Related Experiment Video
Updated: Aug 9, 2026

Understanding the Development of Compensatory Pathways in a Mutant Malaria Parasite Harbouring Hypomorphic Allele of Plant-Like Kinases
Published on: November 22, 2024
Highly substituted terphenyls as inhibitors of parasite cGMP-dependent protein kinase activity
Chaowei Zhang1, John G Ondeyka, Kithsiri B Herath
1Natural Products Chemistry and Human and Animal Infectious Disease, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065, USA.
Abstract:
Parasite cGMP-dependent protein kinase (PKG) is one of the validated biochemical targets for the treatment of coccidiosis. We screened our library of natural product extracts for inhibitors of parasite PKG for the discovery of anticoccidial leads. Terferol (1) and three new terphenyls (2, 3, and 4) were isolated using bioassay-guided fractionation of the microbial extract of a Phoma sp. by a high-throughput two-step isolation method employing LH-20 and reversed-phase HPLC. These compounds inhibited parasite PKG with IC(50) values in the range 0.9-5.8 microM.
Related Concept Videos
Anthelminthic Agents
Antiprotozoal Agents
Indirect-Acting Cholinergic Agonists: Mechanism of Action
Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex, leading to...
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
GPCRs Regulate Adenylyl Cylase Activity
Two...
Inhibitors of Gram-positive Cell Wall Synthesis

