Abstract: Razors and components thereof are provided, as well as methods of making such.

Abstract: The present invention relates to glycosyl-etoposide prodrugs, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates for treating cancers.

Abstract: Methods for treating or preventing gastritis or gastric injury are disclosed, comprising administering a therapeutically effective amount of an amylin or an amylin agonist. Methods are also disclosed for the treatment of pain, fever, inflammation, arthritis, hypercoagulability, or other conditions for which a non-steroidal anti-inflammatory drug would be indicated, comprising administering an amylin or amylin agonist in conjunction with administering a therapeutically effective amount of a non-steroidal anti-inflammatory agent. Pharmaceutical compositions comprising an amylin or amylin agonist and a non-steroidal anti-inflammatory drug are also disclosed.

Abstract: The present invention relates to novel methods of producing proteins in which one or more domains are full length and correctly folded and which are each tagged at either the N- or C-terminus with one or more marker moieties and arrays containing such proteins, as well as the use of such proteins in arrays for rapid screening.

Abstract: The present invention provides a method for screening of a large number of compounds for their ability to modulate the expression of genes. The method uses gene trap technology and comprises the steps of transfecting a population of cells with a gene-trap vector, sorting cells according to their level of fluorescence, distributing sorted cells into pools and expanding the pools to obtain a sufficient number of cells representing each trapped gene to permit distinction of the effect of a test compound over controls, exposing the cells to the test compounds and identifying compounds which alter the fluorescence distribution pattern of cells using FACS analysis.

Abstract: The invention provides four butyrylcholinesterase variants having increased cocaine hydrolysis activity as well as the corresponding encoding nucleic acids. The invention also provides libraries comprising butyrylcholinesterase variants having at least one amino acid alteration in one or more regions of butyrylcholinesterase and further having at least one butyrylcholinesterase variant exhibiting enhanced cocaine hydrolysis activity compared to butyrylcholinesterase. The invention further provides methods of hydrolyzing a cocaine-based butyrylcholinesterase substrate as well as methods of treating a cocaine-induced condition.

Abstract: A method to enhance the cytotoxic activity of an antineoplastic drug comprising administering an effective amount of the antineoplastic drug to a host exhibiting abnormal cell proliferation in combination with an effective cytotoxicity-increasing amount of an antioxidant. The invention also includes a method to decrease the toxicity to an antineoplastic agent or increase the therapeutic index of an antineoplastic agent administered for the treatment of a solid growth of abnormally proliferating cells, comprising administering an antioxidant prior to, with, or following the antineoplastic treatment.

Abstract: The invention involves identification of a mechanism of ?-amyloid peptide cytotoxicity, which enables treatment of conditions caused by ?-amyloid peptide aggregates by administration of compounds which antagonize the mechanism of cytotoxicity. The invention includes the identification and isolation of compounds which can reduce the neurotoxic effects of such aggregates. Methods for treating conditions resulting from neurotoxic ?-amyloid peptide aggregates, such as Alzheimer's disease and pharmaceutical preparations are provided. Also provided are methods for selecting additional compounds which can reduce the neurotoxic effects of ?-amyloid aggregates.

Abstract: The present invention relates to the death protease CPP32 in crystallized form and a method for the preparation thereof. The invention further provides a three-dimensional model of CPP32 and improved means for the design of CPP32 modulators.

Abstract: A sublancin peptide variant (lantibody) having a spacer region and a subtilin leader peptide fused to the C-terminal end of the mature sublancin peptide provide an anchoring means for inserting and retaining the lantibody in a host cell wall without affecting the intracellular processing of the lantibody, host cell expression of the molecule on the cell surface or the biological activity of the mature sublancin peptide in extracellular, cell-wall-bound form. Target molecules that bind to the antibody and methods of engineering a peptide variant gene, plasmid and a host cell transformant are described as are methods for generating a lantibody display library and identifying new target molecules.

Abstract: The present invention provides a highly sensitive screening assay for the identification of peptide binding partners to virtually any peptide or polypeptide ligand. Utilizing an expression-repression readout system, the inventors have screened libraries of peptides and identified relatively small peptide molecules that bind to the provided target.

Abstract: Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed: wherein A, B, X, R1, and R5 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents as well as inhibitors of central nervous disorders. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.

Abstract: The present invention provides methods of utilizing a complex carbohydrate library which includes a plurality of complex carbohydrate structures each being attached to a specific site of a solid support such as a platform for screening and isolating complex carbohydrate structures capable of specifically and uniquely binding with an entity such as a polypeptide.

Abstract: Mixtures of chemical compounds are provided having antibacterial and other utility. The mixtures are formed, preferably in solution phase, from the reaction of a purine or pyrimiding heterocyclic scaffold with a set of related chemical substituients, optionally through employment of a tether moiety. Libraries formed in accordance with the invention have utility per se and are articles of commerce. They can be used to screen for pesticides, drugs and other biologically active compounds.

Abstract: Pharmaceutical preparation containing an effective amount of acetylsalicylic acid and a compound of Formula I. A1—A2—NH—(CH2)n—B wherein A1, A2, n and B are as defined in the specification, which is either the compound as such, or a stereoisomer thereof, and which may be in the form of a physiologically acceptable salt, in association with a pharmaceutical carrier. The combinations are suitable for use in inhibiting thrombin, or in the treatment or prophylaxis of thrombosis or hypercoagulability in patients in need thereof.

Abstract: The present invention provides compounds and methods of identifying and designing compounds which inhibit activity of inward-rectifier K+ channels. In particular, compounds having a tertiapin-like ? helix, such as a stable tertiapin derivative wherein the methionine residue in position 13 of tertiapin is replaced by glutamine, are described. Methods of using these compounds to control insulin secretion, and cardiac rhythm and electrical conduction, to modulate neurotransmissions of neurons, and to induce diuresis in mammals are also provided.

Abstract: Methods and materials for scintillation assays are disclosed. The scintillation assays rely on differences in general molecular property-based binding interactions, such as charge or hydrophobicity, to localize a radioactive substance near a scintillating material, stimulating scintillation. They are thus described as a direct adsorption scintillation assay (DASA) to distinguish them from the scintillation proximity assay (SPA). The assays are more convenient and inexpensive to implement than SPAs, which rely on specific binding of ligand-receptor pairs, antibody-antigen pairs, or other binding partners which rely on the precise and specific structural complementarity of the partners. The assays can be employed for studying enzymatic reactions, such as those involved in the synthesis of Mur-pentapeptide. The assays are readily adaptable to high throughput screening for use in conjunction with combinatorial libraries of compounds.

Abstract: The present invention provides a complex carbohydrate library which includes a plurality of complex carbohydrate structures each being attached to a specific site of a solid support such as a platform, thereby making each of the plurality of complex carbohydrate structures uniquely addressable. The addressable nature of the complex carbohydrate library of the present invention makes it particularly suitable for screening and isolating molecules that bind specifically and uniquely to complex carbohydrate structures associated with various disorders and conditions, thus enabling identification of new drugs candidates.

Abstract: Pharmaceutically acceptable compounds for administering to a subject, comprising the general structure II: wherein R1 is an L-amino acid or salt or ester thereof, or an L-amino acid containing peptide or salt or ester thereof; and wherein the stereochemistry about the carbon-carbon double bond is trans. The invention further relates to pharmaceutical compositions comprising the aforementioned compounds.

Abstract: Topical compositions which include urea and carbamide peroxide are described. Compositions having a pH in the acidic range, particularly in the range of about 2.5 to about 9 are also described. Methods for treating dermatological disorders using the composition are also described.