Structure-guided design of PfPKG inhibitors for malaria chemoprevention

Inventor (s): Purnima Bhanot

Date Awarded: July 2021

Summary:

Drugs targeting Plasmodium's liver stages have been identified as one of two target product profiles for next-generation anti-malarial drugs. These drugs are needed to quickly contain local outbreaks and prevent new infections amongst populations that have lost their natural immunity to disease in previously-endemic countries. In addition to endemic countries, Western tourists, business-travelers, foreign troops, and international aid workers need protection from malaria infection. It is essential to find new anti-malarial with mechanisms of action that are distinct from current drugs compromised by the spread of resistant parasites. Our medicinal chemistry program has identified a promising lead molecule, whose optimization will be significantly accelerated by structure-guided design. We will obtain the structure of the  molecule bound to its target, PfPKG and use this structural information to rapidly advance medicinal chemistry.

Market applications:

• Prevention of malaria