Abstract: Conjugated compounds which comprises an ST receptor binding moiety and a radiostable active moiety are disclosed. Pharmaceutical compositions comprising a pharmaceutically acceptable carrier or diluent, and a conjugated compound which comprises an ST receptor binding moiety and a radiostable active moiety or an ST receptor binding moiety and a radioactive active moiety are disclosed. Methods of treating an individual suspected of suffering from metastasized colorectal cancer comprising the steps of administering to said individual a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent, and a therapeutically effective amount of a conjugated compound which comprises an ST receptor binding moiety and a radiostable active moiety or an ST receptor binding moiety and a radiostable active moiety are disclosed.

Abstract: The problem of how to select out of a large chemically accessible universe molecules representative of the diversity of that universe is resolved by the discovery of a method to validate molecular structural descriptors. Using the validated descriptors, optimally diverse subsets can be selected. In addition, from the universe, molecules with characteristics similar to a selected molecule can be identified. The validated descriptors also enable the generation of a huge virtual library of potential product molecules which could be formed by combinatorial arrangement of structural variations and cores. In this virtual library it is possible to search billions of possible product compounds in relatively short time frames.

Abstract: The invention concerns a polypeptide possessing thyrotropin receptor activity characterized in that it comprises the amino acid sequence shown in FIG. 11 (i.e., SEQ ID NO: 59) and cDNA molecules encoding this polypeptide. The invention also relates to vectors comprising cDNAs which encode the polypeptide of FIG. 11, cells transformed with these vectors, and the use the transformed cells expressing the thyrotropin receptor as in the detection of TSH or antibodies against the thyrotropin receptor.

Abstract: Invented is a method of preparing combinatorial libraries and combinatorial libraries prepared thereby. Also invented is a method for identifying compounds having desired characteristics from a combinatorial library or a set of combinatorial libraries by the use of flow cytometry. Also invented is a method for encoding combinatorial libraries using fluorophore labeled beads.

Abstract: Linear substituted oligoalkyleneimine molecules and libraries of molecules are disclosed, as are their methods of synthesis and use in acceptor binding assays. Each molecule or chain of a library contains the same number of 2 to about 10 substituted alkyleneimine repeating units, whose substituents are reduced amino acid side chains bonded to the repeating units at a position alpha to the nitrogen atom, and the member chains of a library are present in equimolar amounts. The chains of a library contain one or more predetermined reduced amino acid side chain-substituted repeating units at one or more predetermined positions of the substituted oligoalkyleneimine chain. The library contains equimolar amounts of at least six different reduced amino acid side chain-substituted repeating units at one or more of the same predetermined positions of the substituted oligoalkyleneimine chain. Particularly preferred linear substituted oligoalkyleneimine molecules and libraries are linear substituted oligoethyleneimines.

Abstract: The use of biological screening purposes of a subset (library) of a large combinatorially accessible chemical universe increases the efficiency of the screening process only if the subset contains members representative of the total diversity of the universe. In order to insure inclusion in the subset of molecules representing the total diversity of the universe under consideration, valid molecular descriptors which quantitatively reflect the diversity of the molecules in the universe are required. A unique validation method is used to examine both a new three dimensional steric metric and some prior art metrics. With this method, the relative usefulness/validity of individual metrics can be ascertained from their application to randomly selected literature data sets.

Abstract: The invention provides a system and method for synthesizing chemicals onto supports in a parallel manner to produce a combinatorial collection of compounds. The system includes a plurality of middle plates, with each middle plate defining a plurality of reaction zones arranged in a two dimensional array. The reaction zones are adapted to receive a solid support, such as a sheet of membrane, and the middle plates are stackable on each other to form a three dimensional array of reaction zones. The system also includes a pair of end plates, where the middle plates are located between the end plates, and where the end plates include an array of fluid guides corresponding to the array of reaction zones, to allow for selective routing of reagents through the reaction zones.

Abstract: The present invention relates to coding combinatorial chemical libraries synthesized on a plurality of solid supports by attaching “tags” that comprise fluorine containing compounds in combinations and/or ratios. The tags can be decoded while attached to the solid support by fluorine nuclear magnetic resonance spectroscopy to follow the reaction history of individual beads, and to determine the particular member of the library that is attached on the bead.

Abstract: This instant invention is directed to a precooked pizza pop-up toaster product designed to be sold in the frozen state for consumers to heat in a conventional toaster, toaster oven or microwave oven. The product is provided with a sauce formulated to prolong the shelf life of the product and to minimize moisture migration to the crust.

Abstract: A method has been developed which utilizes functionalized optical fibers as a solid support for the assembly of combinatorial libraries of compounds. The optical fibers are used to direct light, heat or a combination thereof to the compounds tethered to the fibers surface. Utilizing the method of the instant invention reactions occurring by both photochemically and thermally allowed pathways are accessible. In a preferred embodiment of the invention, the optical fibers are used to screen the array by fluorescence spectroscopy of labeled target molecules which bind to the immobilized library compounds.

Abstract: The instant invention is directed to a method of making a library of compounds using a segmentable support material comprised of a particulate resin affixed to a porous laminar material.

Abstract: The present method provides for a method of conducting solid state NMR distance measurements between nuclei in compounds attached to a surface. In specific embodiments the measurements are made by rotational echo double resonance (REDOR). Other embodiments are directed to the use of the method wherein the distances measurements involve peptides.

Abstract: A chemical moiety is disclosed which comprises a chemical, biochemical, or biological substance attached to one or more electrochemiluminescent organometallic compounds. In a preferred embodiment of the invention the substance is attached to one or more ruthenium-containing or osmium-containing luminescent organometallic compounds. Methods are disclosed for detecting low concentrations of the chemical moiety using chemiluminescent, electrochemiluminescent, and photoluminescent means. Compounds are disclosed which are useful for labeling substances of interest with ruthenium-containing and osmium-containing labels or other electrochemiluminescent labels. These labeled substances are useful in methods provided for detecting and quantifying analytes of interest in binding assays and competitive binding assays. The labeled substances are of particular use in homogeneous binding assays.

Abstract: The present invention is directed to the use of a soluble polyvalent support for the preparation of combinatorial libraries of compounds. The resultant combinatorial libraries are useful in screening for biologically active moieties in the drug discovery process or in developing compounds with desired physical and chemical properties.

Abstract: A technique is disclosed for generating nonrandom combinatorial libraries on solid phase supports in which each of a set of predetermined species of test compounds is present on a predetermined number of solid phase supports, preferably on only one, and each solid phase support has only a single species of test compound. Each of the predetermined species of test compounds is prepared with absolute certainty because the technique does not employ any random division of the solid phase supports. Rather, the method is based on the stepwise division of a continuous solid phase support matrix prior to each synthetic step in which more than one type of subunit is added. Non-limiting examples of matrices of the solid phase supports include polypropylene membranes, polytetrafluoropropylene membranes and cotton thread. The combinatorial libraries made by the technique are also disclosed.

Abstract: The present invention provides a library of compounds, each comprised of a common aminobenzenedicarboxylic acid core structure (scaffold) that serves as a template for synthesizing approximately 10.sup.1 -10.sup.6 compounds which are analogs of the scaffold. The library is employed to study ligand binding by biological receptors, such as enzymes, G-protein coupled receptors and membrane channels. For example, certain individual compounds within the library selectively bind and inhibit the action of trypsin-like serine proteases. The present invention also relates to combinatorial synthetic methods for making such libraries of compounds. Additionally, the present invention relates to novel scaffold-modified solid supports, particularly scaffold-modified polymer resins and methods for preparing said resins.

Abstract: There is disclosed a structural alignment method making use of a double dynamic programming algorithm. A distance cut-off approximation is performed, and then .DELTA.N cut-off approximation is performed. An alignment is produced based on the results of the distance cut-off approximation and the .DELTA.N cut-off approximation. Subsequently, an .epsilon.-suboptimal region defined by the obtained approximate solution is determined. Further, double dynamic programing alignment on the full structural environment is performed for residue pairs within the .epsilon.-suboptimal region. The structural alignment method is simpler than conventional methods and can shorten computational time while maintaining high accuracy.

Abstract: A combinatorial chemistry bead that includes an electromagnetic spectral emitter that radiates a distinct electromagnetic code for each bead that uniquely identifies each bead, a terminal apparatus for receiving the electromagnetic code from each bead, and a method for performing combinatorial synthesis using a bead that transmits a distinct electromagnetic code. The invention includes a large number of spectrally narrowed light emitting mechanisms for generating distinct optical codes.

Abstract: Radiation-activated catalysts (RACs), autocatalytic reactions, and protective groups are employed to achieve a highly sensitive, high resolution, radiation directed combinatorial synthesis of pattern arrays of diverse polymers. When irradiated, RACs produce catalysts that can react with enhancers, such as those involved in autocatalytic reactions. The autocatalytic reactions produce at least one product that removes protecting groups from synthesis intermediates. This invention has a wide variety of applications and is particularly useful for the solid phase combinatorial synthesis of polymers.

Abstract: A method is disclosed for obtaining affinity ligands for isolating tissue-type plasminogen activator (tPA). Ligands binding tPA with high specificity at pH 7 and releasing tPA at pH 5 or lower are disclosed.