Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.

Abstract: An inhibitory compound having the structure: Group I-Group II. Group I has the structure: where H represents a hydrogen; C represents a carbon; O represents an oxygen; N represents a nitrogen; each R, independently, is chosen from the group consisting of the R groups of an amino acid, including proline; each broken line, independently, represents a bond to an H or a bond to one R group, and each H′ represents that bond or a hydrogen; and p is an integer between 0 and 4 inclusive. Alternatively Group I has the structure: where n is between 0 and 3 inclusive, each G2 and G3 independently is H or C1-3 (one to three carbon atoms) alkyl, G1 is NH3 (H3 represents three hydrogens), (H2 represents two hydrogens), or where G5 and G6 can be NH, H, or C1-3 alkyl or alkenyl with one or more carbons substituted with a nitrogen. G1 bears a charge, and G1 and Group II do not form a covalently bonded ring structure at pH 7.0.

Abstract: The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. In particularly preferred embodiments, these compounds are attached to the solid support through a covalent interaction.

Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I), and methods for the synthesis thereof. In another aspect, the present invention provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. In yet another aspect, the present invention provides methods for treating cancer comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof.

Abstract: The present invention provides compositions and methods for promoting wound healing. The composition comprises virgin monomers of tropoelastin and lysyl oxidase. When the lysyl oxidase comes in contact with the tropoelastin, cross-linking of the tropoelastin monomers will occur to form elastin. Contacting the tropoelastin and lysyl oxidase together and applying the mixture to a wound before substantial cross-linking has occurred promotes wound healing by holding the damaged tissue together, increasing the rate of healing, and decreasing the amount of scarring.

Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.

Abstract: A method for stimulating proliferation of T-cells containing cytoplasmic post-prolyl dipeptidase activity; the method, in one aspect, involves contacting the T-cells with an organic compound at a concentration below 10−8M, wherein the compound is characterized in that: (a) it is capable of crossing the membrane of T-cells to enter the cytoplasm, (b) it binds to the dipeptidase activity at a concentration of below 10−8M, and thus (c) stimulates proliferation of the T-cells at that concentration.

Abstract: The present invention provides improved cell delivery compositions. In particular, the invention provides biocompatible endosomolytic agents. In a preferred embodiment, the endosomolytic agents are also biodegradable and can be broken down within cells into components that the cells can either reuse or dispose of. Preferred endosomolytic agents include cationic polymers, particularly those comprised of biomolecules, such as histidine, polyhistidine, polylysine or any combination thereof. Other exemplary endosomolytic agents include, but are not limited to, other imidazole containing compounds such as vinylimidazole and histamine. More particularly preferred are those agents having multiple proton acceptor sites and acting as a “proton sponge”, disrupting the endosome by osmolytic action. In preferred embodiments, the endosomolytic agent comprises a plurality of proton acceptor sites having pKas within the range of 4 to 7, which endosomal lysing component is polycationic at pH 4.

Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.

Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.

Abstract: The present invention provides assays for identifying compounds that affect the transcriptional activity of a protein of interest or affect the stability of the protein of interest. The triple readout assay system which can be used to identify compounds that affect the transcriptional activity of a protein of interest uses three cell lines to control for non-specific effects such as sequences flanking the inserted gene and cytotoxicity. The double readout assay system assesses protein stability and uses a fusion protein of a reporter and the protein of interest. These assay systems may be particularly useful in identifying compounds that affect transcription factors and tumor suppressors. In a particular embodiment, the tumor suppressor p53 is the target protein being studied.

Abstract: A hair treatment composition including a non naturally-occurring keratin protein in combination with a hair treatment formula is described. The protein is preferably of human origin and has not been previously cross-linked. The protein is most preferably selected from the group of soluble keratin proteins found in human hair. Preferably, the composition contains one, preferably at least two allelic variants of the protein, most preferably in substantially the same ratio at which they are found in hair of a selected individual. The individual may be selected, for example, on the basis of having appealing hair, of being the future user of the hair treatment composition of other reasons.

Abstract: Novel compounds that are anti-angiogenic or immunosuppressive are described. Also described are methods for determining if an animal is at risk for a disease involving abnormal angiogenesis or an immune reaction resulting in pathology comprising evaluating an aspect of MetAP2 metabolism or structure; methods for identifying agents that are anti-angiogenic or immunosuppressive comprising evaluating the effect of the agent on an aspect of MetAP2 metabolism; methods for treating a cell having an abnormality in metabolism or structure of MetAP2; and methods for treating abnormal angiogenesis or an immune reaction which results in pathology in an animal. Pharmaceutical compositions are also provided.

Abstract: The present invention provides a system for analyzing polymer molecules by detecting their effects on an optical agent. Certain preferred embodiments of the invention involve the analysis of polynucleotide molecules through detection of their quenching effects on a fluorescent reporter.

Abstract: A method for increasing immune responses of a human patient infected with HIV, involving contacting the T-cells, in vitro or in vivo, with an organic compound at a concentration effective to cause T-cell proliferation, but below an amount that causes detectable cytotoxicity.