Song, Chiman Kim, Namkyoung Park, Miri Lee, Jiyeon Oh, Ki-Bong Sim, Taebo 2024-01-19T21:03:37Z 2024-01-19T21:03:37Z 2021-09-02 2019-01 0144-8463 https://pubs.kist.re.kr/handle/201004/120547 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. English PORTLAND PRESS LTD Procaspase activating compound 1 controls tetracycline repressor-regulated gene expression system Article 10.1042/BSR20180793 1 BIOSCIENCE REPORTS, v.39 BIOSCIENCE REPORTS 39 N scie scopus 000456367300016 2-s2.0-85059622291 Biochemistry & Molecular Biology Cell Biology Biochemistry & Molecular Biology Cell Biology Article TET REPRESSOR STEPWISE SELECTION MAMMALIAN-CELLS HIGH-AFFINITY DERIVATIVES MECHANISM REVEALS BINDING anti-induction antagonist gene regulation PAC-1 tetracycline repressor TetR-regulated system