-2-yl]-acetic acid}, methods for producing them, and the use of said solid materials in pharmaceuticals.

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 present invention discloses compositions and methods for treating diseases such as cancer by targeting luteinizing hormone (LH) or its receptor (LHR) involved in androgen synthesis or testosterone production.

Abstract: A method for modulating Sonic hedgehog (Shh)-mediated signalling and proliferation based on agents that modulates the binding of GAS1, BOC and/or CDON to Ptch1 is disclosed. Methods and compositions for treating cancer using agents that inhibit the binding of GAS1, BOC and/or CDON to Ptch1 are also disclosed. Methods for identifying agents that may be used to inhibit Shh-mediated signalling/proliferation and cancer based on their capacity to inhibit the binding of GAS1, BOC and/or CDON to Ptch1 are also disclosed.

Abstract: The present invention discloses anti-cancer compositions, and associated methods, including an anti-cancer composition comprising: a cellular energy inhibitor having the structure according to formula I wherein X is selected from the group consisting of: a nitro, an imidazole, a halide, sulfonate, a carboxylate, an alkoxide, and amine oxide; and R is selected from the group consisting of: OR?, N(R?)2, C(O)R??, C1-C6 alkyl, C6-C12 aryl, C1-C6 heteroalkyl, a C6-C12 heteroaryl, H, and an alkali metal; where R? represents H, alkali metal, C1-C6 alkyl, C6-C12 aryl or C(O)R??, R? represents H, C1-C6 alkyl, or C6-C12 aryl, and R?? represents H, C1-C20 alkyl or C6-C12 aryl. The anti-cancer composition can additionally comprise at least one sugar, which stabilizes the cellular energy inhibitor by substantially preventing the inhibitor from hydrolyzing. Also, the anti-cancer composition can comprise a hexokinase inhibitor.

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: A composition and method for cancer treatment comprising FK330 or a salt thereof as an active ingredient, which is for combined administration with one or more anti-tumor agents selected from taxane-family anti-tumor agents, and according to an embodiment, a composition for treatment of prostatic cancer or ovarian cancer. This abstract is not limiting of the invention.

Abstract: The present invention relates to a novel endocytic motif, and in particular, to a fusion polypeptide including the motif represented by an amino acid sequence of SEQ ID NO. 1 and a protein transduction domain, a pharmaceutical composition for preventing or treating cancer including the same, and a method for treating cancer including the step of administering the composition. The present invention shows the effects of suppressing metastasis, infiltration, angiogenesis, and growth of cancer by specifically inhibiting c-Met endocytosis and effectively inhibiting HGF/c-Met signaling pathway associated with metastasis and growth of various types of cancer cells. Therefore, the present invention can be applied to an anticancer agent for various types of cancer.

Abstract: It is disclosed herein that SPANX-B is uniquely expressed in a number of human tumors and that SPANX-B is an immunogenic antigen that is recognized by human T cells inducing helper CD4+ and cytolytic CD8+ T cell responses. Specific SPANX-B polypeptides and polynucleotides are disclosed that can be used to generate an immune response. In several embodiments, these polypeptides can be used for the treatment of a variety of cancers, including melanoma, colon carcinoma, ovarian cancer, breast cancer, myeloma, lung carcinoma and renal cancer.

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 provides human secreted proteins (SECP) and polynucleotides which identify and encode SECP. The invention also provides expression vectors, host cells, antibodies, agonists, and antagonists. The invention also provides methods for diagnosing, treating, or preventing disorders associated with aberrant expression of SECP.

Abstract: Provided are a pharmaceutical composition which enhances the sensitivity of a cancer to a molecular target drug, such as gefitinib and erlotinib, wherein the cancer has resistance to the molecular target drug, and a cancer therapeutic agent effective against a cancer having resistance to a molecular target drug, such as gefitinib and erlotinib. The pharmaceutical composition comprising an HGF-MET receptor pathway inhibitor enhances the sensitivity of a cancer to a molecular target drug, such as gefitinib and erlotinib, even though the cancer has resistance to the molecular target drug. The cancer therapeutic agent comprising a molecular target drug in combination with an HGF-MET receptor pathway inhibitor is effective against a cancer having resistance to the molecular target drug.

Abstract: Short peptide mimetics of adiponectin suitable for development as pharmaceutical agonists in the treatment of cellular proliferative disorders such as cancer and atherosclerosis are provided.

Abstract: Disclosed herein are PACE4 inhibitors, compositions comprising PACE4 inhibitors and their uses thereof for lowering PACE4 activity, reducing cell proliferation, reducing tumor growth, reducing metastasis formation, preventing and/or treating cancer. Also provided are methods for lowering PACE4 activity, reducing the proliferation of a cell, reducing tumor growth and/or treating and preventing cancer. Methods for screening PACE4 inhibitors and cell proliferation inhibitors are further provided.

Abstract: The proposed pharmaceutical compositions and methods connected thereto relate to the field of biotechnology and medicine, in particular to pharmaceutical compositions having an antiproliferative activity, and to a method of treating oncologic diseases, which includes introducing the aforementioned chimerical peptide into a mammal requiring such treatment. The object of the proposed compositions and methods is the development of a preparation that effectively penetrates the target cells and has a high cytostatic and cytotoxic action.

Abstract: The present invention thus provides microbial products as anticancer agents and pharmaceutical compositions comprising isolated and purified proteins or synthetic peptides, and methods of using them for the treatment of cancer. It is very important to develop new anticancer bioactive peptides having high activity and low toxicity; given that most currently available anticancer therapies either have significant toxicity, and/or are prone to development of resistance.

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 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: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones thereof, represented by the Formula (I) wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.

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

Abstract: This invention relates to a method for stimulation or an activation of immunological function directed to activate natural killer cells and macrophages or increase production of serum antibody in a patient in need of such stimulation or activation, comprising administering an isolated and/or purified polypeptide of a fungal immunomodulatory protein. This invention also relates to a method for suppressing proliferation of a cancer cell and a method for suppressing a tumor cell mobility, comprising providing to the tumor cell a purified polypeptide of a fungal immunomodulatory protein.

Abstract: There is disclosed agents capable of inhibiting the binding of a MAP kinase to a binding domain of an integrin for the MAP kinase, and methods of modulating the activity of a cell utilizing the agents. The methods are particularly suitable for inhibiting the growth of cancer cells.

Abstract: The present invention concerns a combination of (i) a polypeptide comprising ATIP3 or a biologically active fragment thereof, and (ii) a chemotherapeutic drug that is an antimitotic agent, for simultaneous or sequential use in the treatment of a patient suffering from cancer, e.g. a triple-negative breast cancer. The present invention also relates to a polypeptide comprising ATIP3 or a biologically active fragment thereof, for use in sustaining drug effect, increasing or restoring or enhancing sensitivity of a patient suffering from cancer to a chemotherapeutic drug that is an anti-mitotic agent. The present invention further provides biologically active polypeptides that comprise or consist of fragments of ATIP3, and antibodies binding thereto.

Abstract: The subject application pertains to a compound of structure IX or X: or a pharmaceutically acceptable salt thereof, wherein: X is —C(?O)N(R10)— or —CH(OPr3) —; R7, R9 and R10 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid; Pr1 and Pr2 are the same or different and represent hydrogen or a thiol protecting group; Pr3 is hydrogen or an alcohol protecting group; R1, R2, R5 and R6 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid, or R1 and R2 and/or R5 and R6, taken together with the carbon atom to which they are attached, form a spirocyclic moiety, with the proviso that: each of R1 and R2 is not hydrogen, or each of R5 and R6 is not hydrogen.

Abstract: The present invention combines a targeted cargo protein with an active agent for the treatment of a disease or condition.

Abstract: The present invention is directed to methods, kits and compositions for preventing or treating age-related conditions or metabolic disorders. The Klotho fusion polypeptides of the invention include at least a Klotho protein or an active fragment thereof. In one embodiment, the fusion polypeptide comprises a Klotho polypeptide, a FGF (such as FGF23) and (optionally) a modified Fc fragment. The Fc fragment can, for example, have decreased binding to Fc-gamma-receptor and increased serum half-life. The Klotho fusion proteins are useful in the treatment and prevention of a variety of age-related conditions and metabolic disorders. In another embodiment, the fusion polypeptide comprises a FGF (such as FGF23) and a modified Fc fragment.

Abstract: Methods for treating or preventing a Foxp3+ T regulatory cell (Treg) related disease in a subject in need thereof comprise administering to the subject an effective amount of a pharmaceutical composition comprising an inhibitor of a histone/protein acetyltransferase (HAT). Methods for identifying an agent useful for treating or preventing a Foxp3+ T regulatory cell (Treg) related disease comprise (a) contacting a candidate agent with a test sample comprising Foxp3+ T regulatory cells (Tregs), and (b) comparing a function of the Foxp3+ Tregs in the test sample with that in a control sample, wherein inhibition of the function of the Foxp3+ Tregs in the test sample when compared with the control sample indicates that the candidate agent is an agent useful for treating or preventing a Foxp3+ Treg related disease.

Abstract: Disclosed is an isolated or purified polypeptide or peptidomimetic comprising an amino acid sequence of a portion of a Smoothened (SMO) protein, wherein the portion comprises an amino acid sequence of any of the intracellular loops of the SMO protein, a functional fragment thereof, or a functional variant of either the portion or the functional fragment, wherein the functional fragment comprises at least 7 contiguous amino acids of the intracellular loops, and wherein the functional fragment or functional variant inhibits proliferation of a diseased cell, or a fatty acid derivative thereof. Related conjugates, nucleic acids, recombinant expression vectors, host cells, and pharmaceutical compositions are further provided.