Department of Biochemistry, UT Southwestern Medical Center, 5323 Harry Hines Blvd., Dallas, Texas 75390-9038, United States.
Published: September 2020
AI Article Synopsis
Article Abstract
A series of -acyl benzothiazoles shows selective and potent cytotoxicity against cancer cell lines expressing cytochrome P450 4F11. A prodrug form is metabolized by cancer cells into an active inhibitor of stearoyl-CoA desaturase (SCD). Substantial variation on the acyl portion of the inhibitors allowed the identification of ()-, which balanced potency, solubility, and lipophilicity to allow proof-of-concept studies in mice. The prodrugs were activated inside the tumor, where they can arrest tumor growth. Together, these observations offer promise that a tumor-activated prodrug strategy might exploit the essentiality of SCD for tumor growth, while avoiding toxicity associated with systemic SCD inhibition.
Aims/hypothesis: The key pancreatic beta cell transcription factor v-maf musculoaponeurotic fibrosarcoma oncogene homologue A (MafA) is critical for the maintenance of mature beta cell function and phenotype. The expression levels and/or activities of MafA are reduced when beta cells are chronically exposed to diabetogenic stress, such as hyperglycaemia (i.e.
Department of Laboratory Medicine, Key Laboratory of Precision Medicine for Viral Diseases, Guangxi Health Commission Key Laboratory of Clinical Biotechnology, Liuzhou People's Hospital affiliated to Guangxi Medical University, No.8 Wenchang Road, Liuzhou, Guangxi 545006, China. Electronic address:
Background: In recent years, more and more studies have shown that reprogramming lipid metabolism plays an important role in the occurrence and development of hepatocellular carcinoma (HCC). However, there is a lack of systematic exploration of fatty acid (FA) profiles in HCC.
Aims: This study aims to systematically investigate the FA profile in HCC and assess the diagnostic potential of stearoyl-CoA desaturase 1 (SCD1) as a biomarker for HCC.
Traditional Chinese medicine, specifically astilbin, is studied for its effectiveness in managing pain, focusing on its active components and methods of action.
Experiments using neuropathic rat models demonstrated that both systemic and spinal delivery of astilbin significantly reduced both chronic and acute pain behaviors, with specific effective dosing identified.
The study highlighted that astilbin works by influencing neuronal metabolic processes and modulating excitatory synaptic activity, leading to its pain-relieving effects.
Fatty acids are known to have significant effects on the properties of cancer cells. Therefore, these compounds have been incorporated into therapeutic strategies. However, few studies have examined the effects of individual fatty acids and their interactions in depth.
Ferroptosis is a form of cell death linked to iron and lipid damage, showing potential for cancer treatment, particularly involving lipid peroxidation of specific fatty acids.
GPX4 normally prevents ferroptosis by converting harmful lipid hydroperoxides into less harmful forms, making it a potential drug target whose sensitivity is not well understood.
Research indicates that cancer cells cultured in 3D conditions produce fewer polyunsaturated fatty acids and more monounsaturated fatty acids, which can help them resist ferroptosis and reduce the effectiveness of GPX4 inhibitors.
