Friday, April 09, 2021 3:22:15 PM
From there site. https://www.regenbiopharmainc.com/products.html
Small Molecules Targeting Cancer and Autoimmunity
Regen has identified and filed patents on small molecules that activate and inhibit a novel gene (NR2F6) which controls
how the immune system reacts to cancer cells and to inflammatory responses.
Objective is to identify small molecules that can activate and inhibit NR2F6
?Currently in pre-clinical development
Initial indications (inhibitor): bladder cancer, myelodysplastic syndrome, lung cancer
Initial indications (activator): rheumatoid arthritis, inflammatory bowel disease, psoriasis
Additional indications include solid tumors, acute leukemia and GVHD
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Googles page https://patents.google.com/patent/US9091696B2/en
PDF of patent https://patentimages.storage.googleapis.com/c1/c4/8e/b433df0914cc1f/US9091696.pdf
Modulation of NR2F6 and methods and uses thereof.
The invention claimed is:
1. A method for identifying compounds that can modulate the function of NR2F6 in mammalian cells comprising the steps of:
(i) selecting a cancer (a) cell line or (b) cell-free lysate to use;
(ii) expressing in the cancer cell-line or cell-free lysate proteins encoded by one or more recombinant DNA vectors that comprise a reporter assay system, having a portion of the gene with SEQ ID NO:1 that has been predetermined to control the transcriptional activity of the gene NR2F6 and that encodes for expression of an amino acid sequence of at least 75% sequence identity to a portion of the amino acid sequence of SEQ ID NO: 2;
(iii) contacting the cancer cell-line or or cell-free lysate with a candidate compound;
(iv) measuring the ability of the candidate compound to inhibit or stimulate said reporter assay system; and
(v) comparing the measurement of the ability of the candidate compound to inhibit or stimulate said reporter assay system with a suitable control so as to determine whether said inhibition or stimulation of said reporter assay system is indicative of a compound for modulating the function of NR2F6 in a mammal.
2. The method of claim 1 wherein HeLa cells are used for the cancer (a) cell-line or (b) cell-free lysate.
3. The method of claim 1, wherein the method is a high-throughput screening.
4. The method of claim 1, wherein the portion of the nucleotide that encodes for expression of an amino acid sequence of at least 75% sequence identity of the amino acid sequence of SEQ ID NO: 2 is the ligand binding domain of NR2F6.
5. The method of claim 1, wherein the reporter assay system measures the ability of the candidate compound to cause a conformational change in the ligand binding domain of NR2F6.
6. The method of claim 1, wherein the reporter assay system measures the compound's ability to modulate the ability of NR2F6 to repress or activate transcription.
7. The method of claim 1 wherein a cell based assay is used in which the host cell contains an expression vector, said expression vector comprising a polynucleotide, said polynucleotide comprising a nucleotide sequence encoding a polypeptide comprising the amino acid sequence of SEQ ID NO: 2.
8. The method of claim 1 wherein a cell based assay using cultured mammalian cells transfected with a vector encoding for a protein with amino acid sequence of SEQ ID NO: 2 and a reporter construct, where the cells are treated with candidate compounds and assessed for the activity of the reporter construct.
9. The method of claim 1 wherein the reporter assay system consists of at least one or more DNA vectors, one of which contains a DNA binding site positioned adjacent to an expressible reporter element; another contains a chimeric transactivatable vector comprising nucleotides that encode for a portion of the NR2F6 gene and a DNA binding domain that specifically binds to the DNA binding site.
10. The method of claim 9 wherein the DNA binding site further comprises a GAL4 binding element.
11. The method of claim 9 wherein the expressible reporter element is luciferase.
12. A method of claim 9 wherein the DNA binding domain that specifically binds to the DNA binding site consists of multiple Gal4 Upstream Activator Sequences.
MY2BITS
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