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Preparation of 20-Demethyl DM1 using microbial transformation
Pages: 168-172+185
Year: Issue:  3
Journal: Bulletin of Fermentation Science and Technology

Keyword:  T-DM120-demethyl DM1biotransformationStreptomyces platensis;
Abstract: T-DM1 is an antibody-drug conjugate(ADC),which is covalently linked by trastuzumab and maytansinederivative(DM1) through thioether connection, and 20-dimethyl DM1 is an important compound for the evaluation of T-DM1 pharmacokinetics. In this study, a method for preparation of 20-demethyl DM1 by microbial transformation was developed. It was found that Streptomyces platensis CGMCC 4.1975 could convert DM1 intermediate II into 20-demethyl DM1 intermediate II. The reaction conditions including substrate concentration and reaction time were optimized to improve the reaction efficiency. When the fermentation was carried out for 48 h, 0.5 mL of 2.9 g/L DM1 intermediate II solution was added. The concentration of 20-demethyl DM1 intermediate II reached 24.4 mg/L after fermentation for another 72 h. 20-Demethyl DM1 intermediate II samples were obtained by separation and purification. 20-Demethyl DM1 was obtained by sulfhydryl reduction of 20-demethyl DM1 intermediate II in a yield of 19.3%. And the obtained product was identified as 20-demethyl DM1 using HPLC, LC-MS and H NMR.
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