54 results about "Nuclear transport" patented technology

The present invention relates to internalizing peptides which facilitate the uptake and transport of cargo into the cytoplasm and nuclei of cells as well as methods for the identification of the peptides, and methods of use for the peptides. The internalizing peptides of the present invention are selected for their ability to efficiently internalize cargo into a wide variety of cell types both in vivo and in vitro.

The present invention relates to internalizing peptides which facilitate the uptake and transport of cargo into the cytoplasm and nuclei of cells as well as methods for the identification of such peptides. The internalizing peptides of the present invention are selected for their ability to efficiently internalize cargo into a wide variety of cell types both in vivo and in vitro. The method for identification of the internalizing peptides of the present invention comprises incubating a target cell with a peptide display library, isolating peptides with internalization characteristics and determining the ability of said peptide to internalize cargo into a cell.

The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).

The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).

The present invention relates to compounds of formula I:

and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.

The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I:

or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.

The invention provides methods of determining the presence of a nuclear localization signal and/or the presence of a nuclear export signal in a protein of interest. The invention further provides chimeric nucleic acids and recombinant host cells for use in such methods. Additionally provided is a nucleic acid molecule encoding a modified LexA protein, wherein the modified LexA protein has no nuclear localization signal, as well as the modified LexA protein itself. In the nuclear import assay, if a protein of interest fused to a mLexA-Gal4AD hybrid contains a functional NLS, the fusion product will enter the yeast cell nucleus and activate the expression of reporter genes. In the nuclear export assay, if a protein of interest fused to a mLexA-SV40 NLS-Gal4AD hybrid contains a functional NES, the fusion product localized to the cell nucleus will exit into the cytoplasm, decreasing the reporter gene expression levels.

The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I or their pharmaceutically acceptable salts, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.

The present invention relates to compositions and methods for treating diseases associated with dyslipidemia, including hypercholesterolemia, hypertriglyceridemia, steatohepatitis, atherosclerosis, obesity, hyperglycemia, metabolic syndrome, and related aspects of and conditions associated with metabolic syndrome. The compositions and methods disclosed herein are useful for regulating the lipid balance (lipid homeostasis) in a subject. Compositions and methods including a Nuclear Transport Modifier may be administered to a subject to modulate the transport of transcription factors, mediated by nuclear import adaptors, into the nucleus of a cell resulting in a decrease in cholesterol and triglyceride levels in the blood and liver, a decrease in atherosclerotic lesion size, a decrease in body weight and in hyperglycemia, a reduction of fatty liver inflammation, and an improvement in liver function.

The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula (I) or their pharmaceutically acceptable salts, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.

The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula (I) or their pharmaceutically acceptable salts, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.

The present invention relates to a transport agent for transporting nucleic acids into eukaryotic cells and a method for producing said agent. The invention further concerns methods for transporting nucleic acids into eukaryotic cells using the transport agent according to the invention. The present invention provides an alternative transport agent and a method which are effective to allow an efficient transport of nucleic acids into eukaryotic cells. The transport agent comprises a complex forming moiety that is capable of forming complexes with at least one nucleic acid molecule and condensing said nucleic acid molecule, and at least one nuclear localization moiety comprising at least one nuclear localization signal and having an approximately neutral net charge.

A method of identifying a lead or candidate compound that modulates the activity of GTPase-Activating Protein SH3 Domain-Binding Proteins (G3BP) is provided, which includes determining whether a compound modulates the interaction between the N-terminal Nuclear Transport Factor 2-like (NTF2L) domain of G3BP and FGDF peptide of ubiquitin specific protease 10 (USP10) or non-structural protein 3 (nsP3).

The invention discloses a five-membered nitrogen azole heterocyclic derivative, and discloses a preparation method and an application thereof. The invention belongs to the technical field of medicines, and provides a five-membered nitrogen azole heterocyclic derivative which reduces the cytotoxicity of a compound and improves the cell viability, oral absorption rate and bioavailability of a medicine. The compound provided by the invention has the advantages of low cytotoxicity, good cell viability, high oral absorbability and good bioavailability. In addition, a second object of the invention is to provide the compounds and pharmaceutically acceptable salts and compositions thereof that are also useful for the treatment of a variety of diseases, disorders or conditions associated with abnormal cell responses triggered by improper nuclear transport. The compounds provided by the invention are also useful for the study of nuclear transport modulation in biological and pathological phenomena, such as the study of kinase-mediated intracellular signal transduction pathways and the comparative evaluation of new nuclear transport modulators.