Browse Category: Medical > New Chemical Entities, Drug Leads

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Novel molecular target and approach(es) for the bidirectional modulation of T-cell function

Researchers at UC Irvine have identified and tested a molecular target that regulates T cell function during chronic viral infection and cancer. The molecular target is one of the high mobility group proteins (HMGB2). HMGB2 is a DNA binding protein that regulates transcriptional processes, meaning that its modulation will have profound effects on T cell differentiation and ultimate function by altering the expression of many genes.

Small molecule drug leads for p53 mutant cancers

Researchers at UC Irvine have used a computationally powered method to identify small molecule drug leads that exhibited anti-cancer activity in a human-cell-based assay. These small molecules and the approach used to find them will accelerate the research and development of anti-cancer therapeutics.

Pharmacological fortification and/or restoration of protective nerve coverings via a novel therapeutic target

Researchers at UC Irvine have discovered a novel mechanism by which restoration of protective nerve coverings fails in degenerative disease like multiple sclerosis. While therapeutics to slow disease progression exist, there are currently none aimed at preventing or restoring damage to nerve coverings.

Small Molecules for Restoring Activity of p53 Mutants found in Human Cancer

This invention consists of novel small molecule compounds that bind to mutant variants of p53 and induce conformational changes to restore p53 function for treatment of human cancers.

Teixobactin O-Acyl Isopeptide Prodrugs

Recently, teixobactin was investigated to treat antibiotic-resistant pathogens, but the drug has yet to reach clinical trial due to its tendency to form gels which prevents accurate dosing. To address this, researchers at the University of California, Irvine have invented a new library of teixobactin related prodrugs which show improved solubility and efficacy versus teixobactin.

Peptide Inhibitors of Human Voltage Gated Proton Channel hHv1 Activity to Reduce Inflammation

Human voltage-gated proton channels (hHv1) are implicated in a wide range of biological responses, including capacitation of sperm and stimulation of the innate immune response. Human sperm undergo a process called capacitation in the female reproductive tract, whereby intracellular pH rises and stimulates a progesterone-induced Ca2+ influx.  Researchers at the University of California, Irvine have discovered that this calcium influx is controlled by albumin activation of Hv1 voltage-gated proton channels.  Albumin activation of hHV1 in neutrophils also supports production and release of reactive oxygen species and protease during the immune respiratory burst.  These findings demonstrating a stimulatory role of albumin in both sperm and neutrophils has led to new therapeutic approaches to fertility and the treatment of inflammatory diseases.

Cyclic Peptide Inhibitors of The SARS-Cov-2 Main Protease

The SARS-CoV-2 virus has rapidly spread across the globe with severe medical, social, and economic costs. The Researchers at the University of California Irvine have designed novel cyclic peptide inhibitors based on a crystal structure of an inactive variant of SARS-CoV, known as Mpro318. Based on a small library of cyclic peptide inhibitors, some candidates showed promising in vitro activity at low micromolar concentrations.

Novel Prodrug For Anti-Cancer Therapeutic Applications

Inventors at UCI have developed a modified nutrient transporter inhibitor for use as a cancer therapeutic with minimal side effects.

Novel Mixtures For Synergistic Activation Of M-Channels

Epilepsy is a seizure causing neurological disorder that affects over 50 million people, and it is estimated that half are ineffectively treated with current therapeutic options. Researchers at UCI have isolated components of a plant extract used to treat epilepsy in Africa and discovered that, when combined with an existing epilepsy medication, the mixture greatly decreases epileptic episodes and significantly increases survival rates in rodent models of epilepsy.

Potent, State-Independent, and Specific Inhibitor of the Human Proton Channel Hv1

Researchers at UCI have engineered a class of Hv1 polypeptide modulators that selectively modulate Hv1 voltage gated channels while leaving other voltage gated channels unaffected. With no Hv1 modulators currently on the market, this class of Hv1 polypeptide modulators could provide solutions in birth control, autoimmune therapies, tumor reduction, and inflammatory disease treatment.

A New Approach To Treat/Manage Inflammatory Bowel Disease

Researchers at UCI have developed a safe, inexpensive drug for the treatment of inflammatory bowel diseases.

Drug Combinations For Treatment Of Tinnitus, Vertigo, and Headache

UC Irvine researchers propose various combinations of medications for treatment of tinnitus and vertigo.

A High Potency CYP3A4 Inhibitor for Pharmacoenhancement of Drugs

      CYP3A4 is the most clinically relevant drug metabolizing enzyme in the body, as it is responsible for the oxidation and breakdown of ~60% of current drugs on the market.  Researchers at UCI have developed novel CYP3A4 inhibitors, that are highly potent and more specific, exhibit fewer side effects, and are both cheaper, and easier to-synthesize than current commercially available CYP3A4 inhibitors. 

Therapy to improve survival in patients with end stage renal disease

Despite many recent improvements in dialysis treatment, End Stage Renal Disease (ESRD) patients on hemodialysis continue to experience an annual mortality rate of approximately 20%, a rate worse than many cancers. Researchers at UCI have identified an association between increased levels of endocannabinoid (EC) in ESRD patients’ serum and decreased risk of death thereby providing a potential therapy to enhance survival times for patients.

A Highly Error-Prone Orthogonal Replication System For Targeted Continuous Evolution In Vivo

Inventors at UC Irvine have engineered an orthogonal DNA replication system capable of rapid, accelerated continuous evolution. This system enables the directed evolution of specific biomolecules towards user-defined functions and is applicable to problems of protein, enzyme, and metabolic pathway engineering.

Antimicrobial, Stimuli-responsive Polysaccharide

State of the art antimicrobial therapeutics, while effective and promising, remain only short-term solutions to the overall challenge of drug-resistant microbes. UCI researchers have developed a chitosan-based nanoantibiotic that is non-toxic and carries potential for broad spectrum use.

Controlled 'One-Cell-One-Bead' Encapsulation in Droplets

The invention relates to a technique using a microfluidic device to perform co-encapsulation of samples in droplets and sorting of said droplets. This technique can achieve a one-one-one encapsulation efficiency of about 80% and can significantly improve the droplet sequencing and related applications in single cell genomics and proteomics. .

Small Molecules for Melanoma Treatment

Traditional anti-cancer treatments used for metastatic melanoma (skin cancer) can result in cell toxicity, poor efficacy, and low patient survival. UCI researchers have uncovered a class of potent compounds that inhibit cancer cell growth and induce cancer cell death by targeting RhoJ signaling pathways.

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.

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.

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.

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.

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.

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.

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