Abstract: This invention relates to compounds of the general formula: 1

Abstract: The invention relates to compounds of the general formula (and pharmaceutically acceptable derivatives thereof): in which RA, RB, RC, RD, R5, R7, R9, R9a, AK, p, q, r and X are as defined herein, and to their preparation and use.

Abstract: This invention relates to compounds of the general formula: in which RA, RB, RC and RD are as defined herein, and to their preparation and use.

Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediate by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutic compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of formula (1) as defined herein.

Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of the formula as defined herein.

Abstract: This invention relates to compounds of the general formula: 1

Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of the formula as defined herein.

Abstract: Compounds and methods of treating or preventing bone disorders including osteoporosis, rheumatoid arthritis, and metastatic bone disease are provided. The inventive compounds comprise a bone targeting moiety and a payload. The payload portion of these inventive compounds inhibit the proton pump of osteoclasts, thereby, reducing bone resorption.

Abstract: The present invention provides methods and compositions for identifying inhibitors of the interaction between phosphopeptide binding pairs, i.e., a protein domain having at least one phosphopeptide binding domain and the phosphorylated ligands that bind these domains. These inhibitors may be used for pharmaceutical compositions and in therapeutic treatments for diseases in which a phosphopeptide domain binding is implicated.

Abstract: This invention concerns derivatives of rapamycin and their antifungal uses. Also disclosed are materials and methods relevant to the identification of non-immunosuppressive antifungal rapamycin derivatives.

Abstract: The invention relates to human ZAP-70, and in particular, to the region of ZAP-70 containing the tandem Src homology-2 (“SH2”) domains, to crystalline forms thereof, liganded or unliganded, which are particularly useful for the determination of the three-dimensional structure of the protein. The three dimensional structure of the tandem SH2 region of ZAP provides information useful for the design of pharmaceutical compositions which inhibit the biological function of ZAP and other members of the ZAP family of SH2 domain-containing proteins, particularly those biological functions mediated by molecular interactions involving one or both SH2 domains.

Abstract: An in vitro assay method permits the identification of a test substance which inhibits the mutual association of two molecules. The method includes the steps of providing two components capable of mutual association, one of said components bearing a covalently linked fluorophore; preparing a mixture containing the two components and at least one test substance; irradiating the mixture with polarized light of a suitable wavelength permitting excitation of the fluorophore as indicated by emission of polarized light; measuring the degree of polarization of the emission, and determining the effect of the presence or concentration of the test substance in decreasing the observed emission polarization of a mixture of the two components alone. Inhibitory activity of the test substance correlates with decreased depolarization values.

Abstract: Materials and methods are disclosed for regulation of biological events such as target gene transcription and growth, proliferation or differentiation of engineered cells.

Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains.

Abstract: The present invention relates to the discovery of novel proteins of mammalian origin which are immediate downstream targets for FKBP/rapamycin complexes.

Abstract: The present invention relates to the discovery of novel proteins of mammalian origin which are immediate downstream targets for FKBP/rapamycin complexes.

Abstract: The present invention relates to chimeric transcriptional activators.

Abstract: The molecular cloning of humansyk DNA, compositions containing same and uses thereof are disclosed.

Abstract: This invention relates to compounds of formula: ##STR1## and pharmaceutically acceptable salts thereof, where A is H, R.sup.1, --CO--R.sup.1 or --CO--OR.sup.1 where R.sup.1 is a substituted or unsubstituted alkyl, heteroalkyl, aryl or heteroaryl group and J is H or NO.sub.2. L-forms of the compounds are currently preferred, although D-forms and racemic mixtures are also encompassed by this invention.

Abstract: Novel compounds related structurally to Brefeldin A useful as antiviral, antifungal, antiproliferative, immunosuppresive and detoxifying agents as well as pharmaceutical compositions and methods based thereon are disclosed.