Procaspase activating compound 1 controls tetracycline repressor-regulated gene expression system

Chiman Song, Namkyoung Kim, Miri Park, Jiyeon Lee, Ki Bong Oh, Taebo Sim

Research output: Contribution to journalArticlepeer-review


The tetracycline repressor (TetR)-regulated system is a widely used tool to study gene functions through control of its expression. Various effectors such as tetracycline (Tc) and doxycycline (Dox) quickly induce or shut down gene expression, but reversing gene expression has not been eligible due to long half-lives of such effectors. Here, we found that procaspase activating compound 1 (PAC-1) rapidly reduces transient expression of TetR-regulated green fluorescent protein (GFP) in mammalian cells. Next, we applied PAC-1 to control of expression of transient receptor potential melastatin 7 (TRPM7) protein, whose downstream cellular events can be monitored by cell morphological changes. We observed that PAC-1 quickly reduces TRPM7 expression, consequently affecting cell morphology regulated by TRPM7. The present study demonstrates the first small molecule that efficiently turns off the TetR-regulated gene expression in mammalian cells, thereby precisely regulating the expression level of target gene.

Original languageEnglish
Article numberBSR20180793
JournalBioscience Reports
Issue number1
Publication statusPublished - 2019 Jan 8

Bibliographical note

Funding Information:
This work was supported by the Korea Institute of Science and Technology (KIST); the KU-KIST Graduate School of Converging Science and Technology Program; Korea Basic Science Institute; and Candidate Development Program [grant number NRF-2016M3A9B5940991] of the National Research Foundation of Korea funded by the Ministry of Science and ICT.

Publisher Copyright:
© 2018 The Author(s).

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology


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