Jacobson, Kenneth (NIDDK)
Research quantities of compounds have been synthesized and tested for receptor selectivity.
This technology relates to specific (N)-methanocarba adenine nucleosides that have been developed and dendrimers that connect these compounds to create molecules with multiple targets. Dendrimers are essentially repeated molecular branches presenting the core receptor-binding molecules. The compounds synthesized function as agonists and antagonists of a receptor of the G-protein coupled receptor (GPCR) superfamily. In particular, the receptors of interest for this invention include A3 adenosine receptors and agonists and antagonists of P2Y receptors, such as P2Y1 and P2Y14.
Dendrimer conjugates may have one or more advantages, such as increased solubility, reduced toxicity, and improved pharmacokinetic properties. They can also be used to connect other types of molecules without affecting the agonist or antagonists properties. For instance, molecules such as those used for imaging or tracing can be added. Dendrimers can also be used to link more than one type of agonist or antagonist to confer multiple functionalities. This technology provides a novel mechanism to treat a number of disorders related to dysregulation of A3 adenosine receptors.
- cardiac arrhythmias or ischemia