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Renal Selective Unsaturated Englerin Analogues

Researchers at the National Cancer Institute (NCI) have developed a number of analogs of the natural product englerin A, an inhibitor of renal cancer cell growth. Englerin A is thought to exert its anticancer effects by activating protein kinase C (PKC) theta, and exert cytotoxic effects through activation of transient receptor potential cation (TRPC) channels. The invention englerin analogues provide promising treatment strategies for various cancers, diabetes, and HIV, and other diseases associated with the PKC theta and/or TRPC ion channel proteins. Researchers at the NCI seek licensing and/or co-development research collaborations for englerin A analogue compounds.

siRNA Delivery Using Hexameric Tetrahedral RNA Nanostructures for Gene Silencing

Researchers at the National Cancer Institute (NCI), in collaboration with researchers at the University of California, Santa Barbara (UCSB), developed a tetrahedral-shaped RNA nanoparticle for the delivery of siRNA to activate RNAi. The tetrahedral RNA nanoparticles can contain twelve Dicer substrate RNA duplexes for gene silencing. The NCI seeks parties interested in co-development or licensing of these tetrahedral RNA nanoparticles.

Dopamine D3 Receptor Agonist Compounds, Methods of Preparation, Intermediates Thereof, and their Methods of Use

Scientists at the National Institute on Drug Abuse (NIDA) have developed novel dopamine D3 receptor (D3R) agonists with high affinity and selectivity. Two lead compounds, 53 and eutomer 53a, have demonstrated significantly higher D3R binding selectivity than reference compounds. Moreover, 53 and 53a showed metabolic stability in liver microsomes, which is favorable for the future use of these compounds as therapeutic agents for diseases related to dopamine system dysregulation such as Parkinson’s Disease and Restless Legs Syndrome. Researchers at NIDA seek licensing and/or co-development research collaborations for the use of these D3R agonists as molecular tools for the study of D3R physiology and as potential therapeutics to treat neurological and neuropsychiatric disorders.

Chimeric Antigen Receptors that Recognize Mesothelin for Cancer Immunotherapy

Researchers at the NCI have developed chimeric antigen receptors (CARs) with a high affinity for mesothelin to be used as an immunotherapy to treat pancreatic cancer, ovarian cancer, and mesothelioma. Cells that express CARs, most notably T cells, are highly reactive against their specific tumor antigen in an MHC-unrestricted manner to generate an immune response that promotes robust tumor cell elimination when infused into cancer patients.

RNA/DNA Nanoparticles as Cancer Therapeutics

The technology is directed to the use of single-stranded RNA overhangs or toeholds of varying lengths (< 12 nucleotides) contained in nucleic acid-based nanoparticles which trigger the association of these nanoparticles and activates multiple functionalities such as gene silencing and/or cell-specific targeting. The use of RNA toeholds is superior to that of DNA toeholds in that it allows for smaller nanoparticles (fewer nucleotides for the toeholds) resulting in greater chemical stability, less immunogenic and higher yield of production. The National Cancer Institute (NCI) seeks licensing and/or co-development research collaborations for use of RNA overhangs or toeholds in nucleic acid nanoparticles.

Nanoparticle-hydrogel Composite for Nucleic Acid Molecule Delivery

The National Cancer Institute (NCI) seeks research a co-development partner and/or licensees for applications utilizing the nanoparticle platform technology for delivery of cancer-specific microRNAs, particularly for therapeutic uses in surface cancers, such as mesothelioma.

Anti-Viral Compounds that Inhibit HIV Activity

The National Cancer Institute (NCI) Molecular Targets Laboratory is seeking parties interested in collaborative research to co-develop antiviral tropolone derivatives developed by systematic medicinal chemistry on the lead series.

Margaric Acid Decreases PIEZO2 Mediated Pain

Investigators at the National Center for Complimentary and Integrative Health (NCCIH) and the University of Tennessee Health and Science Center have shown that administration of margaric acid can ameliorate pain induced by a variety of noxious stimuli in mice. In vitro and ex vivo studies in human and murine neural cells indicate that the mechanism of action of margaric acid is mediated by PIEZO2 (Piezo-type mechanosensitive ion channel component 2) function. NCCIH seeks research co-development partners and/or licensees for methods of using the fatty acid, margaric acid to treat pain.

Fusion Proteins as HIV-1 Entry Inhibitors

Novel fusion proteins with good stability and potency against HIV-1. These fusion proteins have good drug properties and potential as prophylactics or therapeutics against HIV-1 infection. Researchers at the NCI seek licensing for the development and commercialization of novel fusion proteins as therapeutics or prophylactics against HIV-1 infection.

Immunogenic Antigen Selective Cancer Immunotherapy

Researchers at the National Institute on Aging working on cancer immunotherapy and detection report the use of SPANX-B polypeptides in the treatment and identification of cancer. Specific human malignancies targeted for the treatments disclosed include melanoma and lung, colon, renal, ovarian and breast carcinomas. The NIA seeks parties interested in licensing or collaborative research to further develop, evaluate, or commercialize SPANX-B polypeptides in the treatment and identification of cancer.

Antibody and Immunotoxin Treatments for Mesothelin-expressing Cancers

The National Cancer Institute Laboratory of Molecular Biology is seeking statements of capability or interest from parties interested in licensing or collaborative research to further develop, evaluate, or commercialize antibody-based treatments of mesothelin-expressing cancers.

Use of Interleukin (IL)-34 to Treat Retinal Inflammation and Neurodegeneration

Researchers at the National Eye Institute have developed a new cytokine therapy that delivers functional interleukin 34 (IL-34) to the retina for treating ocular inflammatory diseases – such as uveitis and degenerative retinal diseases. Intraocular delivery of IL-34 protein or IL-34 gene expression system can effectively prevent retinal inflammation. Thus, it may be a promising strategy to produce long-lasting effects in suppressing abnormal retinal inflammation and preventing photoreceptor death.

Reprogrammed Tumor Infiltrated Lymphocytes for Efficient Identification of Tumor-Antigen Specific T-Cell Receptors

Adoptive T Cell Therapy (ACT) has proven to effectively treat established tumors. This treatment consists of harvesting Tumor Infiltrated Lymphocytes (TIL) which specifically recognize cancer, expanding the tumor-specific TIL in vitro, and then reinfusing these cells into the patient for treatment. Both these lymphocytes and their T cell receptors (TCR) are valuable for cancer immunotherapy. Inventors from the National Cancer Institute (NCI) have developed an improved method to identify tumor-specific TCRs by reprogramming TIL into stem cells. This invention is available to license further development.

Small Molecule Inhibitors of Drug Resistant Forms of HIV-1 Integrase

Researchers at the National Cancer Institute discovered small-molecule compounds whose activity against HIV-1 integrase mutants confer greater resistance than currently approved INSTIs. Preliminary DMPK and ADME studies have been completed by the NCI researchers. The National Cancer Institute seeks partners to commercialize this class of compounds through licensing or co-development.

Peptide Mimetic Ligands of Polo-like Kinase 1 Polo Box Domain

Researchers at the National Cancer Institute (NCI) have developed peptidomimetic inhibitors that disrupt Polo-like kinase 1 (Plk1)-mediated protein interactions by targeting polo-box domain (PBD). The compounds are designed to selectively cause mitotic arrest in cancer cells with abnormal Plk1 expression. Researchers seek licensing and/or co-development research collaborations to further develop the inhibitors.

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