Chemical modification of pradimicin A to suppress aggregation without impairing D-mannose-binding and antifungal activities
2022
Nakagawa, Yu | Oya, Yuzuka | Ojika, Makoto | Igarashi, Yasuhiro | Ito, Yukishige
Pradimicin A (PRM-A) is an actinomycete-derived antibiotic that shows antifungal activity through binding to d-mannose (Man)-containing glycans of fungi. Despite its unique mode of antifungal action, therapeutic application of PRM-A has been severely limited by the aggregate-forming property. In this study, we demonstrated that C4′-N-formyl PRM-A and the dexylosylated derivative of C4′-N-acetyl PRM-A showed significant Man-binding and antifungal activities without any aggregation or precipitation. The presented results provide a promising modification strategy for exploring the therapeutic application of PRM-A.
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