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September 12, 2025ACS OmegaOpen Access

Mutasynthesis of C17- and C21-Substituted Ansamitocins for Use as ADC Payloads

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Authors

ASAnna E. Stanley-SmithNCNigel CoatesJFJ. Fox

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Overview

Strain engineering improves ansamitocin titer and produces fluorinated derivatives, indicating potential ADC efficacy.

Key Points

  • Fluoro and bromo ansamitocins were generated through mutasynthesis, enhancing their cytotoxic activity.
  • C21 fluoro ansamitocin was successfully converted to a cytotoxic payload for ADC applications.
  • Strain engineering in Actinosynnema pretiosum improved the production of ansamitocins using specific AHBA analogs.
  • C17 and C21 substituted ansamitocins exhibited cytotoxic activity comparable to Ansamitocin P3.

Cite This Study

Stanley-Smith et al. (2025) studied this question.

synapsesocial.com/papers/68d44a1d31b076d99fa52f89https://doi.org/10.1021/acsomega.5c05529
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