574 results about "Molecular targets" patented technology

The present invention provides methods for the determination of the structure of biomolecular targets, as well as the site and nature of the interaction between ligands and biomolecular targets. The present invention also provides methods for the determination of the relative affinity of a ligand for the biomolecular target it interacts with. Also provided are methods for screening ligand or combinatorial libraries of compounds against one or more than one biological target molecules. The methods of the invention also allow determination of the relative binding affinity of combinatorial and other compounds for a biomolecular target. The present invention further provides methods for the use of mass modifying tags for screening multiple biomolecular targets. In a preferred embodiment, ligands which have great specificity and affinity for molecular interaction sites on biomolecules, especially RNA can be identified. In preferred embodiments, such identification can be made simultaneously with libraries of ligands.

Solutions for perioperative intraocular application by continuous irrigation during ophthalmologic procedures are provided. These solutions include multiple agents that act to inhibit inflammation, inhibit pain, effect mydriasis (dilation of the pupil), and / or decrease intraocular pressure, wherein the multiple agents are selected to target multiple molecular targets to achieve multiple differing physiologic functions, and are included in dilute concentrations in a balanced salt solution carrier.

Objective methods for detecting and diagnosing small cell lung cancer (SCLC) are described herein. In one embodiment, the diagnostic method involves determining the expression level of an SCLC-associated gene that discriminates between SCLC cells and normal cells. In another embodiment, the diagnostic method involves determining the expression level of an SCLC-associated gene that distinguishes two major histological types of lung cancer, non-small cell lung cancer (NSCLC) and SCLC. Finally, the present invention provides methods of screening for therapeutic agents useful in the treatment of small cell lung cancer, methods of treating small cell lung cancer and method for vaccinating a subject against small cell lung cancer. Furthermore, the present invention provides chemotherapy resistant lung cancer- or SCLC-associated genes as diagnostic markers and / or molecular targets for therapeutic agent for these cancers. These genes are up-regulated in chemoresistant lung cancer or SCLC. Accordingly, chemoresistant lung cancer or SCLC can be predicted using expression level of the genes as diagnostic markers. As the result, any adverse effects caused by ineffective chemotherapy can be avoided, and more suitable and effective therapeutic strategy can be selected.

The invention discloses an application of nanometer structure lipid carrier administration system in the antineoplastic drug to reverse the multiple-drug tolerance of tumour cell, which comprises the following parts: solid lipid material, liquid lipid material and antineoplastic drug, wherein the rate of the liquid lipid (such as oleic acid) is 0-30wt%; the solid lipid is selected from monoglyceride; the liquid lipid is oleic acid; the antineoplastic drug is Paclitaxel or adriablastina. The invention has highly effective cell uptaking and cytolymph condensing function with packing molecular target in the antineoplastic drug of cell, which avoids P-glucoprotein in the drug tolerant cytolymph from identifying the antineoplastic drug to reduce exclusion.

A method of detecting or quantifying a molecular target in a sample utilizing the molecular interaction between molecular targets, bead-bound probes, and support-bound probes. Laser light or a magnetic sensor may be used to detect the beads after the interaction. The detection of the beads indicates the presence of the molecular target in the sample.

The invention provides devices that improve tests for detecting specific cellular, viral, and molecular targets in clinical, industrial, or environmental samples. The invention permits efficient detection of individual microscopic targets at low magnification for highly sensitive testing. The invention does not require washing steps and thus allows sensitive and specific detection while simplifying manual operation and lowering costs and complexity in automated operation. In short, the invention provides devices that can deliver rapid, accurate, and quantitative, easy-to-use, and cost-effective tests.

The present invention provides phosphaplatins, stable isolated monomeric phosphate complexes of platinum (II) and (IV), and methods of use thereof for treating cancers, including cisplatin- and carboplatin-resistant cancers. Unlike cisplatin, these complexes do not readily undergo hydrolysis and are quite soluble and stable in aqueous solutions. Moreover, these complexes—unlike cisplatin, carboplatin, and related platinum-based anti-cancer agents—do not bind DNA. Rather, data suggests that phosphaplatins trigger overexpression of fas and fas-related transcription factors and some proapoptotic genes such as Bak and Bax. Nevertheless, the complexes exhibit tremendous cytotoxicity towards cancer cells. Thus, the present invention provides novel platinum anticancer agents that have a different molecular target than those in the art.

Novel methods and compositions are provided for preferentially bonding an oligomeric molecule to a macromolecular target where the target is a member of a complex mixture and / or there is preferential bonding at one of a plurality of available bonding sites of the macromolecular target. The methods represent a complete system for both producing and identifying affinity label molecules from a combinatorial library which preferentially bind to a marcomolecular target or target site and preferentially binding those affinity labels to a macromolecule of interest either ex vivo or in vivo. Macromolecular targets include a variety of cellular- and non-cellular-associated proteins.

The present invention relates to the field of medical treatments for diseases and disorders. More specifically, the present invention relates to the use of the lanthionine synthetase component C-like (LANCL) proteins as therapeutic targets for novel classes of anti-inflammatory, immune regulatory and antidiabetic drugs. This includes but it is not limited to abscisic acid (ABA), ABA analogs, benzimidazophenyls, repurposed drugs or drug combinations, including thiazolidinediones (TZDs); naturally occurring compounds such as conjugated diene fatty acids, conjugated triene fatty acids, isoprenoids, and natural and synthetic agonists of peroxisome proliferator-activated receptors that activate this receptor through an alternative mechanism of action involving LANCL2 or other membrane proteins to treat or prevent the common inflammatory pathogenesis underlying type 2 diabetes, atherosclerosis, cancer, some inflammatory infectious diseases such as influenza and autoimmune diseases including but not limited to inflammatory bowel disease (Crohn's disease and Ulcerative colitis), rheumatoid arthritis, multiple sclerosis and type 1 diabetes and other chronic inflammatory conditions.

The invention discloses a tetravalent platinum complex with a bioactive group and a preparation method of the tetravalent platinum complex. The tetravalent platinum complex is a platinum (IV) complex and has the structure shown in the formula II (please see the formula in the description), wherein in the formula II, Y is OH or Cl, and Bio represents the bioactive group. The platinum (IV) complex is prepared according to the equation in the formula III (please see the formula in the description), wherein in the formula III, Y is OH or Cl, Bio-OH represents a compound with bioactivity, TBTU represents a coupling agent O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate, TEA represents a catalyst triethylamine, DMF represents solvent N,N-dimethyl formamide, and DMSO represents solvent dimethylsulfoxide. Cis-platinum is adopted for the bottom face of an octahedron, a small-molecular targeted or medicine active group is introduced to one axial position, a hydroxyl group or helium atom is introduced into another axial position, and the anti-tumor tetravalent platinum complex overcoming cisplatin resistance is provided, so the high-efficiency and low-toxin platinum (IV) complex is obtained.

A method for identifying a patient for cancer therapy can include administering a diagnostic dose of a detectably labeled first binding agent to a patient, the detectably labeled binding agent being capable of binding a molecular target. The method also includes selecting a patient for administration of a therapeutic dose of a second binding agent capable of binding a cellular target, wherein the selected patient exhibits a positive reading for the detectably labeled first binding agent. Furthermore, the method can include administering a therapeutic dose of the second binding agent to the patient.

The disclosure relates to metallic nanophotonic crescent structures, or “nanocrescent SERS probes,” that enhance detectable signals to facilitate molecular detections. More particularly, the nanocrescent SERS probes of the disclosure possess specialized geometries, including an edge surrounding the opening that is capable of enhancing local electromagnetic fields. Nanosystems utilizing such structures are particularly useful in the medical field for detecting rare molecular targets, biomolecular cellular imaging, and in molecular medicine.

Processes for producing a microCT image for virtual histology using x-ray microscopic computed tomography are described along with processes for rapid and inexpensive high-throughput methods of high resolution imaging for screening an ex vivo embryo for phenotype using computed tomography imaging. Staining of particular components of specimens with one or more staining agents is described which contributes to high quality image generation and identification of anatomical structures as well as localization of molecular targets. Inventive animal and specimen holders are detailed which allow for reduced post-imaging processing of generated images. In particular, animal and specimen holders are provided which include a highly transparent bed or liner which separates the animal or specimen from a less transparent structure. A further animal holder is provided for placing and / or maintaining the animal in a desired position during an imaging procedure or multiple imaging procedures including a bed conforming to the animal's body.

The purpose of this invention is to provide an agent useful for prevention and / or treatment of psychosis, schizophrenia and cognitive impairments. To solve this problem, this invention provides epidermal growth factor receptor inhibitors as therapeutic agents for psychosis, schizophrenia and cognitive impairments.

The present invention relates to a nucleic acid aptamer having a first domain that binds to a fluorescent protein. The nucleic acid aptamer forms a molecular complex whereby the aptamer binds a fluorescent protein at the first domain. A constructed DNA molecule, expression systems, and host cells containing the molecular complex are also disclosed. The invention also relates to a system containing a first DNA molecule encoding the nucleic acid aptamer of the present invention and a second DNA molecule encoding a fluorescent protein capable of being bound by the first domain. Methods of detecting a molecular target and determining location of a molecular target using the nucleic acid aptamer of the invention are also disclosed.

The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.

Solutions for perioperative intraocular application by continuous irrigation during ophthalmologic procedures are provided. These solutions include multiple agents that act to inhibit inflammation, inhibit pain, effect mydriasis (dilation of the pupil), and / or decrease intraocular pressure, wherein the multiple agents are selected to target multiple molecular targets to achieve multiple differing physiologic functions, and are included in dilute concentrations in a balanced salt solution carrier.

The invention discloses a micro-molecule polypeptide TAT-p53DM and an application thereof to preparing a medicine for treating or preventing ischemic stroke. A fusion protein polypeptide TAT-p53DM of a TAT protein transduction domain and p53DM is artificially synthesized; TAT carries p53DM protein polypeptide to pass through a blood brain barrier through blood so as to be taken by nerve cells; used in an in-vitro and in-vivo ischemic stroke model, the micro-molecule polypeptide TAT-p53DM is capable of effectively playing a biological role in blocking binding between death domain of death associated protein kinase 1 (DAPK1DD) and tumor suppression protein p53DNA binding motifs (p53DM), inhibiting signals capable of causing neuronal apoptosis and necrosis at DAPK1 downstream, and reducing ischemic stroke brain injury; moreover, molecular targets are provided for further developing medicines for clinically treating ischemic stroke.

Hyper-inflammatory responses can lead to a variety of diseases including sepsis. It is now shown that extracellular histones released in response to inflammatory challenge are mediators contributing to endothelial dysfunction, organ failure and death during sepsis. As such, they can be targeted pharmacologically by inhibitors, as well as used as biomarkers for prognosis of sepsis and other diseases.

The application discloses methods for identifying and using compounds that inhibit extra-cellular matrix (ECM) degradation and inflammation, using a polypeptide sequence including SEQ ID NO: 17-127 (hereinafter “TARGETS”) and fragments thereof, expression inhibitory agents such as antisense polynucleotide, a ribozyme, and a small interfering RNA (siRNA), comprising a nucleic acid sequence complementary to, or engineered from, a naturally occurring polynucleotide sequence encoding a polypeptide of SEQ ID NO: 17-127, useful in pharmaceutical compositions comprising said agent, for the treatment, or prevention, of chronic joint degenerative and / or inflammatory diseases such as rheumatoid arthritis.

Though copper is elevated in the tumor tissue and plasma of patients with various malignancies, the molecular targets for copper binding agents in angiogenesis and tumor progression remain poorly understood. It is disclosed that one anti-angiogenic target for the copper binding agent tetrathiomolybdate is intracellular CuZn-superoxide dismutase (SOD1). A second generation tetrathiomolybdate analog, ATN-224, inhibits endothelial cell (EC) proliferation in vitro, binds to SOD1 and inhibits its activity without displacing bound copper ATN-224 can accumulate in ECs and inhibit CuZnSOD activity with an IC50 similar to the IC50 for EC proliferation, resulting in increased generation of intracellular reactive oxygen species. Inhibition of EC proliferation by ATN-224 in vitro is substantially reversed by a synthetic porphyrin SOD mimetic. Similar results were observed in vivo, where inhibition of angiogenesis by ATN-224 in a Matrigel plug model was also reversed by MnTBAP. Thus, a distinct molecular target for copper depletion therapy has been identified and SOD1 is now validated as a target for anti-angiogenesis. Methods for screening, or designing, such SOD1 inhibitors for use as angiogenesis inhibitors and anti-cancer agents are disclosed.

The present invention, among other things, provides technologies for detecting and / or quantifying nucleic acids in cells, tissues, organs or organisms. Pre-designed barcodes are associated specific molecular targets through sequential hybridization experiments. A pseudo-color based barcoding scheme is developed to overcome limitations in the previous generation of the technology such as lack of visual signals that can be associated with the probes or small internal within cell when carrying out in situ experiments. The current method can be applied to both in vitro and in situ analysis. According to the method, each barcoding round comprises multiple serial hybridizations where a small number of colored signals (that are associated with probes) are used in each hybridization experiment within a serial hybridization round. Images from each serial hybridization experiment within the same serial hybridization round are combined to form a composite image for each barcoding round. In each barcoding round, the same set of molecular targets are analyzed. After all barcoding rounds are completed, associated of the barcode with these molecular targets is completed.

Hyper-inflammatory responses can lead to a variety of diseases including sepsis. It is now shown that extracellular histones released in response to inflammatory challenge are mediators contributing to endothelial dysfunction, organ failure and death during sepsis. As such, they can be targeted pharmacologically by inhibitors, as well as used as biomarkers for prognosis of sepsis and other diseases.

The invention provides a novel target gene for diagnosing and treating tongue squamous carcinoma and application thereof and particularly relates to application of a KLK14 gene and an expression product thereof to diagnosis and treatment of tongue squamous carcinoma. To research the occurrence and development mechanisms of tongue squamous carcinoma, search for an effective molecular target gene for diagnosing and treating tongue squamous carcinoma, promote early diagnosis, prevention and treatment of the disease and lower the death rate of tongue cancer, firstly, RNA-seq sequencing is utilized to detect differential expression genes of tongue squamous carcinoma, cancer branch and normal oral mucosa; secondly, a Real-time PCR technology is utilized to verify the sequencing result; then, an interference technology is utilized, and expression of the candidate gene KLK14 in tongue squamous carcinoma cells SCC15 is silenced. By means of the novel target gene for diagnosing and treating tongue squamous carcinoma and application thereof, an experimental foundation is laid for clinical application of the KLK14 gene to tongue squamous carcinoma, and a new target gene and theoretical basis are provided for early diagnosis and treatment of tongue squamous carcinoma.

The invention discloses a mangosteen total xanthone extract and a preparation method thereof and well as application in the preparation of a TR3 receptor inducer, belonging to the field of pharmaceuticals and foods. The mangosteen total xanthone extract is applied to preparing foods or medicines for preventing or treating cancers, hepatitis or atherosclerosis as the TR3 receptor inducer. The TR3 receptor inducer and pharmaceutically-acceptable vectors are mixed to prepare powders, tablets, capsules, pills, suppositories, dropping pills, enteric-coated agents, injections, syrups, emulsions, suspensions, tinctures, ointments or sprays. Based on a mechanism that TR3 is possible to be an ideal molecular target for screening anti-tumor and cardiovascular medicines, the invention discovers and develops compounds for selectively controlling the TR3 expression approach or medicine compositions with the advanced treating characteristic and has practical meaning.

Electronic sensors configured to detect single molecule targets and methods of using and manufacturing such electronic sensors are disclosed. A sensor may include a first electrode and a second electrode separated by a sensor gap. The first and second electrodes can be coupled by a sensor complex that can include a biopolymer bridge molecule and a probe. The probe can interact with a target molecule, and interaction of the probe and target molecule can produce a signal suitable to provide detection of the target molecule.

The invention provides a peptide radioactive medicine comprising an iRGD sequence. The sequence of the peptide comprises CRGDKGPDC or CRGDRGPDC or CRGDKGPEC and is formed by marking through coupling radioactive metal nuclides or positron nuclides, the peptide radioactive medicine comprising the iRGD sequence has three functions of molecular target integrin alpha v beta 3 receptor, Neuropilin-l receptor and cellular transduction, and the peptide radioactive medicine comprising the iRGD sequence can be used as a diagnostic medicine capable of greatly increasing the target / non-target ratio, so that the sensitivity can be effectively improved, and the development quality can be improved, and the peptide radioactive medicine can be used as a therapeutic medicine capable of obviously improving the treatment effect.

The invention provides the components of in vivo and in vitro systems and methods which use them to study the effects of altered expression of a gene activity, such as the human akt, bcl-2, eIF4E or PTEN activities, on the descendants of stem cells that have been engineered to give rise to hematopoietic tumorigenic or tumor cells, such as lymphomas, with a high frequency. The present invention provides vectors, cells and mammals, and methods which in part depend on such products, useful for understanding tumorigenesis and its treatments, and in particular, for identifying and studying inhibitors and activators associated with tumor cell growth and growth inhibition, cell death through apoptotic pathways, and changes in apoptotic pathway components that affect drug sensitivity and resistance in tumorigenic cells. Methods for identifying molecular targets for drug screening, identifying interacting gene activities, for identifying therapeutic treatments and for identifying candidates for new therapeutic treatments are provided.

Autotaxin (ATX) is a prometastatic enzyme initially isolated from the conditioned media of human melanoma cells that stimulates a myriad of biological activities including angiogenesis and the promotion of cell growth, survival, and differentiation through the production of lysophosphatidic acid (LPA). ATX increases the aggressiveness and invasiveness of transformed cells, and ATX levels directly correlate with tumor stage and grade in several human malignancies. To study the role of ATX in the pathogenesis of malignant melanoma, we developed antibodies and small molecule inhibitors against recombinant human protein. Immunohistochemistry of paraffin embedded human tissue demonstrates that ATX levels are markedly increased in human primary and metastatic melanoma relative to benign nevi. Chemical screens identified several small molecule inhibitors with binding constants ranging from nanomolar to low micromolar. Cell migration and invasion assays with melanoma cell lines demonstrate that ATX markedly stimulates melanoma cell migration and invasion, an effect suppressed by ATX inhibitors. The migratory phenotype can be rescued by the addition of ATX's enzymatic product, LPA, confirming that the observed inhibition is linked to suppression of LPA production by ATX. Chemical analogues of the inhibitors demonstrate structure activity relationships important for ATX inhibition and indicate pathways for their optimization. These studies suggest that ATX is an approachable molecular target for the rational design of chemotherapeutic agents directed against human malignancies driven by the ATX / LPA axis, especially including malignant melanoma, among numerous others including breast and ovarian cancers.