Differential effects of tautomycetin and its derivatives on protein phosphatase inhibition, immunosuppressive function and antitumor activity.

The Korean Journal of Physiology & Pharmacology : Official Journal of the Korean Physiological Society and the Korean Society of Pharmacology
Mingshan NiuRongguo Qiu

Abstract

In the present work, we studied the structure-activity relationship (SAR) of tautomycetin (TMC) and its derivatives. Further, we demonstrated the correlation between the immunosuppressive fuction, anticancer activity and protein phosphatase type 1 (PP1) inhibition of TMC and its derivatives. We have prepared some TMC derivatives via combinatorial biosynthesis, isolation from fermentation broth or chemical degradation of TMC. We found that the immunosuppressive activity was correlated with anticancer activity for TMC and its analog compounds, indicating that TMC may home at the same targets for its immunosuppressive and anticancer activities. Interestingly, TMC-F1, TMC-D1 and TMC-D2 all retained significant, albeit reduced PP1 inhibitory activity compared to TMC. However, only TMC-D2 showed immunosuppressive and anticancer activities in studies carried out in cell lines. Moreover, TMC-Chain did not show any significant inhibitory activity towards PP1 but showed strong growth inhibitory effect. This observation implicates that the maleic anhydride moiety of TMC is critical for its phosphatase inhibitory activity whereas the C1-C18 moiety of TMC is essential for the inhibition of tumor cell proliferation. Furthermore, we measured ...Continue Reading

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Citations

Oct 21, 2014·Future Medicinal Chemistry·Sam ButterworthAlastair J Barr
Jul 23, 2016·Biochemical and Biophysical Research Communications·Ming LiLi Tang
Oct 14, 2016·Journal of Industrial Microbiology & Biotechnology·Si-Sun ChoiEung-Soo Kim
Apr 24, 2014·The Korean Journal of Physiology & Pharmacology : Official Journal of the Korean Physiological Society and the Korean Society of Pharmacology·Hong ZhangRongguo Qiu
May 1, 2021·Journal of Industrial Microbiology & Biotechnology·Hee-Ju NahEung-Soo Kim

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Methods Mentioned

BETA
phosphatase
FACS
Assay
ELISA

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