Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.

Abstract: The preset invention relates to use of antipsychotic phenothiazine derivative for eliminating cancer stem cells (CSCs) and/or preventing a cancer. The invention also provides a pharmaceutical composition for treating a cancer, and/or preventing or delaying cancer recurrence comprising trifluoperazine and an anti-cancer drug, such as gefitinib or cisplatin.

Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing a PGAM1 mediated condition such as cancer or tumor growth comprising administering an effective amount of PGAM1 inhibitor, for example, an anthracene-9,10-dione derivative to a subject in need thereof. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, head and neck cancer, and leukemia, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.

Abstract: The present invention provides that Ras-like, estrogen-regulated, growth inhibitor (RERG) is a malignant mesothelioma biomarker of clinical course and treatment sensitivity and, itself a target for mesothelioma treatment. A low RERG level in a mesothelioma subject indicates poor prognosis. Analyzing RERG expression level along can help mesothelioma patients make treatment choices. Furthermore, mesothelioma can be treated by modulating RERG activity, for example, with treatment with estrogen or estrogen-like agents.

Abstract: The present invention relates to novel gold-platinum based bi-metallic nanocrystal suspensions that have nanocrystal surfaces that are substantially free from organic or other impurities or films associated with typical chemical reductants/stabilizers and/or raw materials used in nanoparticle formation processes. Specifically, the surfaces are “clean” relative to the surfaces of metal-based nanoparticles made using chemical reduction (and other) processes that require organic (or other) reductants and/or surfactants to grow (and/or suspend) metal nanoparticles from metal ions in a solution. The invention includes novel electrochemical manufacturing apparatuses and techniques for making the bi-metallic nanocrystal suspensions. The techniques do not require the use or presence of chlorine ions/atoms and/or chlorides or chlorine-based materials for the manufacturing process/final suspension.

Abstract: The present invention relates to compositions for the treatment of cancerous tissues in warm-blooded animals containing one or two anticancer agents attached to polymeric carriers having monomer units derived from one or more of N-(2-carboxypropyl)methacrylamide (2-CPMA), N-(3-carboxypropyl)methacrylamide (3-CPMA), N-(2-aminopropyl)methacrylamide (2-APMA) and/or N-(3-aminopropyl)methacrylamide (3-APMA) are also included. Anticancer agents in compositions can be attached to said polymeric carrier by side-chains which can be susceptible to hydrolysis by lysosomal enzymes intracellularly. Compositions can also include a targeting ligand attached to the polymeric carrier, optionally through a second linker.

Abstract: The application is directed to a fibrin sealant (FIBRINGLURAAS®) consisting of a kit of lyophilized or frozen high concentrate fribinogen in which 5% a1at will be added into the final bulk and or 5% a1at as a diluent for high concentrate fibrinogen and new found proteins kh30, kh31, kh32, kh44, kh46, kh47, and kh52 in which the kh good healthy cells are present, either non-heated or heating to at least 1° C. and above, preferably at least 101° C., and lyophilized or frozen thrombin used to compound glue membrane, the diameter of which is less than 10 micrometers the actual size of the glue membrane of the fibrin sealant (FIBRINGLURAAS®) is from 0.6 ?m, to 101° C. heating 0.

Abstract: Provided are methods of determining a response to a chemotherapeutic agent in a subject with ovarian cancer, comprising: determining a RNA integrity value of a sample comprising ovarian cancer cell RNA from the subject after the subject has received one or more doses of the chemotherapeutic agent; wherein a low RNA integrity value and/or RNA degradation of the cancer cell RNA is indicative that the cancer is responding to the chemotherapeutic agent and/or a high RNA integrity value and/or stable RNA integrity of the ovarian cancer cell RNA is indicative that the cancer is resistant to the chemotherapeutic agent.

Abstract: Provided herein are methods and kits for evaluating potential for invasiveness, metastasis, or recurrence of an epithelial cell cancer. In the methods the expression profile of giant obscurins is detected in a tissue sample of tumor cells or suspected tumor cells and assessed for giant obscuring expression level and distribution therein. Decreased levels or altered distribution of giant obscurins in the cells compared to a control non-invasive standard or to a sample taken at a different point in time is indicative of increased potential of at least one of the invasiveness, metastasis, or recurrence of the epithelial cell cancer. The kit comprises a detection reagent suitable for detecting the presence and distribution of giant obscurins or an amount of the gene product(s) encoding giant obscurins in cells of a tissue sample and instructions for using the detection reagent.

Abstract: A pharmaceutical combination comprising a platinum-containing anticancer agent, and an Hsp90 inhibitor according to the following formulae (I) & (Ia), a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein. Also provided is a method of treating a proliferative disorder such as cancer in a subject in need thereof, using the pharmaceutical combination described herein.

Abstract: The present invention is a method and compound for treating cancer and tumors. The invention treats cancer by encapsulating certain cancer fighting drugs in a liposome. Peptides attached to the compound then guide the compound towards its target. During its journey, DSPE-PEG is used to stabilize the compound, to allow more time in the blood stream before losing effectiveness.

Abstract: The present invention generally relates to the neuroprotective activity of condensed diazepinones, e.g. condensed benzodiazepinones such as pirenzepine or compounds which are metabolized to condensed benzodiazepinones such as olanzapine. These compounds are suitable as co-medicaments for the prevention and/or treatment of drug-induced neurotoxic effects in general and neurotoxic side effects during cancer treatments with cytostatic drugs such as platinum-derivatives, e.g. cis-, carbo- and oxaliplatin, taxanes, bleomycin, cyclophosphamide and vincristine etc. Further, these compounds have an intrinisic anti-cancer activity on their own due to PARP-1 inhibition, which prevents NADH depletion in oxidative metabolism of healthy cells thus preventing the shift to anoxygenic, glycolytic metabolism present in many types of tumour cells thus eliminating this crucial metabolic advantage favouring tumour growth.

Abstract: Polymorphic forms of onapristone and methods of making and using such polymorphic forms are provided. Crystalline polymorphic forms can be characterized by their X-ray powder diffraction patterns and other properties.

Abstract: An extract of Carica papaya leaves obtained from a plant of age six months and younger from the date of germination of the seed is used as an inhibitor of HIF to effectively block hypoxia-inducible factor (HIF) function and methods of use thereof. More specifically it relates to the use of the Carica papaya plant extract to eliminate unwanted cells by inhibiting HIF in the prevention and treatment of hypoxia-related conditions and diseases such as inflammatory diseases, vascular diseases, cancer and infectious diseases. In a particular embodiment, a solid hypoxic tumor in a patient is treated by administering to the patient a therapeutically acceptable amount of an extract of Carica papaya leaves obtained from a plant of age six months and younger from the date of germination of the seed, preferably an alcohol extract such as a methanol extract, whereby to inhibit hypoxia-inducible factors in the tumor.

Abstract: The present invention provides a composition for the treatment of cancer including zwitterionic liposomes consisting essentially of: 50-65 mol % of a phosphatidylcholine lipid, 30-45 mol % of cholesterol, and 2-8 mol % of a PEG-lipid; and cisplatin. Cisplatin is encapsulated in the liposomes in an amount such that the ratio of the total lipid weight to the cisplatin weight is from about 65:1 to about 95:1. Methods for the preparation of liposomal cisplatin and the treatment of cancer are also disclosed.

Abstract: Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.

Abstract: The present invention relates to substituted imidazopyridine compounds of general formula (I) in which R3, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

Abstract: The invention relates to fusion constructs, methods of using fusion constructs and methods of treating undesirable or aberrant cell proliferation or hyperproliferative disorders, such as tumors, cancers, neoplasia and malignancies.

Abstract: In an aspect, the invention relates to compositions and methods for permeabilizing membranes of cells. In an aspect, the invention relates to compositions and methods for killing cells. In an aspect, the invention relates to compositions and methods of permeabilizing the membranes of cancer cells or microbial cells.

Abstract: Most human tumors find ways to resist anticancer drug monotherapy. Akt is considered a likely peptide providing such monotherapy drug resistance. Data indicates that Akt chemoresistance is induced in a p53-dependent manner and that inhibition of Akt may be an effective means of overcoming chemoresistance in cancer cells expressing wild-type p53. Breast, ovarian, lung cancer and leukemia cells lines were treated with combinations of Akt activation inhibitor Triciribine (TCN) or Triciribine phosphate (TCNP) and chemotherapeutic drugs to determine the efficiency of combination therapy. Additionally, cells were introduced into xenograft models to determine in vivo effects of combination treatment. Combining TCN or TCNP with other anticancer drugs overcame cytotoxic or treatment resistance. Thus, TCN and TCNP are shown to broaden the spectrum of human tumors that can be effectively treated.

Abstract: This invention relates to compounds and their use as inhibitors or activators of Rab7 GTPase to treat or prevent the onset of Rab 7 GTPase-associated disorders such as neuropathies, cancer, metabolic diseases of bone and lipid storage. The invention is also applicable to infectious diseases where Rab7 is inactivated or its protein-protein interactions are modulated to facilitate intracellular survival of pathogens. The compound described acts as a competitive inhibitor of nucleotide binding and as such also has utility as a scaffold for targeting other small GTPases. In one aspect, methods of treatment of the invention are used to treat or prevent the onset of hereditary sensory neuropathies such as Charcot-Marie-Tooth type 2B disease. Related pharmaceutical compositions, assays, and drug screens are also provided.

Abstract: The invention provides a method for treating cancer using a coadministration strategy that combines local codelivery of a therapeutic agent and an intracellular penetration enhancing agent, and optionally in further combination with local administration of an immunotherapeutic agent, such as a cancer vaccine or NKT agonist. The invention also provides a method for treating cancer using an intracellular penetration enhancing agent. The methods of the invention aim to substantially kill and/or destroy the target tumor cells, as well as those cancerous cells that have metastasized to other parts of the body.

Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.

Abstract: The present invention relates generally to new chemical combinations and methods for their use in the treatment of proliferative diseases and in particular cancer.

Abstract: Methods for preventing and/or reducing side effects of an anti-cancer agent in a subject in need thereof are disclosed. The method comprises administering to the subject, who is under an anti-cancer agent treatment, a composition comprising a therapeutically effective amount of isolated deoxyelephantopin and/or an analogue thereof; and a pharmaceutically acceptable carrier.

Abstract: A method for providing antisense therapy which reduces the expression of clusterin to provide therapeutic benefits in the treatment of cancer comprising administering from 40 to 640 mg anti-clusterin antisense oligonucleotide to a patient in need of treatment for a cancer expressing clusterin is provided. The method may include administering chemotherapeutic agent or agents, radiotherapy, and/or hormone ablation therapy. The invention also encompasses pharmaceutical compositions formulated to provide a dosage of 40 to 640 mg, and use of antisense in formulating a medicament.

Abstract: This invention relates to bio synthesis of novel nano gold through environment friendly process with the aid of plant materials classified under the taxonomical genus Dalbergia, Citrus, Ferula and Dolichos or Macrotyloma. The present inventive product novel nano gold finds utility in, the treatment of humans and animals, nutraceutical, cosmeceutical and herbal composition, the field of technology including but not limited to nano technology, green technology and bio technology. The invention also relates to the use of plant materials in the purification and particle size reduction of metals.

Abstract: A caged platinum nanocluster complex is disclosed. The complex comprises (a) an amine-terminated dendrimer; and (b) a platinum nanocluster comprising platinum oxides, the platinum nanocluster being confined inside of the amine-terminated dendrimer. The complex exhibits cytotoxicity to cancer cells. A double-caged platinum nanocluster complex is also disclosed, which comprises polyethylene glycol (PEG) coated on the surface of a dendrimer caged platinum nanocluster complex. The double-caged caged platinum nanocluster complex comprises pH-sensitive bonds on the surface thereof. Also disclosed are methods of preparing and using the same.

Abstract: The various embodiments herein provide super paramagnetic iron oxide nanoparticles (SPIONs). The SPIONs have a plurality of metallic coatings and plurality of polymeric gaps. The embodiments herein also provide a method of synthesizing the SPIONs with metallic rings and polymeric gaps. The metallic coatings form a ring like structure on the outer surface of the SPION. The SPION has a size of 13 nm. The ring has a thickness of 2-3 nm. The rings are one or more in number. The polymeric gaps have a thickness of 3-5 nm. The polymeric gaps are one or more in number. The method involves mixing the SPIONs with a plurality of polymers and then forming a metallic ring on the outer surface of the SPIONs. The SPIONs have anti-bacterial properties and stop a growth of bacterial biofilms. The SPIONs also have SERS properties.

Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

Abstract: A delivery device for topical and systemic delivery of agents to targeted oral locations, such as mouth cancer cells, has been developed. The formulation includes a mucoadhesive polymeric matrix such as chitosan, which contains one or more therapeutic and/or diagnostic agents, taste masking agents, permeation enhancers, the therapeutic or diagnostic agent to be delivered, and a hydrophilic polymeric coating such as polyethyleneglycol (“PEG”). In the preferred embodiment, the matrix is formulated with one side having the PEG-mucoadhesive polymer exposed for topical placement onto epithelial or cancer cells in the mouth or other mucosal area and the side(s) facing the inside of the oral cavity being covered with a biocompatible, inert membrane that is impermeable to the therapeutic and/or diagnostic agent(s) to be delivered.

Abstract: The invention relates to the use of encapsulates of cancer cells, in agarose coated, agarose containing beads, for isolating chemotherapeutic resistant cells which have at least one stem cell property, such as expression of OCT4.

Abstract: Provided herein is a pharmaceutical composition comprising at least one isoflavonoid. Also provided herein are methods of treating cancer, sensitizing cancer cells, and inducing apoptosis in cancer cells by administering such compositions.

Abstract: A method of improving longevity and/or alleviating a symptom of aging or preventing age related diseases is provided. The method includes a step in which the subject's average and type of daily protein intake, IGF-I, and IGFBP1 levels, and risk factors for overall mortality, cancer and diabetes are determined. With respect to protein consumption, the relative amounts of protein calories from animal and plant sources are determined. A periodic normal calorie or low calorie but low protein fasting mimicking diet with frequencies of every 2 weeks to 2 months is provided to the subject if the subject's average daily protein intake level and type and/or IGF-I levels, and/or IGFBP1 levels is identified as being greater or lower than a predetermined cutoff intake/level and if the subject is younger than a predetermined age. The method is also shown to alleviate symptoms of chemotoxicity.

Abstract: Erastin analogs are useful in treating various cancers, particularly multiple myeloma. Erastin analogs are also useful in treating cancers that are resistant to other anticancer agents.

Abstract: The problem of the present invention is to provide a highly effective therapeutic drug for pancreatic cancer and/or biliary tract cancer. A therapeutic drug for pancreatic cancer and/or biliary tract cancer containing the following (1) and (2) as essential components: (1) at least one kind of branched-chain amino acid selected from the group consisting of isoleucine, leucine and valine, (2) gemcitabine or a salt thereof.

Abstract: Described herein are compounds, compositions and methods for treatment of cancer. Also described are methods and uses for identifying subject with cancer that are suitable for treatment with the compounds, composition and methods are described herein. In one aspect of the present invention, there is provided a method of treating a subject having a cancer deficient in NMT2, comprising: administering to said subject an NMT inhibitor.

Abstract: The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates, in part, to methods for determining a prognosis of early stage lung cancer in an individual using one or more biomarkers.

Abstract: The present invention relates to peptidomimetics for reactivating p53. Methods of using the peptidomimetics are also disclosed.

Abstract: Methods and products for detecting in vitro the presence of damage on DNA or the presence of a biological response to damage on DNA at the molecular level. Molecular Combing or other nucleic acid stretching methods are employed together with compounds reacting with DNA, probes binding DNA, or nucleic acid monomers, especially labeled nucleic acid monomers.

Abstract: The invention features methods of treating an immune disorder characterized by elevated Pin1 marker levels in a subject by administering a retinoic acid compound. Additionally, the invention features methods of treating immune disorders (e.g., immune disorders characterized by elevated Pin1 marker levels) by administering a retinoic acid compound in combination with an anti-inflammatory, anti-viral, or anti-microbial compound.

Abstract: The present invention relates to methods of diagnosing lung cancer in a patient, as well as methods of monitoring the progression of lung cancer and/or methods of monitoring a treatment protocol of a therapeutic agent or a therapeutic regimen. The invention also relates to assay methods used in connection with the diagnostic methods described herein.

Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.

Abstract: Administration of compositions comprising cell-permeable caPCNA-derived peptides and their variants reduces the proliferation of cancer cells and also augments cytotoxic effects of chemotherapeutics. The compositions are effective in cells harboring mutations in DNA repair proteins.

Abstract: The present invention relates to peptidomimetics for reactivating p53. Methods of using the peptidomimetics are also disclosed.

Abstract: Gelatinous foam, coated paper, fabric, and polymer materials combined with the Colloidal Silver or Gold additive to formulate products with antimicrobial surfaces. Some embodiments of the present invention can include gelatinous materials selected from a group consisting of thermosetting polymer, Styrene-Ethylene-Butadiene-Styrene polymer (SEBS), Thermoplastic Elastomer (TPE), and Polyurethane (PU) gelatin with and without a raised geometry on an outer surface and in any shape. The various embodiments include coated polymer sheets, polymer trays, bamboo and/or cotton towels and fabric, polymer foam, or polymer mats containing nano-silver or nano-gold in an scheduled and organized manner (with input/requests from the customer) to create permanent or semi-permanent anti-microbial surfaces.

Abstract: It is an object of the present invention that the novel nicotinic receptor antagonists disclosed herein may be used in a broad array of clinical or medicinal facets. For example, it is a contemplated use of the present invention that the novel nicotinic receptor antagonists be used to inhibit the growth cycle of non-small cell lung cancer cells. Without being bound by theory, it is an object of the present invention that the nicotinic receptor antagonists disclosed herein are believed to possess reversible binding properties. Moreover, the compounds of the present invention are selective for 0.7 nAChR. For example, the compounds of the present invention are not believed to bind to 0.4 (32 nAChR neuromuscular receptors. It is also contemplated that the nicotinic receptor antagonists of the present invention will be used as a counter measure to treat exposure, or potential exposure, to a wide array of potential neurotoxins.

Abstract: Methods of treating, preventing or managing cancers are disclosed. The methods encompass the administration of SNS-595 in combination with a second active agent. In certain embodiments, the method of treatment comprise administering SNS-595 in combination with cisplatin, carboplatin, gemcitabine or a combination thereof.

Abstract: The present invention relates to oligooxopiperazines for reactivating p53. Methods of using the oligooxopiperazines are also disclosed.