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Tios T-te – A Prototypical Thioesterase Responsible for Cyclodimerization of the Quinoline- and Quinoxaline-type Class of Chromodepsipeptides

Authors: Lars Robbel, Katharina M. Hoyer, Mohamed A. Marahiel

Field: Biochemistry / Chemistry

Document Content: This study presents the first in vitro characterization of TioS T-TE, a thioesterase enzyme crucial for the iterative assembly of quinoline- and quinoxaline-type chromodepsipeptides. The research details the enzyme’s capability to catalyze both macrolactonization and macrothiolactonization. It explores the substrate specificity of TioS T-TE and optimizes macrocyclization reactions to achieve maximum yields. The study confirms the backward mechanism proposed for iterative thioesterases and investigates chemoenzymatically generated macrocycles for their DNA-bisintercalation activity. TioS T-TE is highlighted as a robust and versatile catalyst for producing chromodepsipeptide analogs, potentially leading to compounds with enhanced pharmaceutical properties.

Detailed Table of Contents:

  • Keywords
  • Correspondence
  • Abstract
  • Introduction
  • Results
  • Discussion
  • Experimental Procedures
  • Acknowledgements
  • References
  • Supporting Information