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Dopamine D3 Receptor Agonist Compounds, Methods of Preparation, Intermediates Thereof, and their Methods of Use

Scientists at the National Institute on Drug Abuse (NIDA) have developed novel dopamine D3 receptor (D3R) agonists with high affinity and selectivity. Two lead compounds, 53 and eutomer 53a, have demonstrated significantly higher D3R binding selectivity than reference compounds. Moreover, 53 and 53a showed metabolic stability in liver microsomes, which is favorable for the future use of these compounds as therapeutic agents for diseases related to dopamine system dysregulation such as Parkinson’s Disease and Restless Legs Syndrome. Researchers at NIDA seek licensing and/or co-development research collaborations for the use of these D3R agonists as molecular tools for the study of D3R physiology and as potential therapeutics to treat neurological and neuropsychiatric disorders.

Methods of Producing Thymic Emigrants from Induced Pluripotent Stem Cells

Pluripotent stem cells are a promising source of T cells for a variety of clinical applications. However, current in vitro methods of T cell differentiation result in the generation of cells with aberrant phenotypes. Researchers at the National Cancer Institute (NCI) have now developed methodology for generating induced pluripotent stem cell thymic emigrants (iTE). Antigen-specific CD8αβ+ iTEs exhibited functional properties in vitro that were almost indistinguishable from natural naïve CD8αβ+ T cells, including vigorous expansion and robust anti-tumor activity. iTEs recapitulated many of the transcriptional programs of naïve T cells in vivo and revealed a striking capacity for engraftment, memory formation, and efficient tumor destruction. The NCI seeks licensing and/or co-development research collaborations for this invention.

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