ArticleDiabetes2014
Inhibition of SREBP transcriptional activity by a boron-containing compound improves lipid homeostasis in diet-induced obesity.
Article in Diabetes, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
27 citing papers in PubMed.
- Trial
- The Mediator Complex: A Regulatory Hub for Transcriptional Activity of Nuclear Receptors.Cells · 2025Review
- SREBP2 as a central player in cancer progression: potential for targeted therapeutics.Frontiers in pharmacology · 2025Review
- Transcriptional coactivator MED15 is required for beta cell maturation.Nature communications · 2024Article
- Gkongensin A, an HSP90β inhibitor, improves hyperlipidemia, hepatic steatosis, and insulin resistance.Heliyon · 2024Article
- MED15 is upregulated by HIF-2α and promotes proliferation and metastasis in clear cell renal cell carcinoma via activation of SREBP-dependent fatty acid synthesis.Cell death discovery · 2024Article
- Boron-Containing Compounds for Prevention, Diagnosis, and Treatment of Human Metabolic Disorders.Biological trace element research · 2023Review
- Physiological and pathological roles of lipogenesis.Nature metabolism · 2023Review
- Role of the AMPK/SIRT1 pathway in non‑alcoholic fatty liver disease (Review).Molecular medicine reports · 2023Review
- Unmasking the enigma of lipid metabolism in metabolic dysfunction-associated steatotic liver disease: from mechanism to the clinic.Frontiers in medicine · 2023Review
- Postnatal eye size in mice is controlled by SREBP2-mediated transcriptional repression of Lrp2 and Bmp2.Development (Cambridge, England) · 2022Article
- Boron Chemicals in Drug Discovery and Development: Synthesis and Medicinal Perspective.Molecules (Basel, Switzerland) · 2022Review
- Turmeric and its bioactive constituents trigger cell signaling mechanisms that protect against diabetes and cardiovascular diseases.Molecular and cellular biochemistry · 2021Review
- BF175 inhibits endometrial carcinoma through SREBP-regulated metabolic pathways in vitro.Molecular and cellular endocrinology · 2021Article
- Lipid Regulatory Proteins as Potential Therapeutic Targets for Ovarian Cancer in Obese Women.Cancers · 2020Review
- The Function and Mechanism of Lipid Molecules and Their Roles in The Diagnosis and Prognosis of Breast Cancer.Molecules (Basel, Switzerland) · 2020Review
- NONO and tumorigenesis: More than splicing.Journal of cellular and molecular medicine · 2020Review
- The subunit assembly state of the Mediator complex is nutrient-regulated and is dysregulated in a genetic model of insulin resistance and obesity.The Journal of biological chemistry · 2019Article
- Emodin Induced SREBP1-Dependent and SREBP1-Independent Apoptosis in Hepatocellular Carcinoma Cells.Frontiers in pharmacology · 2019Article
- KIX domain of AtMed15a, a Mediator subunit of Arabidopsis, is required for its interaction with different proteins.Plant signaling & behavior · 2018Article
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
Dysregulation of lipid homeostasis is intimately associated with obesity, type 2 diabetes, and cardiovascular diseases. Sterol regulatory-element binding proteins (SREBPs) are the master regulators of lipid biosynthesis. Previous studies have shown that the conserved transcriptional cofactor Mediator complex is critically required for the SREBP transcriptional activity, and recruitment of the Mediator complex to the SREBP transactivation domains (TADs) is through the MED15-KIX domain. Recently, we have synthesized several boron-containing small molecules. Among these novel compounds, BF175 can specifically block the binding of MED15-KIX to SREBP1a-TAD in vitro, resulting in an inhibition of the SREBP transcriptional activity and a decrease of SREBP target gene expression in cultured hepatocytes. Furthermore, BF175 can improve lipid homeostasis in the mouse model of diet-induced obesity. Compared with the control, BF175 treatment decreased the expression of SREBP target genes in mouse livers and decreased hepatic and blood levels of lipids. These results suggest that blocking the interaction between SREBP-TADs and the Mediator complex by small molecules may represent a novel approach for treating diseases with aberrant lipid homeostasis.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.