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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.

Inhibitors Of Ires-Mediated Protein Synthesis

The Gera group at UCLA has discovered a novel analog of a known compound with significant anti-glioblastoma potential when used in combination with mTOR inhibitors.

Sensitive Probe for In Vitro Detection of A-beta Aggregates

The extreme sensitivity of Probe‐Enabled Fluorescence Correlation Spectroscopy (PE‐FCS) can enable significantly improved sensitivity for monitoring the aggregation of amyloidogenic proteins vs. current methods which measure the fluorescence of the amyloid‐binding dye Thioflavin T (ThT) or Thioflavin S (ThS) using bulk fluorescence measurements. A significant limitation of the conventional method is that neither ThT nor ThS fluoresce appreciably over background fluorescence until the size and number of amyloid or amyloid‐like species is quite large. Hence, one cannot detect early formed aggregate intermediates that are implicated as the most active species involved in the pathology of amyloid‐associated diseases, such as Alzheimer’s Disease.

A Novel Therapeutic Against HIV Using Human T Cell Immunoglobulin Mucin (TIM-3) Ligands to Modulate Immune Response

Blocking human T cell immunoglobulin and mucin domain-containing molecule 3 (TIM-3) signaling can restore functionality to defective T cells in HIV-1 infected patients. Additionally, measuring TIM-3 provides clinicians with a novel way of evaluating, staging, and monitoring the progression of HIV infections.

Synthesis of Lipobactins and Teixobactin Analogues – New Antimicrobial Compositions against Gram-Positive Bacteria

With the discovery of penicillin in the 1940’s, many scientists proclaimed the defeat of infectious diseases which had plagued mankind. However, the remarkable healing power of antibiotics unfortunately invited widespread and indiscriminate use of antibiotics. This misuse and overuse of antibiotics has led to the dramatic rise in antibiotic resistant bacterial strains and increased healthcare costs.

Novel Small Molecule CFTR Activators for the Treatment of Constipation

This invention identifies novel small molecule activators of CFTR (cystic fibrosis transmembrane conductance regulator) that can be developed as effective therapies to treat constipation.

Novel Small Molecule CFTR Activators For the Treatment of Dry Eye

This invention identifies novel small molecule activators of CFTR (cystic fibrosis transmembrane conductance regulator) that can be developed as effective therapies for dry eye disorders.

Pyrite Shrink-Wrap Laminate As A Hydroxyl Radical Generator

The invention is a diagnostic technology, as well as a research and development tool. It is a simple, easy to operate, and effective platform for the analysis of pharmaceuticals and biological species. Specifically, this platform generates hydroxyl radicals for oxidative footprinting – a technique commonly employed in protein mapping and analysis. The platform itself is inexpenisve to fabricate, scalable, and requires nothing more than an ordinary pipet to use. In addition, it is highly amenable to scale-up, multiplexing, and automation, and so it holds promise as a high-throughput method for mapping protein structure in support of product development, validation, and regulatory approval in the protein-based therapeutics industry.

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