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This technology includes a class of A3AR-selective agonists to be used therapeutically to treat a variety of conditions, including chronic pain, cancer, and inflammatory diseases. This class of compounds produced full agonists of the human A3AR of nanomolar affinity that were consistently highly selective (>1000-fold vs. A1AR and A2AAR). The selectivity at mouse A3 receptors is smaller, but the compounds are still effective in vivo in reducing or preventing development of neuropathic pain.

This technology includes three new chemical entities discovered for antibacterial and antifungal activities. The compounds are novel tetramic acid containing polyketides obtained from two different Amycolatopsis strains. Their planar structures and relative stereochemistry were elucidated by 1D and 2D NMR methods, including 1H-1H and 13C-13C COSY, TOCSY, HSQC, HMBC and ROESY. Whole genome sequencing of these two strains revealed a 158 kb biosynthetic gene cluster (BGC) containing a 23-module, mixed NRPS-PKS pathway responsible for their biosynthesis.

This technology includes a sphingosine kinase 1 (Sphk1) knockout mouse model for use in developmental biology research. Sphingosine-1-phosphate (S1P) is synthesized from sphingosine and ATP by the action of sphingosine kinase, and activates cell signaling. Two sphingosine kinases, SPHK1 and SPHK2, have been identified. To study the physiological function of SPHK1, Sphki null mice were generated. The mice were viable, fertile, with no obvious abnormalities. Total SPHK activity in most tissues was substantially reduced, suggesting the presence of other sphingosine kinases.

This technology includes the use of the (N)-methanocarba phosphonate analogues of 5’-AMP as cardioprotective agents for use in conditions such as cardiomyopathy and heart failure. We previously found a compound, MRS2339 (a phosphate derivative that can be slowly cleaved in vivo and lose potency), which activates the appropriate receptors and is protective in models of heart failure in several species (mouse, dog). MRS2339 is a phosphate derivative that can be slowly cleaved in vivo and lose potency. We now extend this technology to more stable derivatives, i.e.

This technology includes a new class of oligomeric molecules called thyclotides for diagnostic and therapeutic development. Thyclotides is described where chiral tetrahydrofuran (THF) diamine units are linked together with alternating glycines, and nucleobases are attached to this backbone as sidechains. The thyclotide sequence consists of a series of nucleobases similar to that of a nucleic acid sequence. Thyclotides are easily synthesized and purified with excellent solubility in water. Thyclotide sequences bind to complementary DNA and RNA sequences with very strong affinity.

This technology includes a mouse model for S1 pr1 to be used in development biology research. Sphingosine-1-phosphate is a potent bioactive compound that activates a family of G-protein coupled receptors known as Edg or S1P receptors. Triggering these receptors on cells may have important effects related to inflammation, immunity, cancer, angio-genesis, cell proliferation, adhesion, cardiovascular function, nervous system function and injury responses.

This technology includes P2X4R adenosine receptor antagonists, including NP-1815-PX and 5-BDBD, for treating stroke. Stroke is the fifth leading cause of death for Americans and a leading cause of serious long-term disability. Current approaches to treating ischemic stroke are primarily limited to the administration of thrombolytic therapeutics such as tissue plasminogen activator, or to an invasive endovascular procedure involving the use of a clot removing/retrieving device.

This technology includes a novel family of adenosine kinase (AdK) inhibitors, including pharmaceutical compositions containing the adenosine kinase inhibitors, and their use for preventing epilepsy and its progression in patients. Endogenous adenosine (i.e., naturally occurring adenosine) acts on G protein-coupled receptors (adenosine receptors, ARs) in the central nervous system to suppress seizures and pain, and to blunt the effects of ischemia (a restriction in blood supply to tissues).

This technology includes polyclonal antibodies against MLL3 (KMT2C), MLL4, PA1, UTX And PTIP for the development of treatments for development diseases and cancer. Enhancers play a central role in cell-type-specific gene expression and are marked by H3K4me1/2. Active enhancers are further marked by H3K27ac. However, the methyltransferases responsible for H3K4me1/2 on enhancers remain elusive. Furthermore, how these enzymes function on enhancers to regulate cell-type-specific gene expression is unclear.

This technology includes PPTN which can be used to study treatments of inflammatory diseases. PPTN is currently a useful pharmacological probe that many labs in the field of purinergic signaling are interested in obtaining. The availability of PPTN as a research tool will stimulate basic advances in the field and possibly eventually lead to new treatments. However, PPTN itself is unsuitable for therapeutic applications. Separately, we are working on new and improved antagonists of the P2Y14 receptor.