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A Novel Method to Generate Specific and Permanent Macromolecular Covalent Inhibitors

UCSF researchers have invented a novel method to generate covalent macromolecular inhibitors. This strategy allows a peptide inhibitor to bind to its target protein specifically and irreversibly through proximity-enabled bioreactivity.

Protein Kinase C Epsilon Small Molecule Inhibitors to Treat Pain, Anxiety, Alcoholism, and Nicotine Addiction

This invention provides new inhibitors to protein kinase C epsilon (PKCε) for the treatment and prophylaxis of various diseases such as pain, anxiety, alcoholism, inflammation, cancer, diabetes, and other conditions.

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.

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.

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.

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

SALT-SPARING UREA TRANSPORT INHIBITOR DIURETICS FOR TREATMENT OF CARDIOVASCULAR AND RENAL DISORDERS

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

NOVEL MUCOLYTIC COMPOUNDS FOR TREATMENT OF PATHOLOGIC MUCUS IN AIRWAY DISEASES.

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.

Small Molecule Inhibitors of IRE1 for Unfolded Protein Response (UPR)-Dependent Diseases

Novel small molecules that effectively inhibit IRE1, an enzyme critical for the activation of the unfolded protein response (UPR), providing a new method for therapeutic intervention in UPR-dependent diseases, such as cancer, inflammatory disease, autoimmune disease, and neurodegeneration.

Next-Generation Platinum Agents for the Targeted Treatment of Cancers

Platinum-based compounds are one of the most successful anticancer drugs that have been widely used to treat a variety of cancers, especially solid tumors. The major limitation of platinum-based drugs is the high toxicity, most notably oto- and nephrotoxicity. Since the discovery of the first platinum-based drug, cisplatin, additional compounds have been developed with more acceptable side-effect profiles, however dose-limiting toxicities still persist. To complicate this, tumors have acquired resistance to currently utilized platinum drugs. Possible strategies for overcoming resistance include specific targeting of platinum-containing drugs to tumors, thereby resulting in the direct killing of cancer cells.   To take advantage of platinum’s anti-cancer activity, cancer drug development efforts need to focus on compounds with reduced side effects that can also directly target cancer cells to efficiently kill tumors and prevent resistance formation.

Chemically Novel Beta-Lactamase Inhibitors

The market for new therapeutic products that will combat resistant strains of infectious pathogens commands $26 billion annually.  The U.S. market share for new generation antibiotics alone is expected to reach $10 billion this year.  To overcome the growing problem of microbial resistance, drug development companies have adopted a number of strategies based on the production of beta-lactamases, including developing new beta-lactamase inhibitors that can be co-administered with beta-lactam antibiotics.  This particular strategy has yielded three beta-lactamase inhibitors are all active against most class A enzymes, such as TEM-1, but not against class C enzymes, like AmpC.  Also, these inhibitors afford no protection to cephalsoporins clinically and have never been combined, for example, with the 3rd generation cephalosporins, leaving these widely used drugs susceptible to the evolution of the extended spectrun beta-lactamases (ESBLs).  Thus there is pressing need for new inhibitors that can be combined with a primary beta-lactam, especially a cephalosporin, rescuing these first-line antibiotics for continued clinical utility.

Novel Activators Of Executioner Procaspases 3, 6 And 7 and initiator caspase 9

UCSF researchers have created new small molecule activators of executioner procaspases 3, 6 and 7 and initiator caspase 9. These compounds have been shown to activate the relevant caspase targets in vitro and to induce apoptosis in a p53 deficient cell line. In addition, a coupled screening assay has been developed which can identify compounds that activate the executioner procaspases in the presence of caspase 9.

Small Molecule Therapy for Obesity, Dyslipidemia, and Metabolic Disease

  BACKGROUND: Cardiovascular disorders are leading causes of death worldwide and products have been developed to treat several of their addressable risk factors. Today’s market for anti-hypertensive agents is $35 billion and dyslipidemia treatments is $30 billion. While these therapies have been effective in the majority of patients in lowering blood pressure and LDL (low-density lipoprotein), they do not address other major cardiovascular risk factors such as obesity, liproprotein (a), HDL (high-density lipoprotein), and triglyceride levels. There is an unmet need for new agents that can be used alone or in combination with existing therapies to address these more elusive risk factors.   DESCRIPTION: Researchers at University of California San Francisco and Oregon Health Sciences University have discovered a new class of thyroid hormone metabolites. The most potent of these, 3-iodothyronamine, has been shown in animal studies to completely switch fuel utilization away from carbohydrates and toward lipids. In single dose hamster studies this lipid-burning effect was sustained for 24 hours, several hours after the compound had been excreted. Further studies showed both reduced LDL and significant weight loss that was selective for fat mass vs. lean mass. 3-iodothyronamine is known to be an endogenous chemical derivative of thyroid hormone, a key hormone in regulating basal metabolic rate, protein synthesis, bone growth, neuronal maturation, and metabolism of lipids and carbohydrates.

Endogenous Small Molecule Immune Response Modulator

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

Novel Pro-Drug Technology for Targeted Delivery of Therapeutic Agents

UCSF investigators have developed a novel targeted pro-drug technology that can selectively deliver a chemotherapeutic payload to cells in areas of high concentrations of endogenous free ferrous iron. The pro-drug can be conjugated to a variety of existing and novel pharmacologically active compounds to increase their therapeutic window and lower systemic toxicity by increasing the selectivity of their delivery. Applications include therapies for cancer and malaria and as imaging agents. 

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