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 relates to fibulin-3 protein and a pharmaceutical composition comprising the fibulin-3 protein as an active ingredient for inhibiting the growth of cancer stem cells. More particularly, in cancer stem cells separated from H460 and A549 cells, which are non-small-cell lung cancer cells, using ALDH1 activity as a marker, fibulin-3 induces the reductions of wnt/?-catenin, MMP2 and 7, which display characteristics of cancer stem cells, thereby decreasing the activated growth and penetration of the cancer stem cells. In addition, the purified fibulin-3 protein inhibits the growth of the non-small-cell lung cancer cell line A549, the breast cancer cell line MDA-MB231, and the cancer stem cell line active ALDH1. Therefore, fibulin-3 can be valuably used as an active ingredient of the pharmaceutical composition for inhibiting the growth of cancer stem cells.

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: 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: 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: The present invention relates to a method for treating breast cancer in a subject having a breast cancer of the triple-negative type, which method comprises the step of administering to said subject a therapeutically effective amount of a modulator of the protein tyrosine phosphatase, non-receptor type 11 (PTPN11) gene or of its gene product (Shp2).

Abstract: The present invention relates to antibodies, antibody fragments, and derivatives thereof that specifically bind to TLR3 cell receptors present on the surface of cells. The invention also relates to hybridomas producing such antibodies; methods of making such antibodies; fragments, variants, and derivatives of the antibodies; pharmaceutical compositions comprising the same; methods of using the antibodies to detect TLR3 levels on the surface of cells, and the use of such antibodies and compositions for diagnostic or therapeutic purposes in subjects.

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: According to the present invention, a cancer antigen protein to be specifically expressed on the surfaces of cancer cells is identified and thus the use of an antibody targeting the cancer antigen protein as an agent for treating and/or preventing a cancer is provided. Specifically, the present invention provides a pharmaceutical composition for treating and/or preventing a cancer, which comprises an antibody comprising a heavy chain variable region that comprises SEQ ID NOS: 39, 40, and 41 and a light chain variable region that comprises SEQ ID NOS: 43, 44, and 45 or a fragment thereof as an active ingredient and having immunological reactivity with a CAPRIN-1 protein.

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: Methods, compositions and articles of manufacture for contributing to the treatment of a solid cancerous tumor are disclosed. The methods, compositions and articles of manufacture can utilize an endothelin B agonist (ETB) to enhance the delivery of a chemotherapeutic agent to a solid tumor in mammals, including humans.

Abstract: Provided is a method of determining the level of resistance or sensitivity of cancer stem cells to a death receptor agonist. The method includes detecting the level of IAP in one or more DR5/DDX3/IAP complexes in or from the cancer stem cells. Also provided is a method of killing cancer stem cells in a subject and a method of reducing the risk of cancer recurrence in a subject.

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: According to the present invention there is provided a specific binding member which is specific for and binds directly to the ED-B oncofoetal domain of fibronectin (FN). The invention also provides materials and methods for the production of such binding members.

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

Abstract: The present invention is related to new peptide antagonists of ?v?3 receptor, designed on the basis of the crystal structure of integrin ?v?3 in complex with c(RGDf[NMe]V) and the NMR structure of echistatin. These peptides are potent and selective antagonists of the ?v?3 receptor and can be used as novel anticancer drugs and/or new class of diagnostic non-invasive tracers as suitable tools for ?v?3-targeted therapy and imaging.

Abstract: This invention pertains to the discovery that an amplification of the CYP24 gene or an increase in CYP24 activity is a marker for the presence of, progression of, or predisposition to, a cancer (e.g., breast cancer). Using this information, this invention provides methods of detecting a predisposition to cancer in an animal. The methods involve (i) providing a biological sample from an animal (e.g. a human patient); (ii) detecting the level of CYP24 within the biological sample; and (iii) comparing the level of CYP24 with a level of CYP24 in a control sample taken from a normal, cancer-free tissue where an increased level of CYP24 in the biological sample compared to the level of CYP24 in the control sample indicates the presence of said cancer in said animal.

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 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 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: 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 present invention relates to an activin receptor type II B (ACVR2B) inhibitor which comprises the delta-like 1 homolog (DLK1) extracellular water-soluble domain. More specifically, the present invention relates to an extracellular soluble domain of DLK1; fragments of the extracellular soluble domain of DLK1; mutants of the extracellular soluble domain of DLK1; a composition for suppressing ligand linkage with the ACVR2B receptor, which includes a fragment of the mutants as an active ingredient; and a pharmaceutical composition for prevention and treatment of diseases which comprises the same. The composition of the present invention competitively binds to the ACVR2B receptor and inhibits the binding of an ACVR2B ligand to the ACVR2B receptor, which inhibits protein signalling associated with such ligands, and will be useful for prevention and treatment of diseases associated therewith.

Abstract: The present invention relates:—to 2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo-[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide dihydrochloride salt of formula (II): or a tautomer, solvate or hydrate thereof;—to methods of preparing said dihydrochloride salt;—to said dihydrochloride salt for the treatment and/or prophylaxis of a disease;—to the use of said dihydrochloride salt for the preparation of a medicament for the treatment and/or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, more particularly for the treatment or prophylaxis of a cancer, particularly lung cancer, in particular non-small cell lung carcinoma, colorectal cancer, melanoma, pancreatic cancer, hepatocyte carcinoma, pancreatic cancer, hepatocyte carcinoma or breast cancer;—to a pharmaceutical composition comprising said dihydrochloride salt; and to a pharmaceutical combination comprising said dihydrochloride salt in combination with one or more further pharmaceutical agent

Abstract: A method of treating or preventing inflammatory related diseases in a subject in need thereof comprising administering to said subject a pharmaceutically effective amount of a composition comprising an immune modulating polypeptide of SEQ ID NO: 1 is provided. A method for inhibiting cancer metastasis or growth of tumor in a subject in need thereof, comprising administering to the subject a pharmaceutically effective amount of a composition comprising an immune modulating polypeptide of SEQ ID NO: 1 is also provided.

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: Disclosed are compositions and corresponding methods for treating fibrocystic breast disease or other breast-related disease or condition. The compositions comprise, per serving or dose, from zero to about 400 ?g selenium, from about 100 mg to about 6000 mg gamma linolenic acid, and about 0.15 mg to about 5 mg iodine, with nutritional embodiments further comprising one or more of protein, fat, carbohydrate, vitamins, and minerals and providing from about 50 to about 1000 kcal of energy per severing or dose. Also disclosed are in-vitro studies showing that certain combinations of gamma linolenic acid, iodine, and/or selenium may 1) inhibit breast cancer or fibrocystic cell proliferation, 2) reinforce the function of tight junctions of endothelial cells and of mammary epithelial cells in estrogen-sensitive conditions, and 3) reduce the risk of vascular invasion by breast cancer cells.

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: 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: 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: Provided herein are peptides and nanoparticles conjugates thereof useful for the treatment of diseases and disorders mediated by GIPC/synectin, such as cancer.

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: 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: 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 relates to methods and compositions for modulating TNF and TNFR signaling. In particular, the disclosure describes methods and compositions for inhibiting TNF? signaling, such as in the prevention or treatment of TNF?-related diseases.

Abstract: The application describes methods for predicting overall survival in subjects with breast cancer. The application also describes for screening subjects with breast cancer to determine if the breast cancer will be responsive to a breast cancer therapy including gemcitabine. The application further describes methods for treating subjects with breast cancer by screening them for the likelihood of the effectiveness of treating the cancer with a therapy including gemcitabine and administering the therapy in subjects when it is found that gemcitabine is likely to be effective.

Abstract: Compounds which are ?-halogenoacryloyl distamycin derivatives of formula (I) wherein R1 is a bromine or chlorine atom; R2 is a distamycin or distamycin-like framework as set forth in the specification; or a pharmaceutically acceptable salt thereof; are cytotoxic agents particularly effective in the treatment of tumors over expressing GSH/GSTs system and which are poorly responsive or even resistant to conventional antitumor therapies.

Abstract: Provided is the composition of a peptide and its mutagenic version, or other derivatives with the same 3-D structure with activity to bind the extracellular domain of PDGFR-?, or -?, but does not dimerize by itself, wherein said peptide comprises the sequence shown as SEQ ID NO: 1, 2 or 3. Also provided is the composition of the nucleotide sequence encoding said peptide and its derivatives, and the usage of said peptide and derivatives of the peptide in preparation of medicine for the prevention and treatment of fibrosis diseases, such as liver, kidney, and lung fibrosis, primary cancer, and cancer metastasis, especially stomach cancer, liver cancer, breast cancer, and lung 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: Methods for diagnosis and treatment of cancer using ID4 are disclosed. Specifically, epigenetic inactivation of ID4 in colorectal carcinomas and breast correlates with poor differentiation and unfavorable prognosis. Further, aberrant hypermethylation of ID4 gene promoter region increases risk of metastasis in colorectal and breast cancer.