Supplementary Materials

Supplementary Material for:

Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration

Fuqin Fan, Zhixiang He, Lu-Lu Kong, Qinghua Chen, Quan Yuan, Shihao Zhang, Jinjin Ye, Hao Liu, Xiufeng Sun, Jing Geng, Lunzhi Yuan, Lixin Hong, Chen Xiao, Weiji Zhang, Xihuan Sun, Yunzhan Li, Ping Wang, Lihong Huang, Xinrui Wu, Zhiliang Ji, Qiao Wu, Ning-Shao Xia, Nathanael S. Gray, Lanfen Chen, Cai-Hong Yun,* Xianming Deng,* Dawang Zhou*

*Corresponding author. Email: dwzhou{at}xmu.edu.cn (D.Z.); xmdeng{at}xmu.edu.cn (X.D.); yunch{at}hsc.pku.edu.cn (C.-H.Y.)

Published 17 August 2016, Sci. Transl. Med. 8, 352ra108 (2016)
DOI: 10.1126/scitranslmed.aaf2304

This PDF file includes:

  • Materials and Methods
  • Fig. S1. Identification, characterization, and optimization of a potent and selective inhibitor of MST1/2.
  • Fig. S2. General synthetic scheme of XMU-MP-1 and its analogs.
  • Fig. S3. Identification, characterization, and optimization of a potent and selective inhibitor of MST1/2.
  • Fig. S4. Effects of XMU-MP-1 on the MST1/2-mediated signaling cascade in HepG2 liver cells.
  • Fig. S5. The complex structure of MST2/XMU-MP-1.
  • Fig. S6. Effects of XMU-MP-1 on wild-type or mutated MST2-mediated signaling cascade in human HepG2 cells.
  • Fig. S7. Effects of XMU-MP-1 on wild-type or mutated MST1-mediated signaling cascade in human HepG2 cells.
  • Fig. S8. Inhibition of MST2 by various XMU-MP-1 analogs.
  • Fig. S9. Effects of XMU-MP-1 on MST1/2 signaling-mediated liver regeneration in mice.
  • Fig. S10. XMU-MP-1 stimulates MST1/2 signaling-mediated liver tissue repair and regeneration in mice.
  • Fig. S11. Full scans of Western blots for Figs. 1 (D and E), 2B, and 4 (A and B), and figs. S2A and S3 (C and D).
  • Fig. S12. Full scans of Western blots for figs. S3E and S4.
  • Fig. S13. Full scans of Western blots for fig. S6.
  • Fig. S14. Full scans of Western blots for fig. S7.
  • Fig. S15. Full scans of Western blots for figs. S8C and S9A.
  • Table S1. Full list of KINOMEscan profiling data of XMU-MP-1.
  • Table S2. Kinase profiling data of XMU-MP-1.
  • Table S3. Pharmacokinetics of XMU-MP-1 in rats.
  • Table S4: Blood chemistry in tolerability studies.
  • Table S5. Crystallographic data collection and refinement statistics for MST2 (residues 16–313) bound to XMU-MP-1.
  • Table S6. The sequences of primers used in this study.
  • Legend for data S1

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Other Supplementary Material for this manuscript includes the following:

  • Data S1. Tabulated raw data. (Microsoft Excel format)

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