Abstract: The present invention relates to inhibitors of Nox1-dependent reactive oxygen species production and their use in the treatment of disorders associated with reactive oxygen species, such as hypertension and cancer.

Abstract: Methods for predicting clinical outcome for a human subject diagnosed with squamous cell lung carcinoma using a panel of molecular markers that includes CDKN2A and CCND1. The markers are related to the subject's increased likelihood of a negative clinical outcome.

Abstract: The present invention discloses peptides such as an isolated peptide consisting of an immunogenic HLA-A*2402-restricted epitope. For example, the isolated peptide may be selected from the group consisting of KYGVLLKTL (SEQ ID NO:11); RYMRQFVAL (SEQ ID NO: 12); RYVSRLLGI (SEQ ID NO: 13); RYGKGWDLL (SEQ ID NO: 14); RYLVQVQAL (SEQ ID NO: 15); and RYWELSNHL (SEQ ID NO: 16).

Abstract: The present invention provides a monoclonal antibody which specifically recognizes RGD in the amino acid sequence of extracellular matrix proteins of a human and a mouse. By specifically inhibiting the RGD sequence-mediated adhesion, exertion of efficient effects on diseases such as inflammation, cancer, infectious disease, autoimmune diseases and osteoporosis and reduction in adverse effects can be expected at the same time. Therefore, better treatment methods can be provided to these diseases.

Abstract: The present invention is directed to peptide reagents, methods for detecting colon pre-cancer (dysplasia with non-polypoid or polypoid morphology) or cancer using the peptide reagents, and methods for targeting pre-cancerous or cancerous colon cells using the peptide reagents.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.

Abstract: An immunity-inducing agent comprising as an effective ingredient(s) at least one polypeptide selected from the following polypeptides, the polypeptide(s) having an immunity-inducing activity/activities, or as an effective ingredient(s) a recombinant vector(s) which comprise(s) a polynucleotide(s) encoding the polypeptide(s) and is/are capable of expressing the polypeptide(s) in vivo can be used for therapy and/or prophylaxis of cancer: (a) a polypeptide consisting essentially of not less than 7 consecutive amino acids in any one of the amino acid sequences shown in the odd number IDs of SEQ ID NOs:3 to 95 in SEQUENCE LISTING; (b) a polypeptide having a sequence identity of not less than 90% with the polypeptide (a) and consisting essentially of not less than 7 amino acids; and (c) a polypeptide comprising the polypeptide (a) or (b) as a partial sequence thereof.

Abstract: A PEG-oligopeptide-irinotecan conjugate has the general formula (I) (shown below) and a pharmaceutical composition containing the conjugate are disclosed. In the conjugate, PEG represents polyethylene glycol with a molecular weight of 300-60,000 Daltons; (AA)i represents an oligopeptide, AA represents the same or different amino acids in the oligopeptide; i is an integer of 2-12 representing the number of amino acids in the oligopeptide; j is an integer of 2-12 representing the number of irinotecan connected with the oligopeptide. In the conjugate, each terminal group of PEG can link with multiple irinotecans through oligopeptides, thereby greatly increasing the drug-loading capacity. Modification of the hydrophilic polymer can provide protection for the irinotecan, thereby improving drug absorption, prolonging the action time, enhancing the efficacy, reducing the dose and avoiding the toxic and side-effects.

Abstract: The invention relates to combining targeted therapies with selected chemotherapeutics for the treatment of melanoma. The invention provides a method for inducing apoptosis in a melanoma tumor cell by reducing Akt3 activity, a method for inducing apoptosis in a melanoma tumor cell comprising contacting a melanoma tumor cell with an agent that reduces Akt3 activity to restore normal apoptotic sensitivity to a melanoma tumor cell, allowing a lower concentration of chemotherapeutic agents resulting in decreased toxicity to a patient. Also disclosed is a method for treating a melanoma comprising administering an agent that reduces Akt3 activity and an agent that reduces V599E B-Raf activity, thereby treating a melanoma tumor.

Abstract: The present invention provides pharmaceutical compositions and methods of treating lower gastrointestinal disorders, including inflammatory bowel disease (IBD), diverticulitis, colon cancer, an inflammatory disorder, obesity, congestive heart failure, benign prostatic hyperplasia (BPH), pain, salt retention or fluid retention.

Abstract: N-acylpeptide derivatives are described. Compositions comprising N-acylpeptide derivatives are therapeutically effective for topical or systemic administration to alleviate or improve conditions, disorders, diseases, symptoms or syndromes associated with tumors or cancers, immune, nervous, vascular, musculoskeletal, cutaneous system, or other tissues or systems in a subject.

Abstract: The present disclosure provides isolated integrin ?L polypeptides, such as ?7 helix polypeptides from the alpha I domain of integrin. Such polypeptides inhibit the interaction between integrin and gp96, thereby inhibiting gp96 activity. Such inhibition can be used to prevent cancer cell growth, cancer metastasis and/or inflammation.

Abstract: Provided are TCL1 peptides that bind to MHC I (HLA-A2) on tumor cells or other antigen-presenting cells and are recognized by T-cell receptors on T cells. The TCL1 peptides may be therapeutically used to treat a cancer, such as a B cell malignancy, leukemia, or lymphoma. Methods for expanding a population of T cells that target TCL1 are also provided.

Abstract: The present invention provides variant activin IIB soluble receptor polypeptides and proteins capable of binding and inhibiting the activities of activin A, myostatin, or GDF-11. The present invention also provides polynucleotides, vectors and host cells capable of producing the variant polypeptides and proteins. Compositions and methods for treating muscle-wasting and other diseases and disorders are also provided.

Abstract: The present invention relates to a modified human tumor necrosis factor receptor-1 polypeptide which is capable of binding to a tumor necrosis factor in vivo or ex vivo, or to a fragment thereof. The modified human tumor necrosis factor receptor-1 polypeptide or the fragment thereof according to the present invention exhibit improved binding affinity to the tumor necrosis factor.

Abstract: The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.

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: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Abstract: Provided is a fusion protein comprising circularly permuted form of TRAIL, and the fusion protein contains circularly permuted form of TRAIL and oligopeptides located at the N-terminus and/or C-terminus of the permuted form. The oligopeptides contain a repeating sequence consisting of 3-10 histidines. The components of the circularly permuted form of TRAIL from N-terminus to C-terminus are: (a) amino acids 135-281 of TRAIL, (b) a linker, and (c) amino acids 121-135 of TRAIL or amino acids 114-135 of TRAIL or amino acids 95-135 of TRAIL or any fragments of amino acids 95-135 of TRAIL containing amino acids 121-135 of TRAIL. Also provided is a method for treating cancer by using the fusion protein.

Abstract: The present invention discloses cell penetrating peptides (CPP or membrane translocating peptide) and their conjugates with cargo molecules. The peptides are useful as drug delivery systems, particularly as delivery vehicles for nucleotide-based theraputics, such as polynucleotides, oligonucleotides and peptide nucleic acids. A CPPs of the invention provides a balance between good cell entry efficency and low toxicity and comprises three contiguous domains: the central one being hydrophobic and the flanking ones consisting of arginine and aminohexanoic acid or beta-alanine residues. The hydrophobic domain contains a sequence selected from YQFLI, YRFLI, IQFLI and IRFLI.

Abstract: The present invention is directed to methods of using HSS1 (Hematopoietic Signal peptide-containing Secreted 1), HSM1 (Hematopoietic Signal peptide-containing Membrane domain-containing 1), or a combination thereof in the treatment of various cancers, such as brain cancers.

Abstract: The present invention provides bivalent and multivalent ligands with a view to improving the affinity and pharmacokinetic properties of a urea class of PSMA inhibitors. The compounds and their synthesis can be generalized to multivalent compounds of other target antigens. Because they present multiple copies of the pharmacophore, multivalent ligands can bind to receptors with high avidity and affinity, thereby serving as powerful inhibitors. The modular multivalent scaffolds of the present invention, in one or more embodiments, contains a lysine-based (?-, ?-)dialkyne residue for incorporating two or more antigen binding moieties, such as PSMA binding Lys-Glu urea moieties, exploiting click chemistry and one or more additional lysine residues for subsequent modification with an imaging and/or therapeutic nuclides or a cytotoxic ligands for tumor cell killing.

Abstract: Provided herein are liposomal glycolipopeptidic vaccine formulations comprising an adjuvant and an immunogen for immunotherapy and/or treatment of cancer.

Abstract: The invention relates to Optineurin-derived polypeptide(s) consisting of a polypeptidic sequence disclosed in SEQ ID no2, which represents the portion of the wild-type human Optineurin protein sequence from its amino-acid residue 131 to its amino-acid residue 297, or having a polypeptidic sequence encompassing the polypeptidic sequence disclosed in SEQ ID no2, or having a polypeptidic sequence derived from the polypeptidic sequence disclosed in SEQ ID no2 to the exclusion of the wild-type Optineurin protein. The polypeptide(s) of the invention retain one, any combination of two, or three of the following functional properties: the capacity to bind Rab8 protein, when the latter are associated with the Golgi apparatus of a cell, the capacity to bind MYPT1 protein, when said protein is engaged in a Myosin-Phosphatase (MP) complex, the capacity to be phosphorylated by Plk1.

Abstract: The invention relates to polypeptides, defined through a consensus sequence, having a length from 10 to 80 amino-acid residues, and whose polypeptidic sequence comprises or consists of the consensus sequence P1(Xa)P3(Xb)P5(Xc)P6(Xd)P7 (SEQ ID NO: 1), presenting specific patterns. The polypeptides of the invention target glycosylated Muc2 proteins. The invention also relates to methods of synthesis of such polypeptides, to their nucleic acids and uses thereof. The polypeptidic sequence of the polypeptides of the invention can be part of the N-terminal sequence of a mucus-binding (MUB) domain, especially a mucus-binding (MUB) domain of several species. The invention also relates to chimeric molecule(s) comprising such polypeptides, which are labelled, and vectors, especially plasmids and population of cells or composition comprising polypeptides of the invention. Synthesis methods encompass biotechnological or chemical production.

Abstract: A compound can destabilize a binding interaction between an epidermal growth factor receptor (EGFR) and a sodium/glucose co-transporter 1 (SGLT 1). In one embodiment, the compound is a peptide derived from the interacting domain of EGFR. In another embodiment, the peptide is administered to a patient to treat cancer.

Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.

Abstract: Described are methods and compositions for treating epithelial tumors with a folate-vinca conjugate in combination with at least one other chemotherapeutic agent in which the tumors include ovarian, endometrial or non-small cell lung cancer tumors, including platinum-resistant ovarian tumors and platinum-sensitive ovarian tumors.

Abstract: The present invention relates to LRP6 constructs that bind to LRP6 receptor. The LRP6 constructs comprise at least one LRP6 binding moiety and a half-life extender molecule such that the LRP6 construct inhibit the Wnt signaling pathway without potentiation of the Wnt signal. The LRP6 constructs also have an increased half-life to provide more time for the therapeutic benefit.

Abstract: Methods for treating cancer comprising administering a DLL4 antagonist and one or more anti-hypertensive agents are described. Also described are pharmaceutical compositions comprising a DLL4 antagonist and one or more anti-hypertensive agents, and kits comprising the same.

Abstract: The present invention relates to compositions and methods for characterizing, diagnosing and treating cancer. In particular, the present invention identifies LGR5 as a protein over-expressed in solid tumor stem cells. The present invention further identifies an interaction between RSPO1 and LGR5 as an alternative pathway for the activation of beta-catenin signaling. In certain embodiments, the present invention provides biomolecules that disrupt functional signaling via a LGR protein, including, in certain embodiments, molecules that inhibit the interaction between one or more RSPO proteins and one or more LGR proteins, such as LGR5. In certain embodiments, the present invention provides methods of treating cancer comprising disrupting functional LGR signaling and inhibiting growth of a solid tumor comprising solid tumor stem cells.

Abstract: The present invention provides oligopeptides comprising the amino acid sequence selected from the group consisting of SEQ ID NOs: 3, 4 and 5. The present invention also provides a pharmaceutical composition containing the amino acid sequence of selected from the group consisting of SEQ ID NOs: 3, 4 and 5 formulated for the treatment or prevention of cancer in a subject. Furthermore, the present invention provides a method of inducing immune response using such oligopeptides and pharmaceutical agents.

Abstract: HER2 binding polypeptides comprising the amino acid sequence EX1 RNAYWEIA LLPNLTNQQK RAFIRKLYDD PSQSSELLX2E AKKLNDSQ wherein X1 in position 2 is M, I or L, and X2 in position 39 is S or C (SEQ ID NO:1) are disclosed. Moreover, such peptides comprising a chelating environment are disclosed. Also radiolabeled polypeptides formed by the peptides comprising a chelating environment and radionuclides are disclosed. Furthermore, methods of in vivo imaging of the body of a mammalian subject having or suspected of having a cancer characterized by overexpression of HER2 comprising administration of such a radiolabeled polypeptide followed by obtainment of an image of the body using a medical imaging instrument and also methods of treating such cancer are disclosed. Furthermore, the use of such a radiolabeled polypeptide in diagnosis and treatment of cancer characterized by overexpression of HER2.

Abstract: The present embodiments provide for compositions and methods that regulate microRNA-binding protein-mediated miRNA biogensis; for example Lin28-mediated biogenesis of let-7; and in particular Lin28A-recruited 3? terminal uridylyl transferase (TUTase) uridylation of pre-let-7. A particular embodiment provide compositions and methods for screening for agents that inhibit TUTase-dependent Lin28A-mediated repression of let-7 miRNA.

Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition, including Crohn's disease and ulcerative colitis, and cancer.

Abstract: The present invention involves the pharmaceutical field, including integrin antagonists, which have the capacities of inhibiting angiogenesis of tumors, binding integrin. These antagonists are a kind of polypeptide, which was modified by polyethylene glycol and after modification, it can be used to treat tumors. The sequence and structure of these antagonists is mPEG-SC20k-Ile-Val-Arg-Arg-Ala-Asp-Arg-Ala-Ala-Val-Pro-Gly-Gly-Gly-Gly-Arg-Gly-Asp, which demonstrates it is scientific, reasonable and feasible in tumor treatment and greatly expands the treatment spectrum. It can provide new ideas and perspectives for drug development and has significant social and market value.

Abstract: The present invention relates to a peptide inhibiting a matrix metalloproteanases activity and use thereof. The peptide inhibiting a matrix metalloproteanases activity exhibits an excellent efficacy of improving the condition of skin by directly inhibiting the matrix metalloproteanases activity. In addition, a composition containing the peptide of the invention has excellent bioactivities of inhibiting the activity of hyaluronic acid degrading enzymes, adipogenesis in fat cells, angiogenesis, and the like, thereby being useful for the treatment of various disease such as anti-obesity, anti-cancer, anti-inflammation, and the like, and skin permeability is excellent due to the small size of the peptide, thereby being useful in various fields. The peptide of the invention having excellent activity and safety can be advantageously applied to drugs, quasi-drugs, and cosmetics.

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 provides a tumor cell-killing peptide and a pharmaceutical composition for treating a cancer. The tumor cell-killing peptide of the present invention selectively homes into tumor cells so that it can induce the death of tumor cells effectively while minimizing the harming of normal cell.

Abstract: There is provided a series of novel neuropeptide Y-cytotoxic conjugates, compositions comprising the same, and methods relating to their therapeutic use for the treatment of disease or condition states associated with aberrant or undesirable proliferation of cells that express NPY-Y1 receptors.

Abstract: Disclosed herein are maytansinoid drug linker derivatives which can be linked to a antigen binding unit (Abu), and maytansinoid drugs linked with an antigen binding unit (Drug-Linker-Antigen binding Unit: D-L-Abu), for targeted delivery to disease tissues. D-L-Abu, D-L-Abu derivatives, and methods relating to the use of such drug conjugates to treat antigen positive cells in cancers and immunological disorders are provided.

Abstract: Therapeutic peptides having guanylyl cyclase C agonist activity are disclosed. The therapeutic peptides are analogues of the E. coli STa peptide with non-natural amino acid, isosteric or D-amino acid substituents. The therapeutic peptides are useful in the treatment of chronic ideopathic constipation, inflammatory bowel disease, and other diseases. Pharmaceutical compositions comprising the therapeutic peptides are also disclosed.

Abstract: Provided are fragments of human p97 (melanotransferrin) polypeptides having blood-brain barrier (BBB) transport activity, including variants and combinations thereof, conjugates comprising said p97 fragments, and related methods of use thereof, for instance, to facilitate delivery of therapeutic or diagnostic agents across the BBB.

Abstract: The invention relates to a method for de-differentiating a cell, i.e. the induction of a pluripotent phenotype. In vivo de-differentiation is carried out using defined factors such as transcription factors, miRNA, DNA, or proteins. This leads to the formation of pluripotent cells, without teratoma formation. Defined factors may be administered to cells such as liver or muscle cells and are useful in therapy.

Abstract: The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.

Abstract: The present invention is directed to improved compositions for cellular delivery of peptides. Using segments of only 3-5 positively-charged residues, one can effectively transfer peptides, including therapeutic peptides, into cells. Also provided are modified peptides such as those include stapled and cyclized peptide technology, as well as peptoids/peptidomimetics.

Abstract: Molecules and compositions are described for use in the treatment and prevention of pro-inflammatory conditions. HDL-related molecules, including ApoA-I, bovine HDL and HDL mimetics, in particular, are demonstrated to prevent UV-induced cell death and oxidative stress in skin cells and to inhibit tumor growth and development in a variety of cancers. HDL-related molecules can be used as an oral supplement and in other compositions to prevent or treat pro-inflammatory skin conditions and systemic proinflammatory conditions, including Alzheimer's disease and various cancers.

Abstract: The invention provides a molecule that inhibits or prevents an interaction between a Src family kinase and an androgen or estradiol receptor, for use in preventing or treating a non-cancerous condition in which an activity of AR and/or ER is a contributory factor in a subject, or for use in preventing or treating a cancerous condition in which an activity of AR and/or ER is a contributory factor in a subject who wishes to preserve fertility, or for use in preventing or treating a gynaecological condition in which an activity of AR and/or ER is a contributory factor in a subject.

Abstract: This invention is related to a pharmaceutical combination that contains a Casein kinase 2 (CK2) peptide inhibitor (termed P15) along with the standard chemotherapeutic drugs used in cancer treatment and which are administered together, separated or sequentially. The chemotherapeutic drugs include cisplatin, taxol, alkaloids from Vinca, 5-fluorouracil, doxorubicin, cyclophosphamide, etoposide, mitomicin C, imatinib, iressa and velcade (vortezomib). The synergism between the P15 peptide and the anticancer drugs achieves an efficient concentration of each cytostatic drug in the combination which is from 10- to 100-fold lower than that for each cytostatic drug alone. The pharmaceutical combination described in this invention exhibits lower toxicity compared to that reported by the anticancer therapeutics and therefore, it represents a crucial advantage for its use in cancer therapy.

Abstract: A pharmaceutical composition for treating or preventing peritoneal dissemination is provided. The pharmaceutical composition includes an effective dose of connective tissue growth factor (CTGF) and a pharmaceutically acceptable carrier thereof.