Anhydrotetracycline (hydrochloride) |
Catalog No.GC16227 |
Effet puissant dans les systèmes de répresseur tétracycline (TetR) et de répresseur inverse TetR (revTetR)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 13803-65-1
Sample solution is provided at 25 µL, 10mM.
Anhydrotetracycline (hydrochloride) is a tetracycline biosynthetic precursor and a competitive broad-spectrum inhibitor of tetracycline destructase[1]. Anhydrotetracycline (hydrochloride) is a regulator of the tetracycline repressor (TetR) and reverse tetracycline repressor (revTetR) transcriptional repressors in eukaryotic cells [2]. TetR is an effector-regulated DNA binding protein that binds tightly to its palindromic tetO operator DNA in the absence of effectors, thereby blocking transcription of any downstream genes [3]. Anhydrotetracycline binds poorly to the 30S ribosomal subunit, so it cannot act as a general translation inhibitor and is a poor antibiotic [4].
In vitro, treatment of NIH3T3-HER2 cells with Anhydrotetracycline (hydrochloride) (10 ng/ml) for 3 days resulted in downregulation of the HER2 gene to below the detection limit [5]. Treatment of N1 cells with Anhydrotetracycline (hydrochloride) (10-200nM) for 7 days significantly reduced the expression level of the Top10-driven GUS gene[6].
In vivo, treatment of mice with NIH3T3-HER2 cell-based tumor model with Anhydrotetracycline (hydrochloride) (10mg/kg; s.c.) resulted in tumor regression of more than 95% within 7 days[5]. Treatment of mice with NIH3T3-HER2 cell-based tumor model with Anhydrotetracycline (hydrochloride) (10mg/kg; i.p.) induced downregulation of ERBB2 mRNA and protein, leading to a rapid reduction in tumor volume[7].
References:
[1] Markley J L, Fang L, Gasparrini A J, et al. Semisynthetic analogues of anhydrotetracycline as inhibitors of tetracycline destructase enzymes[J]. ACS infectious diseases, 2019, 5(4): 618-633.
[2] Gossen M, Bujard H. Anhydrotetracycline, a novel effector for tetracycline controlled gene expression systems in eukaryotic cells[J]. Nucleic acids research, 1993, 21(18): 4411.
[3] Resch M, Striegl H, Henssler E M, et al. A protein functional leap: how a single mutation reverses the function of the transcription regulator TetR[J]. Nucleic acids research, 2008, 36(13): 4390-4401.
[4] Rasmussen B, Noller H F, Daubresse G, et al. Molecular basis of tetracycline action: identification of analogs whose primary target is not the bacterial ribosome[J]. Antimicrobial agents and chemotherapy, 1991, 35(11): 2306-2311.
[5] Eger K, Hermes M, Uhlemann K, et al. 4-Epidoxycycline: an alternative to doxycycline to control gene expression in conditional mouse models[J]. Biochemical and biophysical research communications, 2004, 323(3): 979-986.
[6] Love J, Allen G C, Gatz C, et al. Differential Top10 promoter regulation by six tetracycline analogues in plant cells[J]. Journal of experimental botany, 2002, 53(376): 1871-1877.
[7] Hermes M, Schormann W, Brulport M, et al. Trastuzumab therapy vs tetracycline controlled ERBB2 downregulation: influence on tumour development in an ERBB2-dependent mouse tumour model[J]. British Journal of Cancer, 2008, 98(9): 1525-1532.
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