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Mutasynthesis of fluorinated pactamycin analogues and their antimalarial activity
Khaled H Almabruk1, Wanli Lu, Yuexin Li
1Department of Pharmaceutical Sciences, Oregon State University, Corvallis, Oregon 97331-3507, United States.
Organic Letters
|March 26, 2013
Abstract:
A mutasynthetic strategy has been used to generate fluorinated TM-025 and TM-026, two biosynthetically engineered pactamycin analogues produced by Streptomyces pactum ATCC 27456. The fluorinated compounds maintain excellent activity and selectivity toward chloroquine-sensitive and multidrug-resistant strains of malarial parasites as the parent compounds. The results also provide insights into the biosynthesis of 3-aminobenzoic acid in S. pactum.

