Structure-based Drug Design and SAR Studies of Inhibitors Targeting Protein Kinase C Epsilon for Non-opioid Pain Management




de Kraker, Harmannus Cornelis

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The annual NIH report states that pain affects more Americans than diabetes, heart disease, and cancer combined. Furthermore, chronic pain is the most common cause of long-term disability. One of the most common treatments for lasting pain involves opioids, however, recent statistics indicated over 10 million people misused prescription opioids in 2019 with over seventy thousand overdose-related deaths in the same year. Protein Kinase C epsilon inhibition has been associated with non-opioid pain relief and as such, led to the discovery of our lead compound CIDD-0072424. Development of a robust and efficient enantioselective synthesis route supported SAR studies, producing lead compounds with in vivo efficacy in pain models and improved ADME and drug-like properties. Several potent and selective inhibitors were discovered that can be applied as excellent chemical tools for the study of PKCε-related mechanistic pathways, as well as novel viable drug leads.


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Drug Development, medicinal chemistry, non-opioid, Pain, PKC, Protein Kinase C