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This invention identifies a novel class of HIV inhibitors targeting RNA-protein interactions.

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.

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.

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.

This technology establishes a novel method to identify compounds that are either selective or non-selective modulators of glucocorticoid receptor signaling.

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 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.

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.

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.

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

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