829 results about "Drug screens" patented technology

Mitochondrial targets for drug screening assays and for therapeutic intervention in the treatment of diseases associated with altered mitochondrial function are provided. Complete amino acid sequences [SEQ ID NOS:1-3025] of polypeptides that comprise the human heart mitochondrial proteome are provided, using fractionated proteins derived from highly purified mitochondrial preparations, to identify previously unrecognized mitochondrial molecular components.

The invention provides systems, including apparatus, methods, and kits, for the microfluidic manipulation and/or detection of particles, such as cells and/or beads. The invention provides systems, including apparatus, methods, and kits, for the microfluidic manipulation and/or analysis of particles, such as cells, viruses, organelles, beads, and/or vesicles. The invention also provides microfluidic mechanisms for carrying out these manipulations and analyses. These mechanisms may enable controlled input, movement/positioning, retention/localization, treatment, measurement, release, and/or output of particles. Furthermore, these mechanisms may be combined in any suitable order and/or employed for any suitable number of times within a system. Accordingly, these combinations may allow particles to be sorted, cultured, mixed, treated, and/or assayed, among others, as single particles, mixed groups of particles, arrays of particles, heterogeneous particle sets, and/or homogeneous particle sets, among others, in series and/or in parallel. In addition, these combinations may enable microfluidic systems to be reused. Furthermore, these combinations may allow the response of particles to treatment to be measured on a shorter time scale than was previously possible. Therefore, systems of the invention may allow a broad range of cell and particle assays, such as drug screens, cell characterizations, research studies, and/or clinical analyses, among others, to be scaled down to microfluidic size. Such scaled-down assays may use less sample and reagent, may be less labor intensive, and/or may be more informative than comparable macrofluidic assays.

The invention provides systems, including apparatus, methods, and kits, for the microfluidic manipulation and/or detection of particles, such as cells and/or beads. The invention provides systems, including apparatus, methods, and kits, for the microfluidic manipulation and/or analysis of particles, such as cells, viruses, organelles, beads, and/or vesicles. The invention also provides microfluidic mechanisms for carrying out these manipulations and analyses. These mechanisms may enable controlled input, movement/positioning, retention/localization, treatment, measurement, release, and/or output of particles. Furthermore, these mechanisms may be combined in any suitable order and/or employed for any suitable number of times within a system. Accordingly, these combinations may allow particles to be sorted, cultured, mixed, treated, and/or assayed, among others, as single particles, mixed groups of particles, arrays of particles, heterogeneous particle sets, and/or homogeneous particle sets, among others, in series and/or in parallel. In addition, these combinations may enable microfluidic systems to be reused. Furthermore, these combinations may allow the response of particles to treatment to be measured on a shorter time scale than was previously possible. Therefore, systems of the invention may allow a broad range of cell and particle assays, such as drug screens, cell characterizations, research studies, and/or clinical analyses, among others, to be scaled down to microfluidic size. Such scaled-down assays may use less sample and reagent, may be less labor intensive, and/or may be more informative than comparable macrofluidic assays.

Benzodiazepinc compounds, and methods for using those compounds are provided. Some of the benzodiazepine compounds include 1,4-benzodiazepine-2-one and 1,4-benzodiazepine-2,5-dione compounds of structures (I) or (II): wherein R₁, R₂, R₃ and R₄ are as defined. The invention also includes enantiomers, pharmaceutically acceptable salts, prodrugs or derivatives of the benzodiazepine compounds. Any one or more of these benzodiazepine compounds can be used to treat a variety of dysregulatory disorders related to cellular death. Such disorders include autoimmune disorders, inflammatory conditions, hyperproliferative conditions, viral infections, and atherosclerosis. In addition, the above compounds can be used to prepare medicaments to treat the above-described dysregulatory disorders. The benzodiazepines can also be used in drugs screening assays and other diagnostic methods.

The present invention relates to novel methods and compositions for detection and isolation of cancer cells with metastatic potential. The invention further relates to assays for measuring the metastatic potential of such cancer cells and drug screening assays for the identification of agents having anti-metastatic potential. The present invention further provides methods and compositions for inhibiting the metastatic potential of cancer cells by modulating the activity of serine integral membrane proteases [(SIMP) consisting of seprase and dipedidyl peptidase IV (DPPIV)]expressed on the surface of metastasizing cancer cells.

Disclosed is an one-dimensional biochip belonging to a serial analytic technique for micro-total analysis systems. The one-dimensional biochip is provided with a plurality of cellules on the micro-separation channel of micro flow control chip, microparticles modified by different biomolecules on surface are arranged in different cellules; in the gene or protein analysis, when the sample flows through the microchannel with a plurality of cellules, the microparticles can specifically identify and capture multiple target molecules, then a reagent with fluorescence labels can be introduced, and finally the microparticles will specifically combine with the fluorescence labels on surface to be detected by fluorescent imaging. The one-dimensional biochip provided by the invention not only has advantages of micro flow control technology and array analysis, but also improves the detection sensitivity and identification capability of target molecules, and provides an effective research measure for the gene and protein expression analysis at single cell level, and tumor research and drug screening.

This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.

A system for making molecules, and proteins in particular, suitable for detection by a surface-selective nonlinear optical technique. A first use of the invention is for determining a protein's structure in real space and real time. A second use of the invention is to detect a protein or its activity (conformational change). A third use of the invention is for drug screening. A further aspect of the present invention is measuring probe tilt angle orientation in an oriented protein.

The invention discloses a simple green synthesis method of nitrogen-doped carbon quantum dots. Konjac flour, serving as a carbon source, is subjected to pyrolysis in air and solvent extraction to obtain the nitrogen-doped carbon quantum dots. The synthesized nitrogen-doped carbon quantum dots are easily dissolved in solvents such as ethanol, N,N-dimethyl formamide and dimethyl sulfoxide and can be ultrasonically dispersed in water, the particle size is 0.3-2.4 nm, the highest fluorescence quantum yield is 22%, and the yield is 3%-5%. The nitrogen-doped carbon quantum dots can emit blue light, green light and red light respectively under the excitation of ultraviolet light, blue light and green light, and the fluorescence property of the nitrogen-doped carbon quantum dots can be adjusted through the excitation light wavelength, concentration and pH value. The method is simple and easy to operate and can be applied to large-scale synthesis of carbon quantum dots while the cost is low. The synthesized nitrogen-doped carbon quantum dots can be applied to the development of living cells in vitro and the preparation of stimulus response materials, and have broad application prospects in multiple fields of biomarkers, biomedical imaging, bio-development, drug screening and detection, biochips, biosensing and the like.

Analogs of SRIF which are selective for SSTR4 in contrast to the other cloned SRIF receptors are useful in determining tissue and cellular expression of the receptor SSTR4 and its biological role in regulating tumor growth. SRIF analog peptides, such as des-AA^{1,2,4,5,12,13}[Ala⁷]-SRIF; des-AA^{1,2,4,5,12,13}[Aph⁷]-SRIF, des-AA^{1,2,4,5,12,13}[Aph⁷]Cbm-SRIF; des-AA^{1,2,4,5,12,13}[Tyr²,Ala⁷]-Cbm-SRIF, and des-AA^{1,2,4,5,12,13}[Tyr⁷,C^βMe-L-2Nal⁸]-SRIF, and counterparts incorporating D-Cys³ and/or D-Trp⁸ and/or Ala¹¹, bind with high affinity to the cloned human receptor SSTR4 and activate the receptor, but they do not bind with significant affinity to human SSTR1, SSTR2, SSTR3 or SSTR5. By incorporating an iodinated tyrosine in position-2 in these SSTR4-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, cytotoxins or highly radioactive elements can be N-terminally coupled or complexed thereto.

The invention provides a human brain glioma cell line and an establishing method and application thereof. The human brain glioma cell line is preserved in China Center for Typical Culture Collection with an accession number of CCTCC No. C201115. The human brain glioma cell line is established by subjecting brain glioma cells originated from a clinic specimen to primary culture and subculture, can be directly used for in vitro drug screening or generation of human brain glioma in mammals and is used for establishing a human brain glioma animal model and screening candidate drugs used for treating human brain glioma. The human brain glioma cell line has stable properties, can realize stable multiple passages and maintain stable properties even after in vitro passage to the 50th generation; pathogenesis of human brain glioma, drug susceptibility, transitivity and other related characteristics can be analyzed in vitro and in vivo, so two correlated in-vitro and in-vivo anti-brain glioma drug screening platforms can be established, and novel experimental materials closer to clinic oncobiological characteristics are provided for research on human brain glioma.

The present invention relates to methods and compositions for high content drug screening in C. elegans which may be used to identify compounds that treat disorders associated with protein aggregation.

The invention provides the appraisal and selective method for the antineoplastic drug based on the cell micrograph information, which uses a sort of selection and appraisal hardware system to appraisal and select the antineoplastic drug by different fluorescence dye marking and measuring the multicellular parameter change in cell. The hardware system is made up of the high precision electric hydrous platform, the fluorescence vision system, the image collecting and processing system and working station. The diacetoxyl fluoresceine dyeing measures the active cell number; the double dyeing method of Hoechst33342 and iodized pyridine appraise the drug inducing the cell die; the three dyeing method of FDA, Hoechst33342 and PI analyzes the die mode induced by drug. The invention can measure at least two kinds of single cell or cell subgroup which expresses different drone cell organ. The method is in reason and can be used in study of drug action mechanism and selecting the high hedonic drug and toxicity analyzing, which can be used in selecting drug and appraising the drug toxicity.

The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:

A stochastic algorithm has been developed for predicting the drug-likeness of molecules. It is based on optimization of ranges for a set of descriptors. Lipinski's “rule-of-5”, which takes into account molecular weight, logP, and the number of hydrogen bond donor and acceptor groups for determining bioavailability, was previously unable to distinguish between drugs and non-drugs with its original set of ranges. The present invention demonstrates the predictive power of the stochastic approach to differentiate between drugs and non-drugs using only the same four descriptors of Lipinski, but modifying their ranges. However, there are better sets of 4 descriptors to differentiate between drugs and non-drugs, as many other sets of descriptors were obtained by the stochastic algorithm with more predictive power to differentiate between databases (drugs and non-drugs). A set of optimized ranges constitutes a “filter”. In addition to the “best” filter, additional filters (composed of different sets of descriptors) are used that allow a new definition of “drug-like” character by combining them into a “drug like index” or DLI. In addition to producing a DLI (drug-like index), which permits discrimination between populations of drug-like and non-drug-like molecules, the present invention may be extended to be combined with other known drug screening or optimizing methods, including but not limited to, high-throughput screening, combinatorial chemistry, scaffold prioritization and docking.

The invention relates to ecosustainable and biocompatible, low cost, ambient friendly electronic and optoelectronic devices, such as transistors and light-emitting transistors, made with silk fibroin or blended with other biopolymers, methods for fabrication and methods of using the silk-based electronics and optoelectronics. The silk-based electronics and optoelectronics can be implanted in vivo and in vitro for biomedical applications, such as for drug discovery or drug screening assays and devices. The silk-based devices may be used in the food industry and embedded in packaging for tracking and sensing, for security purposes or exploited as disposable not harmful for the environment efficient general electronic and optoelectronic devices.

Light-generating fusion proteins having a ligand binding site and a light-generating polypeptide moiety and their use as diagnostics, in drug screening and discovery, and as therapeutics, are disclosed. The light-generating fusion protein has a feature where the bioluminescence of the polypeptide moiety changes upon binding of a ligand at the ligand binding site. The ligand may be, for example, an enzyme present in an environment only under certain conditions, e.g., ubiquitin ligase in a hypoxic state, such that the light-generating fusion protein is “turned on” only under such conditions.

The invention discloses a micro-flow control chip for cell tissue culture and real-time monitoring and a use method thereof. The chip comprises a glass substrate layer and a PDMS micro-flow channel layer positioned on the glass substrate layer; the glass substrate layer comprises a glass substrate and a plurality of pairs of microelectrodes arranged on the glass substrate layer; the PDMS micro-flow channel layer comprises a plurality of independent micro-fluidic channels; the microelectrodes on the glass substrate are corresponding to the micro-flow channels on the PDMS micro-flow channel layer one by one; the microelectrodes are electrically connected with an external circuit. The use method comprises the steps of cell capture, cell tissue culture, electrical impedance spectroscopy detection and tissue release. The chip disclosed by the invention is processed by a transparent substrate, microscopic imaging can be taken as a supplementary means of the electrical impedance spectroscopydetection, and the dynamic growth and the physiological behavior of cell tissues and other biological processes are subjected to observation and in-situ analysis. The micro-flow control chip can be used in the fields of biological research, drug screening and the like of cells or tissues.

The invention relates to a microfluidic diffusion and open intervening cell culture array chip and a fabrication method and application thereof. The cell culture array chip is suitable for cell culture, stem cell proliferation, drug screening, regenerative medicine and the like. The cell culture array chip comprises a base and a substrate fixed on the base, wherein a plurality of hole-like cell culture unit are distributed on the substrate; and a microfluidic main channel and a microfluidic diffusion channel, which are intercommunicated with each other, are arranged on the substrate and are communicated with each cell culture unit and the external environment. The cell culture array chip provided by the invention has the following advantages: (1) the required culture solution, growth factors and the like are supplied through a microfluidic diffusion network, so as to result in a zero cell shearing force and ensure the gas and moisture environment required for cell growth; (2) the in vivo microenvironment multichannel microfluidic concentration gradient of cells is simulated, and the quantitative drug release at a fixed time and other functions are realized; (3) the chip is suitable for high-throughput drug screening research on cell phenotype; and (4) the chip has a compact structure and low cost, and is suitable for batch production.