TRC8/RNF139 and von Hippel-Lindau (VHL) both encode E3 ubiquitin (Ub) ligases mutated in clear-cell renal carcinomas (ccRCC). VHL, inactivated in nearly 70% of ccRCCs, is a tumor suppressor encoding the targeting subunit for a Ub ligase complex that downregulates hypoxia-inducible factor-alpha. TRC8/RNF139 is a putative tumor suppressor containing a sterol-sensing domain and a RING-H2 motif essential for Ub ligase activity. Here we report that human kidney cells are growth inhibited by TRC8. Inhibition is manifested by G2/M arrest, decreased DNA synthesis and increased apoptosis and is dependent upon the Ub ligase activity of the RING domain. Tumor formation in a nude mouse model is inhibited by TRC8 in a RING-dependent manner. Expression of TRC8 represses genes involved in cholesterol and fatty acid biosynthesis that are transcriptionally regulated by the sterol response element binding proteins (SREBPs). Expression of activated SREBP-1a partially restores the growth of TRC8-inhibited cells. These data suggest that TRC8 modulation of SREBP activity comprises a novel regulatory link between growth control and the cholesterol/lipid homeostasis pathway.
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http://dx.doi.org/10.1038/sj.onc.1210017 | DOI Listing |
J Hepatocell Carcinoma
January 2025
Departments of Pharmacology, School of Pharmacy, Qingdao University Medical College, Shandong, People's Republic of China.
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View Article and Find Full Text PDFBiochem Pharmacol
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Colorectal cancer (CRC), one of the diseases posing a threat to global health, according to the latest data, is the third most common cancer globally and the second leading cause of cancer-related deaths. The development and refinement of novel structures of small molecular compounds play a crucial role in tumor treatment and overcoming drug resistance. In this study, our objective was to screen and characterize novel compounds for overcoming drug resistance via the B Lymphoma Mo-MLV insertion region 1 (Bmi-1) reporter screen assay.
View Article and Find Full Text PDFJ Med Microbiol
January 2025
Department of Stem Cell and Regenerative Medicine, Medical Biotechnology, Centre for Interdisciplinary Research, D.Y. Patil Education Society (Deemed to be University), Kolhapur- 416-003, Maharashtra, India.
Increased virulence and drug resistance in species of resulted in reduced disease control and further demand the development of potent antifungal drugs. The repurposing of non-antifungal drugs and combination therapy has become an attractive alternative to counter the emerging drug resistance and toxicity of existing antifungal drugs against and non-albicans species. This study aimed to accelerate antifungal drug development process by drug repurposing approach.
View Article and Find Full Text PDFIran J Basic Med Sci
January 2025
School of Medicine, Hangzhou City University, Hangzhou 310015, China.
Objectives: Plinabulin, a marine-derived anticancer drug targeting microtubules, exhibits anti-cancer effects on glioblastoma cells. However, its therapeutic potential, specifically for glioblastoma treatment, remains underexplored. This study aims to elucidate the mechanisms by which plinabulin exerts its effects on glioblastoma cells.
View Article and Find Full Text PDFEur J Med Chem
January 2025
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, 450001, China. Electronic address:
Based on the molecular hybridization strategy, novel thienopyridine indole derivatives were designed and synthesized as tubulin polymerization inhibitors, and the in vitro antiproliferative potency on MGC-803, KYSE450 and HCT-116 cells was evaluated. Among them, compound 20b showed a broad-spectrum antiproliferative activity against 11 cancer cell lines, with IC values below 4 nmol/L. Notably, it demonstrated exceptional efficacy against MGC-803 (IC = 1.
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