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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.

Development of a novel class of small molecules for the treatment of cognitive disorders

Neuronal dendritic spines act as sites of learning and memory in the brain. Dysregulation of dendritic spines is a central problem in a wide range of neurodegenerative and developmental cognitive diseases such as Autism spectrum disorder, Schizophrenia, Stroke, ADHD, and PTSD. There are very few examples of molecules that promote the formation of new dendritic spines.

Diagnostic and Screening Methods for Atopic Dermatitis

Atopic dermatitis (AD) is a chronic itch and inflammatory disorder of the skin that affects one in ten people. Patients suffering from severe AD eventually progress to develop asthma and allergic rhinitis, in a process known as the “atopic march.” Signaling between epithelial cells and innate immune cells via the cytokine Thymic Stromal Lymphopoietin (TSLP) is thought to drive AD and the atopic march. TSLP is up regulated in atopic dermatitis patients and is thought to act on immune cells to trigger atopic dermatitis. Scientists at UC Berkeley discovered that TSLP also activates a subset of sensory neurons to signal itch by acting on TSLPR, which signals to TRPA1. They demonstrated that sensory neurons that transmit itch signals in AD are the only instance of signaling between TSLPR and TRPA1 in the same cell type. Therefore, blocking the signaling between TSLPR and TRPA1 is a novel and specific target for therapeutics for itch in atopic dermatitis. They also discovered that the Orai I/Stim I pathway triggers expression and secretion of TSLP. This pathway has never been directly demonstrated in human primary keratinocytes and has never before been linked to TSLP. Decreasing expression of Orai I or stim I using siRNA, or the downstream transcription factor, NFATc I, significantly attenuates TSLP secretion, as proven in mice studies. Thus inhibition of Orai I/Stim I/NFATc I signaling pathway is a novel target for therapeutics for itch in atopic dermatitis.

New Borylated Heterocycles: Indoles, Isoxazoles, Lactones, and Benzofurans, and the Methods to Make Them (related to UC Case 2013-921)

Boron building blocks play a key role in modern organic chemistry, especially in drug design and materials synthesis. Methods to generate heterocycles and borylated compounds in the same synthetic step are largely unknown; the ability to do both increases efficiency and rapidly builds molecular complexity while providing access to previously unavailable building blocks.

A Method to Identify Novel Glucocorticoid Receptor Modulators

This technology establishes a novel method to identify compounds that are either selective or non-selective modulators of glucocorticoid receptor signaling.

High Affinity CYP3A4 Inhibitors

Cytochrome P450 3A4 (CYP3A4) is a key metabolizing enzyme that regulates the oxidation and clearance of most drugs. The inhibition of this enzyme may be useful in improving the efficacy of drug cocktails and the ability to give lower, less toxic doses of drugs. The development of new CYP3A4 inhibitors with high affinity and specificity is described.

A New Class Of HIV Inhibitors Targeting Viral Accessory Factor vif

Current antiretroviral agents target enzymatic functions of the virus such as reverse transcription (nonnucleoside or nucleoside reverse transcriptase inhibitors; NNRTI and NRTI), protease processing of viral polyporoteins (protease inhibitors), viral membrane fusion (fusion inhibitors) and viral DNA integration (integarase inhibitors). Drug cocktail (a combination of nonnucleoside and nucleoside reverse transcriptase inhibitors as well as protease inhibitors) is effective in suppressing viral infection into a chronic condition which rarely progresses to AIDS, many of the inhibitors have adverse side effects. For example, NRTIs can interfere with mitochondrial DNA synthesis and cause hypersensitivity, anemia, diarrhea, neuropathy, nausea, and fatigue in patients. NNRTI may cause severe liver damage or psychological disorders such as depression and insomnia. Protease inhibitors may cause numerous drug-drug interaction, elevated lipodystrophy, and elevated risk of heart attack. Lastly, integrase inhibitors only have short and medium term medical outcomes but are not suitable for long-term use. Therefore there is a need to search for a different class of HIV inhibitors that are efficacious and better-tolerated by patients. HIV-1 encodes accessory proteins including vif, vpu, and nef; these proteins counteract cellular antiviral factors that otherwise would restrict viral replication. Necessary for the replication of HIV-1, vif promotes viral replication by targeting host antiviral protein apobec 3 for degradation. Apobec 3 is a cytidine deaminase that introduces catastrophic levels of G to A hypermutations in viral cDNA, thus yielding biologically incompetent viral genomes. As viral replication is absolutely dependent on the ability of vif to neutralize apobec 3, the vif-apobec axis is an attractive antiviral target.  Currently, there are no compounds that target the vif/apobec axis.

Methods and Compositions of Treating Diabetic Nephropathy and Insulin Resistance

Researchers at the University of California, Davis have developed novel methods and compositions for the treatment of diabetic nephropathy and insulin resistance.

Compositions and Methods for Treating Estrogen-Receptor Associated Conditions

 Menopausal hormone therapy (MHT) reduces the risk of developing osteoporosis, fractures, obesity and type II diabetes, yet it is only approved for short-term therapy due to the serious risks associated with long-term therapy (e.g., increased risks of breast cancer, stroke, and heart attacks). To target these indications associated with menopause, it will be necessary to develop safer MHT regimens that can be used as continuous therapy. There are two current strategies for developing safer MHT:  First, estrogens have been combined with the selective estrogen receptor modulator, bazedoxifene, which prevents estrogen binding to ERα, thereby blocking the proliferative effects on the uterus. However, this combination is approved only for short-term treatment of hot flashes. Second, ERβ-selective agonists have been developed; unfortunately, ERβ agonists may not be effective for osteoporosis, weight gain or diabetes because ERα is the major active ER in both bone and adipose tissue.   UC Berkeley researchers have discovered a compound that acts as a reprogramming ERα coligand that could improve safety profile of MHT. The compound was found to bind of to a different site on ERα and reprograms the actions of estradiol. This compound represents a new class of drugs that can be combined with existing estrogens to produce safer MHT regimen for long-term treatment to safely prevent chronic diseases associated with menopause. 

Novel Target For Contraceptives And Painkillers

The steroid progesterone (P4) is a major component of follicular fluid and is released by ovaries and cumulus cells surrounding the oocyte.  P4 is known to cause rapid and robust elevation of sperm cytoplasmic calcium levels through binding to a non-genomic receptor.  This rise in intracellular calcium leads to changes in sperm motility and primes the cell for acrosomal exocytosis, which is required for fertilization.     UC Berkeley researchers have identified an enzyme as a P4 non-genomic receptor.  The enzyme was found to possess progesterone-stimulated endocannabinoid hydrolase activity, and regulate human sperm activation.  The technology includes methods of modulating the level and/or activity of the enzyme in a cell in an individual. 

Novel TLR-4 Ligands as Immune Activators

Toll-like receptors (TLRs) are a set of conserved cellular proteins that play an important role in the recognition of microbial pathogens and in initiating the first line of host innate immune response. Although early work suggested that modulating the response could have clinical utility, few agents have been able to clear regulatory hurdles to development. A comprehensive screen for small molecules that activated NF-kB identified substituted 4-aminoquinazolines with potential clinical utility to modulate innate immune responses.

Novel compounds for the treatment of fungal infections

Treatment of fungal infections remains a medical challenge and better and more efficacious treatments are needed. Antifungal agents provide relief from fungal infections that can potentially infect almost any part of the human body, but, systemic fungal infections can be life threatening. A commonly prescribed antifungal drug for systemic fungal infections is fluconazole. Fluconazole tends to be well tolerated; however there have been reports of various undesirable side effects as well as the emergence of fluconazole resistant fungal strains.

Improvements of cognitive function in age-related disorders and Alzheimer's disease

Cognitive deficits associated with aging and other age-related disorders involve deficits in processing sensory information, attention, consolidation of memory, recall of information, and executive functions such as planning, problem solving and self-monitoring among others. There is a large unmet medical need to identify therapies and novel therapeutic regimes for the treatment of cognitive dysfunction, e.g., cognitive deficits related to aging, age-related disorders and Alzheimer's disease. Previously published research suggests a correlation between neurological disorders and trimethylation of histone H3K9 in the brain. Therefore, an inhibitor of histone methyl transferase SUV39h1 and its effects on the progression of age-related disorders was investigated.

Metal Binders for Drug Discovery

The use of compound or fragment libraries are being increasingly used in drug discovery as rational drug design has become more sophisticated and high throughput techniques have made screening these types of libraries faster and less labor intensive.

Methods Of Treating Cancer Using Novel Hsp90/Cdc37 Inhibitors Derived From Cucurbitacin Family

This invention identifies a novel group of cuburbitacin derivatives that inhibit the interaction between Hsp90 and Cdc37, and may be applied to cancer treatment.

Plasma Biomarkers for Monitoring Cancer Chemotherapy Efficacy

Highly sensitive protein biomarkers that can be used to monitor the extent of apoptosis in order to optimize chemotherapy regimen in cancer patients

Novel Neuropathy Treatment Using Soluble Epoxide Inhibitors

Researchers at the University of California, Davis have developed a new method and composition of blocking pain using a novel class of analgesic agents and a synergistic combination involving soluble epoxide inhibitors.

Small Molecule Inhibitors Targeting Digestive System Enzymes to Control Obesity and Type II Diabetes

Researchers in the Department of Chemistry and Biochemistry have identified a compound that can block the enzyme that converts “hunger hormone” precursors to active hormones.

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