Browse Category:


[Search within category]

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.

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.

Engineering Human Proteases for Therapeutic Use

A methodology termed “protease evolution via cleavage of an intracellular substrate” (PrECISE) to enable engineering of human protease activity and specificity toward an arbitrary peptide target. 

New Compositions to Treat Heparin Overdose

Heparin is one of the most frequently prescribed medications in the United States. And despite the fact that protamine has displayed adverse side effects and demonstrates low efficacy towards reversing more recently developed low molecular weight heparins (LMWH), protamine remains the only clinically-approved heparin reversal agent. To treat heparin overdose, new heparinoid reversal agents with high potency and low toxicity are needed - particularly for patients receiving LMWH and unfractionated heparin.

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

A Non-Natural Linker for the Synthesis of Pure, Constrained Tricyclic Peptides

UCLA researchers have developed a novel non-natural linker as the scaffold for the synthesis of pure, single-regioisomer-product of tricyclic peptides, which greatly enhances the efficiency of peptide modification and their pharmaceutical value.

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.

Preparation and Activity of Novel Photosensitizer Acting as a Broad Spectrum Antiviral Agent Against Enveloped Viruses

Professor Michael Jung’s group at UCLA has developed a novel class of compounds with broad spectrum antiviral activity toward enveloped viruses.

Novel Short Netrin-1 Derived Peptides for the Treatment of Myocardial Infarction

UCLA researchers in the Department of Anesthesiology have identified three novel short netrin-1 derived peptides for the treatment of myocardial infarction with improved scalability and fewer adverse side effects.


Therapeutic inhibitors of Urea Transporter A (UT-A) as highly effective diuretics with reduced risk of cardiac and neurological side effects for treatment of cardiovascular and renal disorders

Activating HIV Latency Using Drug Encapsulated Nanoparticles

UCLA researchers in the Department of Microbiology, Immunology, and Molecular Genetics have devised a novel method to target the HIV virus in patients using nanoparticles loaded with therapeutic agents.

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.

Method For Delivery Of Drugs Across The Intact Tympanic Membrane

The current treatment for ear infections such as systemic antibiotics can have serious side effects, especially if used prophylactically to prevent recurrent middle ear infections. Also, the amount of drug that actually reaches the middle ear is not high, and often ineffective. In children, especially, systemic antibiotics lead to drug resistance. Other treatment options include tympanostomy tubes (surgery) which requires general anesthesia, with risks. Therefore local delivery of drugs to the middle ear would address many of these issues. 

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 .

  • Go to Page:

These technologies are part of the UC QuickStart program.

University of California
Innovation Alliances and Services

1111 Franklin Street, 5th Floor,Oakland,CA 94607-5200 |
Tel: 510.587.6000 | Fax: 510.587.6090 |