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New Borylation Methods Generate New Building Blocks For Drug Discovery

Boron plays a key role in modern organic chemistry, but, the utility of boron beyond Brown’s hydroboration and Suzuki’s palladium cross-coupling reactions is limited.

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.

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.

CYP3A4 Epoxygenase Inhibitors for ER+ Breast Cancer Treatment

Small molecule CYP34A inhibitor oncology therapeutics are being developed in collaboration between scientists at UC Irvine and U of Minnesota. These molecules have been shown effective against ER+ xenograft models of breast cancer. Due to their mechanism of action, these molecules may enhance treatment with tamoxifen and paclitaxel to decrease risk of recurrence.

Small Molecules as chemotherapeutics agents for cancer treatment by restoring p53 function.

The tumor suppressor p53 normally functions to prohibit unregulated growth of cells. p53 is the most frequently mutated gene in human cancers. The most frequent p53 mutation is a missense mutation known as R175H. We have discovered 11 small molecules that interact with and stabilize R175H protein. The stabilization of R175H by these small molecules restores p53 function and can be a potential drug candidate. Currently, there are no known drug targets that specifically work on p53 mutants and our compounds will be the first to have specific targeting capacity.

Imprinted Polymer Nanoparticles

Synthetic polymer nanoparticles (NPs) capable of recognizing specific biomacromolecules and can be used as substitutes for natural antibodies .

Novel Chitosan Derivative as a Systemic Drug Delivery Agent and an Antibiotic Treatment

Researchers at the University of California, Irvine have developed a novel chitosan derivative that may be used simultaneously as a systemic drug delivery agent and a systemic antibiotic treatment.

Novel Inhibitors Of Endocannabinoid Inactivation for Treatment of Pain, Anxiety and Depression

Bioactive lipids, including anandamide (AEA), are important signaling molecules in humans. Acting through CB1 cannabinoid receptors in the brain and peripheral tissues, the local concentrations of these lipids have effects on several areas of human health including pain sensation, inflammation, appetite regulation, anxiety, and depression. The regulation of these lipids is partially controlled by their degradation rate by the enzyme fatty acid amide hydrolase (FAAH). The present portfolio of inventions provides novel small-molecule inhibitors FAAH, including molecules that are limited to peripheral FAAH inhibition as well as molecules improved for oral bioavailability. These compounds have been tested in a number of animal models and one molecule has entered clinical trials in humans. This portfolio includes molecules with IC50 values at single digit nanomolar and in some cases, less than 1.0 nanomolar concentrations in vitro.

Novel Acid Ceramidase Inhibitors for Oncology and Hyperproliferative Skin Disorders

Acid ceramidase (AC) catalyzes the hydrolysis of the lipid messenger ceramide thereby regulating ceramide levels in cells. AC is involved in multiple physiological and pathological processes, including cancer resistance and neuropathic pain. Previous AC inhibitors are ceramide analogs with weak inhibitory activity in vitro and virtually no utility in vivo.  The present portfolio of inventions provides two chemically distinct classes of small-molecule inhibitors of intracellular AC activity, which act at single digit nanomolar concentrations in vitro and at low doses in vivo.

Small Molecules for Analgesia and Anti-Nausea

Anandamide is a biologically active lipid molecule that regulates multiple biological functions – including pain, nausea and mood – by activating CB1 cannabinoid receptors in the brain and peripheral tissues. In the brain, the biological actions of anandamide are stopped by a selective mechanism that starts with the uptake of anandamide by neurons and glial cells. Researchers at UCI have developed novel, small molecules that inhibit this transport process, causing anandamide levels to increase. This produced in turn a spectrum of CB1 receptor-mediated responses that include reduced pain and nausea.

Potential Novel Anti-Viral Target For Chemotherapeutics Against Picornaviruses, Such As Human Rhinovirus An Entervirus 71

Picornaviruses, viruses that belong to the family Picornaviridae, are single-stranded RNA viruses that infect both humans and animals. The major picornaviruses that affect humans include enteroviral pathogens (poliovirus, coxsackievirus, enterovirus, echovirus), rhinoviruses (approximately 105 serotypes), hepatitis A virus, and parechoviruses. Currently, there no medications indicated to treat picornavirus infections, and only the symptoms can be treated. New treatments for picornavirus infections would be extremely useful for medical professionals and their patients. Researchers at the University of California, Irvine have discovered an enzyme that is involved in the virus life cycle of the picornavirus. This enzyme may be a novel anti-viral target for chemotherapeutics that can be used against picornaviruses.

Small molecule inhibitors of the Hv1 channel as chemotherapeutics and anti-inflammatory agents

The compounds we propose target a new pathway via (Hv1) molecule implicated in cancer (metastasis) and anti-inflammatory. Our hypothesis is that cancer cells that overexpress the Hv1 channel and are dependent on its activity for proliferation will be sensitive to the Hv1 inhibitors we are developing. Currently, there are no known specific blockers of this channel and our leads will be the first to target this pathway.

Heterodimer of Toll-Like Receptor Agonists for Cancer Immunotherapy

TLR agonists, such as CpG, have been used as immunotherapies against tumors in clinical studies. TLR agonists promote tumor-specific Th1 and cytotoxic T lymphocyte responses that allows the immune system to develop responses to eradicate tumors. Researchers at the University of California, Irvine have developed a heterodimer consisting of lipoteichoic acid (LTA), a TLR2 agonist, and CpG, a TLR 9 agonist, conjugated by a PEG linker. This novel heterodimer greatly enhances Th1 response and elicits the highest activation of dendritic cells and macrophages unlike unconjugated LTA or CpG.

New imaging agents for AB-amyloid plaques and tangles

Researchers at the University of California, Irvine have synthesized new chemical entities that selectively bind to regions in the brain that accumulate Aβ-amyloid plaques.

Chip-Based Droplet Sorting

Microfluidic devices are poised to revolutionize environmental, chemical, biological, medical and pharmaceutical detectors and diagnostics. The term “microfluidic devices” loosely describes the new generation of instruments that mix, react, count, fractionate, detect, and characterize samples in a micro-electro-mechanical system (MEMS) circuit manufactured through standard semiconductor lithography techniques. Although a wide array of microfluidic technologies are currently available, novel MEMS fluidic systems are needed as scientists continue to work with smaller sample volumes and desire devices with increased sensitivity and effectiveness. Researchers at the University of California, Irvine have developed a unique non-contact system for sorting monodisperse water-in-oil emulsion droplets in a microfluidic device. The technology can be coupled to other on-chip processes to increase device efficiency by sorting out un-reacted droplets.

New Treatment for the Prevention and Reversal of Non-Alcoholic Fatty Liver Disease (NAFLD)

Researchers at the University of California, Irvine have found a new use for a known compound for treatment of fatty liver disease which has been shown to be effective in animal studies.

Treatment to protect and / or recover sexual function of the cavernosal nerve (sexual potency) after radical prostatectomy

It is estimated that 1 in 6 men will be diagnosed with prostate cancer in their lifetime. One of the consequences of removing the prostate for prostate cancer is a non-permanent injury of the cavernosal nerve during open radical prostatectomy (RP) or robot-assisted radical prostatectomy (RARP), which may result in post-operative sexual dysfunction. These sexual side effects can severely affect the quality of life for men and their loved ones. Researchers at the University of California, Irvine have developed a new use for an existing compound that can be used to prevent, mitigate, or treat erectile dysfunction associated with prostate removal surgery.

A Rapid Method To Measure Cyanide In Biological Samples In The Field

Cyanide is a highly toxic and rapidly acting poison that is infamous due to its use in murders, suicides, wars and attempted genocide.In the present day, cyanide may be responsible for up to 10,000 deaths annually in the United States due to smoke inhalation.Cyanide may also be used as a terrorist weapon. Prior methods to measure cyanide in the blood have involved acidifying the blood after lysis of red blood cells.However, this method is time consuming (takes at least a few hours) and tedious, and thus, inadequate for rapid detection of cyanide toxicity in field or hospital settings.Field or laboratory devices capable of rapidly measuring cyanide levels in blood or body fluids are not currently available, however such field or laboratory devices would be highly useful. Researchers at the University of California, Irvine have developed a method to rapidly measure cyanide in biological samples, which can be carried out in field settings.This method is based on measuring cyanide based on spectral changes that occur when cyanide binds to the reagent.Advantages of this method are its ease of use, stability, and applicability across a wide range of cyanide concentrations and may be used with ease in the field or on laboratory devices.

Generation Of Choroid Plexus Epithelial Cells From Human Embryonic Stem Cells

The process developed involves the generation of human choroid plexus epithelial cells from human embryonic stem cells to enable novel clinical applications.

Overman Small Molecule Library

The Overman laboratory at the University of California, Irvine has generated a library of ~1,200 unusually diverse small drug-like molecules.

A New Process Of Adding Alkyl Groups To Organic Substrates Using TmI2(MeOCH2CH2OMe)3

In the pharmaceutical industry, synthetic chemists often alkylate starting compounds to generate compounds that have more desirable properties. However, the current reagents used in this modification process can be expensive or harmful to the chemist.

Her2/neu Vaccine Protects Against Tumor Growth

Her2/neu is over-expressed in various types of tumor cells, including 20-30% of breast cancers, adenocarcinomas of the ovary, salivary gland, stomach and kidney, colon cancer, and non-small cell lung cancer. Passive immunotherapeutics like Herceptin control and prevent further tumor cell growth. Unlike active immunotherapeutics, Herceptin does not mediate the immunological cellular destruction. Active immunotherapeutics such as vaccines elicit T helper-1 (Th1) and Cytotoxic T lymphocytes (CTL) biased immune responses and are generally observed for proteins expressed in the intracellular compartment, and less prominently with extracellular or secreted proteins. Rapid degradation of a protein containing polyepitopes can contribute to establishing a bias in the immune response, facilitate antigen presentation and, perhaps assist in establishing specificity of the immune response. This type of immunological response should result in immunological cellular destruction.

New Protein Resistant and Biodegradable Biopolymer

The ability to resist nonspecific protein adsorption (protein resistance) is an indicator of a material's biological inertness or biocompatibility. Protein resistant biomaterials such as the commonly used poly(ethylene glycol) (PEG) have been used in a number of applications such as prostheses, contact lenses, implanted devices, microfluidic systems, drug delivery, and substrates for assays. However PEG has two major limitations. First PEG can only be functionalized at the chain ends, and second PEG is not biodegradable.

Design and Synthesis of PET Radioligands for alpha 4 beta 2 Nicotinic Acetylcholine Receptors

Nicotinic acetylcholine receptors (nAChRs) belong to the superfamily of ligand-gated ion channels and are distributed widely in the human and nonhuman brain. Several nAChRs have been identified and characterized pharmacologically and have distinct patterns of distribution in the brain. The nicotine alpha 4 beta 2 receptor subtypes are thought to play a role in various diseases, including various brain disorders (e.g., Alzheimer's disease), behavioral disorders (e.g., schizophrenia or substance abuse), various neoplasms (e.g., lung cancer), and other diseases, and may also be involved in the addiction to nicotine in chronic tobacco users (tobacco use may increase the number of the alpha 4 beta 2 receptor sites). The development of noninvasive imaging methods using PET and SPECT of the alpha 4 beta 2 receptor system has gained significant interest. Therefore, and not surprisingly, the development of noninvasive imaging methods using PET and SPECT of the alpha 4 beta 2 receptor system has gained significant interest. However, current radiotracers suffer from several drawbacks, including rapid clearance, toxicity, and undesirable kinetic parameters. Consequently, there is still a need to provide improved compositions and methods for radioligands for receptors of the alpha 4 beta 2 receptor type.

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