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A Novel ER Beta Ligand Prodrug to Treat MS and Other Neurodegenerative Diseases

Researchers from the Department of Neurology and the Department of Chemistry and Biochemistry at UCLA have developed a novel ERβ ligand prodrug that is structurally designed to more easily cross the blood-brain barrier for treatment of multiple sclerosis.

Inhibitors Of The N-Terminal Domain Of The Androgen Receptor

UCLA researchers under the guidance of Drs. Matthew Rettig and Mike Jung have developed a novel family of therapeutics for use against castration resistant prostate cancer. These drugs have been shown to inhibit the androgen receptor and are unaffected by the most common drug-resistant mutations found in prostate cancer patients.

A Novel Method to Generate Specific and Permanent Macromolecular Covalent Inhibitors

UCSF researchers have invented a novel method to generate covalent macromolecular inhibitors. This strategy allows a peptide inhibitor to bind to its target protein specifically and irreversibly through proximity-enabled bioreactivity.

Protein Kinase C Epsilon Small Molecule Inhibitors to Treat Pain, Anxiety, Alcoholism, and Nicotine Addiction

This invention provides new inhibitors to protein kinase C epsilon (PKCε) for the treatment and prophylaxis of various diseases such as pain, anxiety, alcoholism, inflammation, cancer, diabetes, and other conditions.

Antisense Oligonucleotides and Drug Conjugates for Obesity and Diabetes Treatment

The obesity epidemic is an ongoing issue leading to significant economic and social burden, in part due to its role in the development of diabetes. Only three DFA-approved drugs for obesity treatment currently exist, none of which are without significant side effects and risks. Researchers at UCI have developed a DNA-based approach that activates metabolism, to target genes only in the fat and liver, causing increased energy expenditure and weight loss without affecting other organs. These present a viable approach to obesity treatment with minimal side effects in comparison to current drug treatments.

Methods for purifying and treating wounds with a proprietary biological agent, and to coat biomaterials designed to be synthetic substrates, aimed at promoting healing.

This invention describes methods for using a proprietary biological agent to improve the quality and speed of wound healing, and for coating a biomaterial to serve as an artificial epithelium for severe wounds. Also described are methods to produce high yields of the biological agent and of its purification.

Novel Antiviral Compounds to Treat Enterovirus Infections

Researchers in UCLA Department of Molecular & Medical Pharmacology have used a rapid, live virus assay to develop potent enterovirus inhibitors.

Compositions for Enhancing Beta Cell Maturation, Health, and Function

Beta cell failure is the central cause of type-2 diabetes. Researchers at UCI have developed molecules for treating diabetes that target proteins on the surface of beta cells and induce their clustering. This clustering results in an increase in insulin secretion and content and promotion of beta cell maturation. Furthermore, the clustering effect seen with these compositions may promote both proliferation and the reversal of de-differentiation.

PharmaCoLogic: Preclinical Cardiac Drug Screening

Researchers at the University of California, Davis have developed PharmaCoLogic: a computer based preclinical screening model to predict the effects of developmental drugs and drug induced cardiotoxicity.

Treatment To Prevent Post-Antibiotic Expansion Of Enterobacteriaceae

Researchers at the University of California, Davis have identified a nuclear receptor as a new target for treatments preventing post-antibiotic Enterobacteriaceae expansion.

Siderophore-Based Immunization Against Gram-Negative Bacteria

Bacterial pathogens such as E. coli and Salmonella hijack the host’s iron to cause infection. This invention describes an immunization strategy for triggering an immune response against the iron-sequestering agent secreted by the pathogen, thus turning the bacterial virulence mechanism against itself, and thereby resulting in host immunity.

Novel therapeutic approach for obesity: Pharmacological targeting of Kv1 potassium channels

Obesity is a global epidemic that is in need of novel and safe therapeutics. Despite the enormous efforts by pharmaceutical companies, there is a shortage for safe therapeutics for obesity. Researchers at UCI have developed a selective inhibitor of Kv1.3 potassium channel, ShK-186, which displays powerful anti-obesity effects in a mouse model of diet-induced obesity. Using critical experimental measures, researchers highlight the potential use of Kv1.3 blockers in the treatment of obesity and insulin resistance.

Thrombospondins as a target to treat neuropathic pain

Neuropathic pain is a common problem, though, there are few existing pain medications have specific targets to treat this type of pain, and often lack efficacy and tolerance. The invention identifies specific proteins and related genes as targets for treating neuropathic pain in an animal model.

Stimuli Responsive Immunostimulants

An immune response typically occurs during inflammation, auto-immune diseases, or cancers. In such cases, chemical triggers, or immunostimulants, recognized by receptor proteins at cell membranes activate the immune cells. Researchers can use these immunostimulants to test how different cell subsets contribute to immune response mechanisms. This invention describes a novel type of immunostimulant that can be toggled on and off, both inside the body and in vitro.

Re-Sensitizing Cancer Cells to Anticancer Drugs

Researchers at the University of California, Davis have discovered a new class of ROR-γ inhibitors which can reduce and reverse cancer cell resistance to anticancer drugs.

Novel Solid Tumor Chemodrug LLS2

Researchers at the University of California, Davis have developed a new library of small molecule LLS2 that can kill a variety of cancer cells

Mi-181: A Potent Small Synthetic Microtubule-Targeting Anticancer Agent

UCLA researchers in the Department of Chemistry & Biochemistry and Department of Molecular & Medical Pharmacology have discovered compound MI-181 and successfully synthesized its derivatives and analogs, which have the potential for use in cancer therapy by arresting cells during the process of cell division and promoting apoptosis.

Enhanced Cell/Bead Encapsulation Via Acoustic Focusing

The invention consists of a multi-channel, droplet-generating microfluidic device with a strategically placed feature. The feature vibrates in order to counteract particle-trapping micro-vortices formed in the device. Counteracting these vortices allows for single particle encapsulation in the droplets formed by the device and makes this technology a good candidate for use in single cell diagnostics and drug delivery systems.

Aptamers that promote neuronal growth by binding to and blocking the protein Nogo

Neuronal growth inhibiting protein (Nogo), blocks regrowth of damaged neuronal projections (axons) in neurodegenerative disorders. Currently, researchers are developing antibody proteins to inhibit Nogo and produce axon regrowth in a variety of disorders. However, such antibodies are unstable and costly to synthesize. At UCI, the synthesis of nucleic acid molecules called aptamers that selectively bind and block Nogo to promote axonal growth presents a promising alternative pharmaceutical target for treating a range of disorders including spinal cord injury, stroke, Amyotrophic Lateral Sclerosis (ALS), and Multiple Sclerosis (MS).

Chiral Polymers Of Intrinsic Microporosity For Membrane Separation Of Enantiomers

Many pharmaceutical drugs exist as enantiomeric pairs, chemically-distinct mirror image of one another that often exhibit marked differences in biological activity. Current methods for separating enantiomeric mixtures to generate pure form of an effective drug involve multiple time-consuming and expensive steps. The invention herein describes a polymer that can selectively separate enantiomers in a simple, continuous process.

microfluidic device for preparation of monodisperse microcapsules and microvesicles

Many applications, ranging from in vivo cell culture growth to drug delivery, rely on microcapsules to encapsulate and protect cells or molecules until their desired release. These microcapsules are typically generated in immiscible fluid, which must be depleted before they can be effectively used. Researchers at UCI have recently developed a paper-based microcapsule extraction technique that is quicker, cheaper, and less damaging than conventional methods.

Splice Modulating Oligonucleotides as a Breast Cancer Therapy

UCR researchers have designed novel splice modulating oligonucleotides (SMOs) that decrease expression of the long form of the prolactin receptor, thereby significantly inhibiting the metastatic spread of breast cancer to the lungs and liver. The SMO treatment also increased central death in the primary breast tumor. These SMOs may also target metastases produced by non-prolactin receptor-expressing primary tumors since all cancer stem cells examined so far are positive for the prolactin receptor. The researchers administered SMOs to two highly aggressive metastatic models of breast cancer, BT474 human xenografts, used for testing Herceptin, and a 4T1 syngeneic mouse model, which allows testing with an intact immune system.   Fig. A shows a reduction in the number of metastatic colonies upon treatment with the UCR SMOs.       Fig. B titled "Control" is a stain of the metastatic colonies without SMO treatment. Fig. B titled "PRLR SMO" is a stain of the colonies after 40 days treatment with the UCR SMOs.

Potent And Highly Soluble Pegylated Compstatin Peptide

UCR researchers have developed novel compstatin peptides with polar amino acid extensions at the N-terminus and PEGylated extensions at the C-terminus. The new peptides have the following advantages compared to previously known compstatin peptides: (i) highly improved aqueous solubility while maintaining high inhibitory potency, and (ii) higher inhibitory efficacy against complement system activation in a human retinal pigmented epithelial cell-based assay that mimics the pathobiology of age-related macular degeneration. The combined solubility and inhibitory potency and efficacy properties render the new peptides excellent candidates to become therapeutics for the treatment of age-related macular degeneration.   A potent and highly soluble compstatin peptide shown in surface representation with an 8 PEG block C-terminal extension displayed in stick form. The surface of the compstatin analog is colored according to amino acid properties: gray for hydrophobic, green for polar neutral, blue for polar positively charged, red for polar negatively charged, yellow for cysteines of the disulfide bridge, and brown for glycine. The molecular image is generated using three-dimensional coordinates from a molecular dynamics simulation trajectory.    

Mesenchymal Stem Cell Derived Exosomes for Treating Peripheral Artery Disease

Researchers at the University of California, Davis have developed a method to isolate exosomes from mesenchymal stem cells that contain signaling molecules that induce angiogenesis. The isolated exosomes can be used for treating peripheral arterial disease.

Functionally Selective Ligands for Study and Inhibition of Inflammation

Background: Due to the complexity of the complement system cascade, biological roles of many signaling receptors are unknown. Additionally, biased ligand binding to cell-bound receptors may lead to selective intracellular effector binding and ligand-specific pathway activation and function. Mechanistic knowledge forms the basis for assay development to explore pharmacology against complement-mediated inflammatory diseases.   Brief Description: A multidisciplinary team of researchers from UCR, Texas A&M, Sheffield, and Queensland have discovered the first functionally selective peptide ligands for a complement system receptor that is involved in inflammation. The peptides are functionally selective ligands of C5aR2 but not C5aR1 or C3aR, and they have been characterized in vitro and in vivo. These peptides are novel tools that can modulate the activity of the receptor in vitro and in vivo, and interrogate the function of the receptor and its implication in inflammatory diseases.

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