摘要:
Provided herein are retinoid X receptor alpha binders that specifically bind to an epitope of a retinoid X receptor alpha, wherein the epitope comprises a phosphorylated serine at position 56 or 70. Also provided herein are retinoid X receptor alpha/polo-like kinase 1 modulators that inhibit the interaction of a polo-like kinase 1 with a retinoid X receptor alpha comprising a phosphorylated serine at position 56 or 70.
摘要:
The current disclosure provides specific peptides, and derived ionization characteristics of the peptides from the estrogen receptor (ER), progesterone receptor (PR), and/or antigen Ki67 (Ki67) proteins that are particularly advantageous for quantifying the ER, PR, and/or Ki67 proteins directly in biological samples that have been fixed in formalin by the method of Selected Reaction Monitoring/Multiple Reaction Monitoring (SRM/MRM) mass spectrometry. Such biological samples are chemically preserved and fixed wherein the biological sample is selected from tissues and cells treated with formaldehyde containing agents/fixatives including formalin-fixed tissue/cells, formalin-fixed/paraffin embedded (FFPE) tissue/cells, FFPE tissue blocks and cells from those blocks, and tissue culture cells that have been formalin fixed and or paraffin embedded. A protein sample is prepared from a biological sample using the Liquid Tissue™ reagents and protocol, and the ER, PR, and/or Ki67 proteins are quantitated in the Liquid Tissue™ sample by the method of SRM/MRM mass spectrometry by quantitating in the protein sample at least one or more of the peptides described for one or more of the ER, PR, and/or Ki67 proteins. These peptides can be quantitated if they reside in a modified or in an unmodified form. An example of a modified form of an ER, PR, and/or Ki67 peptide is phosphorylation of a tyrosine, threonine, serine, and/or other amino acid residues within the peptide sequence.
摘要:
In one aspect, the invention relates to compounds useful as fluorescence assay probes, methods of making same, and methods of using same to assay ligand binding interactions with PXR. In various aspects, the invention pertains to compositions comprising a polypeptide comprising a pregnane X receptor polypeptide, or a ligand binding fragment polypeptide thereof; and a molecule comprising a BODIPY residue and a vinca alkaloid residue. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要:
The current invention discloses compositions of matter, protocols and methods of screening test compounds to identifying agonists and antagonists of the orphan nuclear receptor NR2F6 by measuring the ability of a test compound to occupy the active site of NR2F6, in the presence of a reference compound.
摘要:
The invention provides means of manipulating hematopoietic stem cell differentiation by modulation of levels of NR2F6 (EAR2). Provided are compositions of matter, protocols and methods of use by which inhibiting expression of NR2F6 or activity thereof promotes differentiation of selective hematopoietic lineages, or conversely overexpression of NR2F6 or activity thereof inhibits differentiation. In one embodiment inhibition of differentiation is performed in other cell lineages besides hematopoietic.
摘要:
The current invention discloses compositions of matter, protocols and methods of use of treatment for cancer and other diseases of aberrant cellular proliferation and differentiation by inhibiting expression of NR2F2 or activity thereof. In one embodiment, administration of synthetic oligonucleotides that induce RNA interference mediated degradation of the nuclear receptor NR2F2 in human or animal patients is performed at a sufficient concentration or frequency to achieve regression of tumor.
摘要:
The current invention discloses compositions of matter, protocols and methods of use of treatment for cancer and other diseases of aberrant cellular proliferation and differentiation by inhibiting expression of NR2F6 or activity thereof. In one embodiment, administration of synthetic oligonucleotides that induce RNA interference mediated degradation of the nuclear receptor NR2F6 in human or animal patients is performed at a sufficient concentration or frequency to achieve regression of tumor.
摘要:
The present invention relates to the field of medical treatments for diseases and disorders. More specifically, the present invention relates to the use of the lanthionine synthetase component C-like (LANCL) proteins as therapeutic targets for novel classes of anti-inflammatory, immune regulatory and antidiabetic drugs. This includes but it is not limited to abscisic acid (ABA), ABA analogs, benzimidazophenyls, repurposed drugs or drug combinations, including thiazolidinediones (TZDs); naturally occurring compounds such as conjugated diene fatty acids, conjugated triene fatty acids, isoprenoids, and natural and synthetic agonists of peroxisome proliferator-activated receptors that activate this receptor through an alternative mechanism of action involving LANCL2 or other membrane proteins to treat or prevent the common inflammatory pathogenesis underlying type 2 diabetes, atherosclerosis, cancer, some inflammatory infectious diseases such as influenza and autoimmune diseases including but not limited to inflammatory bowel disease (Crohn's disease and Ulcerative colitis), rheumatoid arthritis, multiple sclerosis and type 1 diabetes and other chronic inflammatory conditions.
摘要:
The application provides methods of modulating NR2F6 in a cell or animal in need thereof by administering an effective amount of a NR2F6 modulator.
摘要:
The present invention relates to methods for identifying susceptibility of impaired hepatic wound healing in a patient, most particularly by identifying modifications of the of PPAR-γ and TGFβ1 genes. It further relates to stratifying populations of patients to determine susceptibility to impaired hepatic wound healing and direct appropriate healthcare resources. More specifically methods can be used to stratify liver disease patient populations to identify those most likely to progress to cirrhosis, or to identify the likelihood that a patient with liver disease will progress to having cirrhosis.