Karen Houseknecht publishes research in ‘Journal of Medicinal Chemistry’

Karen Houseknecht, Ph.D., professor of pharmacology in the College of Pharmacy, in collaboration with Tobin Dickerson (Scripps Research Institute, San Diego) and Garry Smith (Fox Chase Chemical Diversity Center, Doylestown, Pennsylvania), has published the research paper “Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain” in the Journal of Medicinal Chemistry.

Clostridium botulinum neurotoxin serotype A is the most potent toxin known to man and is considered a potential bioterrorism weapon due to its extreme toxicity and ease of production.  Despite significant research efforts in the field, there is currently no available therapeutic to treat botulinum toxin poisoning, largely due to chemical properties that are not amenable for human dosing and drug exposure. 

Houseknecht’s laboratory has focused on determining the drug-like properties (solubility and drug metabolism) of these novel inhibitors as well as evaluating their pharmacokinetic profiles in pre-clinical models. 

The research published in this paper highlights the findings of this NIH-funded multi-site, interdisciplinary research team to identify potent inhibitors with physicochemical properties that are amenable for oral dosing and proof-of-principle studies.