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Ion Channel Ligand Discovery from Phytomedicines

Chad Jansen Headshot

Project Summary: I will begin my first year in INBRE by teaching BI480 Special Topics: Biophysics and pharmacology (a 1-3 credit elective lecture) in Spring 2022 at Chaminade University. This course will be designed for students intending to enter PhD programs and medical school. I will receive mentorship from Dr. Helen Turner for the lab project as well as teaching. Dr. Claire Kendal-Wright offered to provide mentorship for course design and teaching.

Ion channels of the Transient Receptor Potential superfamily are targets in pain and inflammation. Nociceptive TRP (nTRP) channels (TRPA1, V1, M8, V2) respond to physicochemical inputs as well as nociomimetic small molecules found in plant species. Phytomedicines from cultural medical systems (CMS) have identified TRP ligands as analgesics but key questions limit the applicability and translation to mainstream Western medical use. The research objectives of this project are: 1. Compounds such as sesquiterpene lactones are found in numerous CMS indications for pain but paradoxically seem to act as nTRP agonists rather than blockers. Does this indicate that agonist-mediated desensitization rather than antagonism or inverse agonism is the primary analgesic mechanism arrived at by CMS? 2. Are there previously unrecognized nTRP antagonists within the significant chemical diversity inherent to CMS formulations? At the completion of this project, we will know if agonist mediated desensitization in nTRP channels occurs in response to phytomedical compounds and create a streamlined method for nTRP antagonist identification from phytomedicines.


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