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Histone deacetylase enzymes (HDACs) are potential targets for the treatment of cancer and other diseases, but it is challenging to design isoform-selective agents. In this work, we created new analogs of two established but non-selective HDAC inhibitors. We decorated the central linker chains of the molecules with specifically positioned fluorine atoms in order to control the molecular conformations. The fluorinated analogs were screened against a panel of 11 HDAC isoforms, and minor differences in isoform selectivity patterns were observed.
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http://dx.doi.org/10.3390/molecules26133974 | DOI Listing |
Tree Physiol
September 2025
Pollen Biotechnology of Crop Plants Group, Margarita Salas Center of Biological Research, CIB-CSIC, Ramiro de Maeztu 9, 28040, Madrid, Spain.
Somatic embryogenesis (SE) is an in vitro mass propagation system widely employed in plant breeding programs. However, its efficiency in many forest species remains limited due to their recalcitrance. SE relies on the induction of somatic cell reprogramming into embryogenic pathways, a process influenced by transcriptomic changes regulated, among other factors, by epigenetic modifications such as DNA methylation, histone methylation, and histone acetylation.
View Article and Find Full Text PDFG Ital Nefrol
August 2025
UO Nefrologia e Dialisi, Ospedale di Cassino, Italia.
SGLT-2 inhibitors are a relatively new class of antidiabetic drugs. They activate a transcriptional response similar to calorie restriction characterized by the up-regulation of sensors involved in nutrient deprivation, such as SIRT1 and AMPK, and the down-regulation of mTOR, a molecule involved in nutritional excess signaling. The purpose of this review is to illustrate the main pathways of nutrient deprivation: a complex mechanistic framework partly responsible for the cardio-renal benefits that makes these drugs unique.
View Article and Find Full Text PDFJCI Insight
September 2025
Division of Cardiovascular Medicine, Department of Medicine.
Aortic valve stenosis is a progressive and increasingly prevalent disease in older adults, with no approved pharmacologic therapies to prevent or slow its progression. Although genetic risk factors have been identified, the contribution of epigenetic regulation remains poorly understood. Here, we demonstrated that histone deacetylase 3 (HDAC3) maintains aortic valve structure by suppressing mitochondrial biogenesis and preserving extracellular matrix integrity in valvular interstitial fibroblasts.
View Article and Find Full Text PDFJ Mol Histol
September 2025
Physiology Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran.
One of the most prevalent metabolic diseases in recent years, type 2 diabetes is now one of the top causes of death globally and a significant risk factor for cardiovascular diseases. Therefore, the goal of this study is to investigate the impact of HIIT exercises on the levels of specific proteins associated with mitochondrial biogenesis and apoptosis in the heart tissue of male Wistar rats with type 2 diabetes. Animals in diabetic groups were given a high-fat diet and an intraperitoneal injection of STZ to cause diabetes.
View Article and Find Full Text PDFArch Toxicol
September 2025
Mainz University Medical Center, Mainz, Germany.
Opinion Letter to Sin et al (Science Advances, 2025), Sorbate induces lysine sorbylation through noncanonical activities of class I HDACs to regulate the expression of inflammation genes.
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