The incidence and complications arising from airway diseases are constantly increasing and chronic conditions of the airway significantly outnumber those of diabetes, cancer, heart disease combined. A quarter of the U.S. population are affected by airway diseases such as acute and chronic bronchitis, pneumonia, cystic fibrosis, asthma, chronic obstructive pulmonary disease (COPD), bronchiectasis, bronchiolitis, ventilator-associated airway mucus hyper-secretion, and acute and chronic sinusitis. Mucus overproduction and hypersecretion have been implicated to play a key role in these airway diseases.  However, mucus pathology is very poorly understood and hence recent advances have not been sufficient to develop effective treatments. Existing mucolytic drugs provide only moderate relief and have a number of limitations such as weak potency, volatility, bad smell in addition to side effects such as nausea, rash and sores. There is a need to address the large unmet need for novel mucolytic therapies for a wide range of acute and chronic airway disease. (more...)

Cell-based systems for in vitro biomarker profiling of drug efficacy or discovery. (more...)

UC Irvine biologists, chemists and computer scientists have identified an elusive pocket on the surface of the p53 protein that can be targeted by cancer-fighting drugs. The finding heralds a new treatment approach, as mutant forms of this protein are implicated in nearly 40 percent of diagnosed cases of cancer, which kills more than half a million Americans each year. (more...)

Prion diseases are a class of neurodegenerative disorders associated with the accumulation of an infectious isoform of a normally innocuous soluble host prion protein (PrPC). In prion disease, the endogenous alpha-helix rich PrPC protein is converted by an unknown mechanism into a protease-resistant and β-sheet–rich PrPSc form. This conversion can occur spontaneously, result from inherited mutations in the PrPC gene, or be triggered by infection with exogenous PrPSc. Animal prion diseases include Bovine Spongiform Encephalopathy (BSE), Chronic Wasting Disease (CWD), and Scrapie, while human prion diseases include Creutzfeldt-Jakob disease (CJD), kuru, and Gerstmann-Sträussler-Scheinker syndrome. Prion diseases are invariably fatal, and no viable treatments are currently available for these devastating disorders. (more...)

Down Syndrome (aka Trisomy-21), which affects approximately one of every 700 babies born in the United States each year, is characterized by varying degrees of stunted cognitive and physical ability as well as characteristic facial and body features. The extent to which an individual will be able to integrate into society is determined by the severity of the condition as well as the timing and extent of intervention. Historically, intervention has included screening with subsequent dedicated therapy and training. However, recent work on the etiology of Down Syndrome (see Lu et al., below) has suggested that inhibition of a chromosome 21 (HSA21)-associated, oligodendrocyte transcription factor (OLIG2) may blunt the effects of over-expression of a subset of HSA21 genes that inhibit the growth of neural progenitors, which are necessary for normal brain development. This approach provides new hope for a prevalent disease with a tremendous burden on society and for which no medical treatment exists. (more...)

Lung cancer is the leading cause of cancer related death in the United States. In 2012, it is estimated that approximately 230,000 patients will be newly diagnosed, and since more than 160,000 individuals will succumb to this disease, there exists an urgent need for improved therapeutics. In the past, natural products have served as the basis for the development of a number of anti-cancer agents approved for clinical use; examples include the plant derivatives taxol and camptothecin. Interestingly, anti-tumor activity of parthenolide (PTL) - a natural substance that can be isolated from a plant known as feverfew (Tanacetum parthenium) - has also been demonstrated. However, feverfew extract and native PTL exhibit poor bioavailability. Analogs with increased solubility and bioavailability have recently been synthesized and show promise as anti-cancer agents. One of these analogs, dimethylaminoparthenolide (DMAPT), has recently entered early phase clinical testing for the treatment of leukemia. (more...)

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. (more...)

SIO scientists have mined their rare collection of marine organisms to identify, characterize and analog a proprietary, small molecule with anti-cancer properties. SAR studies have identified regions of the molecule that have yielded analogs of greatest interest. Compositions of matter and methods of use are claimed for the treatment of cancer and hyperproliferative disorders. (more...)

Although treatment of cancer through non-surgical methods such as chemotherapy and radiation has dramatically improved survival rates, these therapies are associated with a fair degree of toxicity. The deleterious effects are particularly due to inability of these treatment methods to target cancer cells specifically without affecting surrounding normal cells. The challenge therefore, has been to find methods of selectively protecting normal cells, while maintaining susceptibility of cancer cells to therapy. Apoptosis triggered by chemotherapy and radiation is the most common cause of destruction of normal cells and is due to activation of a fully functional p53 protein present in these cells. p53 protein-induced transactivation of several genes involved in the apoptosis pathway leads to elimination of normal cells when exposed to anti-cancer agents. Therefore, therapeutic suppression of p53 directly or of its pathways leading to apoptosis, are attractive targets to prevent damage to normal cells during anti-cancer therapy. Earlier efforts in this area led to the isolation of a chemoprotectant, pifithrin that protected normal cells against radiation and chemotherapy-induced damage. However, this agent was not potent, was unstable and was not a specific inhibitor of p53-related apoptotic pathways. Hence, there is a clear need for new chemical inhibitors that are more robust, stable and specific as chemoprotectants of normal cells during anti-cancer therapy. (more...)

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. (more...)

The vascular wall is now accepted to play a critical role in activating immune responses. Endothelial cells that comprise the vasculature are active modulators of inflammatory responses. A number of molecular signals have been identified to mediate crosstalk between immune and vascular cells. Specifically, interferon gamma (IFN-γ) is a potent cytokine that mediates anti-microbial and anti-cancer biological functions of immunity and induces over 4000 genes in human endothelial cells. To date, few therapies exploit the interaction between the endothelium and immunity to treat disease. Therefore, great potential exists in identifying small molecules that modulate immunity through endothelial cell interaction. The identification of such compounds would have a particularly promising role in treating cardiovascular disease, chronic inflammatory conditions, and cancer. (more...)

 The agouti-related protein (AgRP) is produced in the brain and is a potent appetite stimulant. The normal 50 amino acid polypeptide is produced in the hypothalamus and binds with high affinity to the melanocortin 3 and 4 receptors (MC3R and MC4R). Along with alpha-melanocyte stimulating hormone (apha-MSH) and neuropeptide Y, AgRP plays a central role in the regulation of mammalian feeding and metabolism. From intracerebroventricular (ICV) injection studies, AgRP is well documented to enhance feeding for one to two days following a single injection, and is probably longer acting than any other known hormone or drug.  (more...)

Midazolam has previously been administered via a variety of routes, including the intranasal route, for the management of acute seizures. UC Davis researchers have demonstrated in rodent chemoconvulsant models that inhaled intrapulmonary (nebulized) midazolam can protect against seizures more rapidly and more potently than when administered by other routes. The lung is highly vascularized and the thin alveolar epithelium represents a large absorptive surface. Blood exiting the lung is delivered directly to the brain so that the seizure protection conferred by intrapulmonary midazolam occurs with very short latency. Unexpectedly, midazolam delivered via the lung is more potent than when administered by other routes, including intravenously. (more...)

Bioactive peptides and peptidic small molecules are of interest as potential intracellular therapeutics in human disease. Peptide therapeutics have great potential for high target specificity, low toxicity, and low accumulation in tissues. Unfortunately natural unmodified peptides often exhibit poor permeability across cell membranes and this has limited the utility of peptides as therapeutics for intracellular targets.  (more...)

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

While inflammation is a beneficial component of the body’s response to harmful stimuli, prolonged or excessive inflammation can damage tissues and initiate a cascade of events that culminate in a wide variety of diseases. Anti-inflammatory drugs include steroids, non-steroidal anti-inflammatory agents (NSAIDs) and immune selective anti-inflammatory derivatives. However, these agents have undesirable side effects and a need remains for novel anti-inflammatory agents that exert their effects through different modes of action. (more...)

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

Expectorants are a class of medications that help dissolve thick mucus and thus relieve respiratory congestion. Widely-used expectorants such as guaifenesin, currently found in many popular over-the-counter formulations like Robitussin® and Mucinex®, can have problems with drug interactions or with side effects such as allergic reactions, nausea, and vomiting. The challenge in creating viable competitors to existing expectorant compounds, however, is that they must also be economical to manufacture and easy to deliver to the respiratory system as well as have fewer side effects. (more...)

Scripps Institution of Oceanography (SIO) at UC San Diego is one of the oldest, largest, and most important centers for global science research and education in the world. With the oceans covering 70 percent of the earth's surface, it is no surprise that approximately two-thirds of the world's animal phyla are found in marine environments and many are exclusively marine. SIO scientists were among the first to explore the natural product chemistry of marine organisms and this research helped to develop the field of marine natural products chemistry and the realization that the oceans harbor myriad new organic molecules with utility for the development of pharmaceuticals and other products. This research led to the discovery of hundreds of new compositions of matter for new products—some of which are already well progressed into commercial development. Two compounds are now entering phase II clinical trials. One of these, Salinosporamide A, is a potent proteasome inhibitor. The second compound, which is derived from the fungal metabolite halimide, acts as a vascular disrupting agent. (more...)

More than 60,000 people in the United States are diagnosed with lymphoma each year and the prognosis for those affected is usually poor. In many cases, patients may respond initially to first-line treatments (e.g. chemotherapy, radiotherapy), but subsequently suffer a relapse. In other cases, a patient may fail to respond to any treatment (refractory cancer). For patients diagnosed with relapsing cancers or patients resistance to conventional treatment, there are no optimal or preferred treatment options, resulting in a poor prognosis. Additional treatment options are needed for this group of lymphoma patients. (more...)

UCSF investigators have isolated set of compounds  to treat cystic fibrosis (CF). The compounds are anticipated to treat the underlying defects in patients with the delta F508 mutation of the CFTR gene, which is present in around 90% of the CF cases. Small molecule therapy directed toward correcting the deltaF508 defects in cellular processing and channel gating of CFTR is thought to hold considerable promise. A panel of novel potentiators (which restore gating defects) and correctors (which restore protein folding and plasma membrane trafficking) are available for licensing. Several of the potentiators identified are very potent (some at submicromolar potency) in restoring the gating defect in both deltaF508 mutants and other CFTR gating mutants, including G551D. They have also identified several highly effective (micromolar potency) correctors of the deltaF508 mutant protein. When used in combination, these compounds may correct the defects caused by the deltaF508 mutation in the CFTR gene.  Additionally, the investigator is currently developing a bifunctional compound capable of both potentiation and corrector activity, with promising results. It is thought that both activities are required to fully address the protein folding/trafficking and gating defects present in this mutation, which is the most prevalent (90%US/66% world population). A single molecule that can address both defects in the deltaF508 mutation could provide a simplified approach that would be easier to study in clinical trials. The investigators believe the bifunctional compounds could be manufactured as either oral tablet or inhaled aerosol formulation.    (more...)

Background: UNAIDS and the WHO estimate that AIDS has killed more than 25 million people since it was first recognized in 1981, making it one of the most destructive pandemics in recorded history. Currently, in USA alone, it is estimated that one million people are living with HIV or AIDS and roughly 55,000 more become infected each year. Although there is no cure for HIV infection, treatment with anti-retroviral drugs that target the HIV virus can significantly extend the lifespan of HIV-infected patients. Unfortunately, due to the rapid evolution of the HIV virus, many antiviral drugs are rendered ineffective by the emergence of drug-resistant viral variants. Therefore, it is imperative that alternative strategies to combat HIV infection are developed. One such creative strategy taken by UCSF scientists is to identify host cell factors that are vital for HIV replication and to generate products to neutralize these factors while preserving normal host cell function. Invention: Innovative scientists at UCSF have a) identified a number of host factors involved in HIV replication using a novel, elegant screening method; and b) generated siRNA products to knockdown the expression of six of these host factors. Importantly, the team successfully demonstrated that knockdown of any one of these six factors significantly reduced HIV replication rates. Therefore, the screen and / or siRNAs would be an important asset to companies with an anti-HIV therapeutic focus. (more...)

Over 190,000 new cases of breast cancer are diagnosed each year. Of all breast cancer patients, two thirds have a positive estrogen receptor (ER) profile. The ER is an intracellular transcription factor that interacts with estrogen to initiate the transcription of growth factor genes. Growth factors are important constituents in the growth and development of breast cells. Blockade of the estrogen pathway by interfering with the binding of estrogen to its respective receptor is the basis of many breast cancer treatments. One example is the use of tamoxifen, an anti-estrogen that works by competitively binding to the ER.Antiestrogen therapy has had a significant impact on disease-free survival in breast cancer patients with a positive ER profile. However, tamoxifen has some undesirable side effects such as formation of liver and endometrial tumors. Moreover, as breast cancer progresses, it usually becomes resistant to estrogen and hence, the strategy of binding the ER with a competitive inhibitor becomes ineffective. (more...)

UCSF investigators have identified a novel endogenous agent that activates the Aryl Hydrocarbon Receptor. (more...)

Background: Prostate cancer, alopecia, hepatocellular carcinoma, and acne vulgaris are a few examples of the myriad of diseases linked to androgen receptor signaling. These diseases have a significant impact on human health; for example, The American Cancer Society estimates that in 2009, prostate cancer will cause 27,360 deaths and 192,280 new cases will be diagnosed. In fact, one man in six will get prostate cancer in his lifetime and one in thirty-five will die from this disease. Androgen receptor inhibitors are the primary treatment option for androgen-related diseases. Current inhibitors prevent ligand binding to the androgen receptor, but these treatments can result in acquired resistance and serious side effects. Due to the limitations of current treatment options, alternative antiandrogen therapies are urgently needed. Inventions: Prominent UCSF scientists have discovered a suite of novel small molecule inhibitors of the androgen receptor. Using an innovative approach to avoid the pitfalls associated with current antiandrogen therapies, Dr Diamond’s team identified multiple compounds that inhibit the androgen receptor post-ligand binding. The team validated this work by demonstrating the ability of these compounds to inhibit endogenous androgen receptor activity in prostate cancer-derived cell lines. Further validation in animal models of prostate cancer is underway for many of the novel compounds. Significantly, the team demonstrated that one such compound, pyrvinium pamoate, inhibits androgen receptor signaling in vivo and induces prostate atrophy. Furthermore, pyrvinium synergizes with known inhibitors that prevent ligand binding (Jones et al. 2009). In addition to the novel compounds, an assay to detect selective gene regulation by ligand dependent transcription factors has been developed. This assay could be used to uncover additional candidates for androgen receptor inhibition. The assay has been successfully tested on the glucocorticoid receptor and led to the discovery of selective modulators of this receptor for treatment of inflammation, allergic, and immune-mediated diseases.  Three patents have been filed on these technologies to provide a strong IP position for a licensee. (more...)

UC San Diego inventors have devised a new structure, isolated from a natural product that can inhibit progression through the cell cycle. The new structure's use as an anti-cancer agent is in the early stage of preclinical studies. The novel structure inhibits mitosis in a fashion that differs from known natural products, with the current hypothesis being that an aspect of its structure inhibits the exit from anaphase. This effect was observed in both colon cancer cells (HCT111), breast cancer cells (HeLa), and neuroblastoma cells (Neuro2a). Cytotoxicity data has been collected in HCT111 cell lines and complete cytotoxicity data is being collected via analyses by the NCI-60 cell screen. Cell cycle screening, uptake, and localization data are complete in HCT111 cells and shall be expanded to other cell lines. (more...)

Although algorithms and chemistries for developing new therapeutic entities are constantly evolving, none can replicate the path and novelty of natural selection over eons of time. Inventors at the Scripps Institution of Oceanography have engaged their fleet of research ships to cull the oceans for marine organisms from which new compositions are isolated.  Using a variety of culture systems, selective fractionation and bioassays, two, distinct classes of compounds, isolated from actinomycetes, have demonstrated potent anti-tumor activity and considerable selectivity toward some cancers. One class of compounds, the ammosamides, are unique molecules that target a previously untargeted intracellular pathway. It is anticipated that proprietary methods and naturally evolved compositions may yield therapeutics that are significantly differentiated from those developed by limited iteration of pre-defined platforms. (more...)

Salinosporamide A (Sal A) is a potent proteasome inhibitor produced by the marine bacterium Salinispora tropica. This natural product is biosynthesized from three metabolic building blocks, namely acetate, a chlorinated tetrose from S-adenosylmethionine, and the non-proteinogenic amino acid cyclohexenylalanine. Sal A exhibits potent cancer cell cytotoxicity apparently through inhibition of the 20S proteasome, a multisubunit protease responsible for proteolysis of proteins targeted for degradation in the cell. Tumor cells may be more sensitive to proteasome inhibitors than normal cells and proteasome inhibition increases the sensitivity of cancer cells to anticancer agents. (more...)

Actinomycetes are well known soil bacteria that were once believed to occur in the ocean only when washed in from land. Today, it is clear that unique populations of marine actinomycetes reside in ocean sediments and that these bacteria are fundamentally different from those on land. Although terrestrial actinomycetes have been the source of many of today's more than 120 drugs, marine actinomycetes have only recently been incorporated into the discovery process. These bacteria are now proving to be a particularly rich source of unique natural products, many of which display potent biological activities. (more...)

UC San Diego researchers have developed a novel class of potent inhibitors of phospholipase A2 (PLA2), an enzyme that initiates the inflammatory cascade by releasing arachidonic acid and other inflammatory mediators. Current anti-inflammatories such as Celebrex and Vioxx target the cyclooxygenase enzymes (COX) that are just downstream from PLA2. Inhibition of PLA2 blocks the protaglandin cascade, as well as the leukotriene and platelet activating factor cascades. Since PLA2 supplies the substrate arachidonic acid, inhibition of PLA2 will also regulate the COX enzymes. The effectiveness of the PLA2 inhibitor has been demonstrated in vitro, and it is being tested in animal models of pain and inflammation. (more...)

Parasitic diseases, such as malaria, African sleeping sickness, Chagas disease and trichomoniasis, are major worldwide health problems for which new chemotherapy is desperately needed. For example, an estimated five million cases of the sexually transmitted disease trichomoniasis occur each year in the United States alone. Malaria kills over a million people a year worldwide and is second only to tuberculosis in its impact on world health. Current treatments for these diseases have varying degrees of effectiveness and serious problems with toxicity, drug-resistant strains, and lack of selectivity. Therefore, there is a need for the development of new therapeutics for the treatment of these diseases.Researchers at the University of California, San Francisco have discovered that a novel series of small molecules, in a class that has previously been evaluated for antiviral and anticancer therapy, is effective in killing a variety of parasites, including those that cause malaria, trichomoniasis, Chagas disease and African sleeping sickness. By screening a library of these novel small molecule compounds, the researchers found several promising lead compounds that killed a range of parasites in cell culture assays and had no toxicity in mouse studies. These compounds therefore represent a potentially powerful new therapeutic avenue for parasitic diseases. (more...)

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. (more...)

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. (more...)

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. (more...)

Microscopy is an important tool used by all researchers in the scientific community. Often, a microscope user will first scan the specimen with a low power dry objective and then wish to switch to an oil, water or glycerin immersion objective to increase optical resolution. In other cases, a user might want to scan a large area, i.e. a multiple-well plate, and would need to replace the immersion media as it is sheared away from the objective lens. In the case of inverted microscopy, both of these examples pose a problem for maintaining the integrity and position of the specimen because the user is required to remove the sample from the stage for application of the immersion media. This procedure is time consuming and difficult to reposition the sample after the immersion fluid is delivered. A more effective method would involve delivery of the immersion media without removing the sample. (more...)

Serotonin 5-HT1A receptors are implicated in Alzheimers disease, dementia, anxiety, schizophrenia, and depression, and significant efforts have been undertaken to develop various compounds that bind to these receptors for potential use in diagnosis and therapy of disorders associated with serotonin 5-HT1A receptors. Among other proposed approaches, particularly desirable compounds include those suitable for selective positron emission tomography (PET) analysis. While currently known compounds target the serotonin 5-HT1A receptors to at least some degree, numerous difficulties nevertheless exist. Among other problems, all or almost all of the known compounds are metabolized at a relatively fast rate, and/or are eliminated from plasma is an undesirably short time. Thus, data analysis is often difficult. Still further, the synthesis of such compounds is frequently difficult to achieve in adequate yields. Moreover, where 18F is used as a radiolabel, compounds are often rendered chemically instable. Worse yet, affinity of 18F-labeled compounds to the target receptor is typically relatively low. Thus, while numerous compositions and methods for serotonin 5-HT1A receptor ligands are known in the art, all or almost all of them suffer from one or more disadvantages. Therefore, there is still a need to provide improved compositions and methods for such ligands, especially for 18F-labeled ligands. (more...)

Sodium/potassium ATPases (Na+/K+-ATPases), a family of multi-subunit ion pumps, are the most important active transporters in animal cells. They are required for maintaining the electrochemical gradient responsible for resting membrane potentials in neuronal cells and for the function of other transport proteins in a variety of cell types. The important regulatory activities of Na+/K+-ATPases make them an attractive therapeutic target for the treatment of neurodegenerative, cardiac, and other diseases. To date, there are unmet medical needs for the treatment of these diseases, and it is desirable to discover and develop novel therapeutic agents aimed at treating ion pump related disorders. (more...)

The determinant factor for the successful applications of delivering drugs is to develop a non-viral and efficient carrier. Cationic lipid based liposomal carriers are the most attractive non-viral solution. Advantages of liposomal vectors include safety, lack of immunogenicity, ability to package large DNA molecules and ease of preparation. However, the conventional processes for catatonic lipids and DNA complex formulation are normally irreproducible. (more...)

Phytochrome-Derived Fluorescent Markers (more...)

Altering chimeric pigs' DNA for the purpose of creating transgenic and knockout pigs (more...)

Amino Acid and Peptide Conjugates of Amiloride allowing for furnishing inactive prodrugs that can be selectively activated by tissue endopeptidases (more...)

Technology for engineering antibodies to bind irreversibly to their receptor has been developed by UC Davis researchers. This technology, enabling the formation of permanent antibody-antigen complexes has a number of potential applications in chemistry and biology, including: targeted medical imaging targeted medical therapies (e.g., cancer therapeutics) synthetic tag to replace avidin-biotin no competition from endogenous ligands no dissociation after capture humanized format Furthermore, UC Davis researchers have constructed a bispecific fusion protein that has tumor targeting properties and irreversibly captures a metal chelate. This combines irreversible metal chelate binding with tumor targeting activity for the first time in a highly homogenous genetic construction that can be expressed at high yields. In addition, this allows the substitution of other targeting sequences allowing for a wide range of cellular targets. The irreversible nature of the chelate binding has not been previously achieved in a single expressed protein fused to a tumor targeting functional segment. (more...)

Aβ-binding Small Molecules for Alzheimer's Disease Treatment and Imaging (more...)

Platform for Testing the Effects of Human PTP1B Inhibition on Insulin Signaling, Adipose Differentiation and Glucose Uptake (more...)

Researchers at the University of California, Davis have developed transgenic mouse models that constitutively express B cell Activating Factor (BAFF) in the Tumor Necrosis Factor (TNF) family, and Green Fluorescent Protein (GFP) under the control of Glial Fibrillary Acidic Protein (GFAP) promoter in astrocytes. (more...)