Lysine-specific demethylase 5A (KDM5A, also named RBP2 or JARID1A) is a demethylase that can remove methyl groups from histones H3K4me1/2/3. It is aberrantly expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, drug resistance, and is associated with poor prognosis. Pharmacological inhibition of KDM5A has been reported to significantly attenuate tumor progression in vitro and in vivo in a range of solid tumors and acute myeloid leukemia. This review will present the structural aspects of KDM5A, its role in carcinogenesis, a comparison of currently available approaches for screening KDM5A inhibitors, a classification of KDM5A inhibitors, and its potential as a drug target in cancer therapy.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejmech.2021.113855 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Effect of anthocyanin rich black sugarcane on milk production and antioxidant capacity in lactating dairy cows.
Sci Rep
January 2025
School of Animal Technology and Innovation, Institute of Agricultural Technology, Suranaree University of Technology, Nakhon Ratchasima, 30000, Thailand.
This study aimed to explore the effect of anthocyanin-rich black sugarcane on milk production, plasma antioxidant capacity, and the storage period DPPH scavenging capacity of milk in lactating dairy cows. Sixteen lactating dairy cows were stratified and randomly assigned into two balanced dietary groups, namely Anthocyanin-rich black sugarcane (AS), and Napier grass (NG). The AS group demonstrated a significant decrease (p < 0.
View Article and Find Full Text PDFInhibition of transcriptional regulation of detoxification genes contributes to insecticide resistance management in Spodoptera exigua.
Commun Biol
January 2025
Key Laboratory of Integrated Management of Crop Diseases and Pests (Ministry of Education), College of Plant Protection, Nanjing Agricultural University, Nanjing, China.
Synthetic insecticides have been widely used for the prevention and control of disease vectors and agricultural pests. However, frequent uses of insecticides have resulted in the development of insecticide resistance in these insect pests. The resistance adversely affects the efficacy of insecticides, and seriously reduces the lifespan of insecticides.
View Article and Find Full Text PDFThe PI4K2A gene positively regulates lipid synthesis in bovine mammary epithelial cells and attenuates the inhibitory effect of t10,c12-CLA on lipid synthesis.
Sci Rep
January 2025
College of Animal Science and Technology, Ningxia Key Laboratory of Ruminant Molecular and Cellular Breeding, Ningxia University, Yinchuan, 750021, China.
Currently, the identification of valuable candidate genes affecting milk fat synthesis in dairy cows is still limited, and the specific regulatory mechanism is still unknown. In this study, we used primary bovine mammary epithelial cells(BMECs)as a model and utilized overexpression and knockdown techniques for the PI4K2A gene to investigate the specific mechanisms by which it regulates lipid metabolism in BMECs. We studied whether PI4K2A regulates the inhibition of trans-10, cis-12 conjugated linoleic acid (t10,c12-CLA) on lipid synthesis in BMECs.
View Article and Find Full Text PDFThe role of homogenization cycles and Poloxamer 188 on the quality of mitochondria isolated for use in mitochondrial transplantation therapy.
Sci Rep
January 2025
Laboratory for Critical Care Physiology, Feinstein Institutes for Medical Research, Northwell Health, Manhasset, NY, USA.
Mitochondrial transplantation (MTx) offers a promising therapeutic approach to mitigate mitochondrial dysfunction in conditions such as ischemia-reperfusion (IR) injury. The quality and viability of donor mitochondria are critical to MTx success, necessitating the optimization of isolation protocols. This study aimed to assess a rapid mitochondrial isolation method, examine the relationship between mitochondrial size and membrane potential, and evaluate the potential benefits of Poloxamer 188 (P-188) in improving mitochondrial quality during the isolation process.
View Article and Find Full Text PDFPharmacological modulation of Sigma-1 receptor ameliorates pathological neuroinflammation in rats with diabetic neuropathic pain via the AKT/GSK-3β/NF-κB pathway.
Brain Res Bull
January 2025
Department of Pharmacology, Shaanxi University of Chinese Medicine, Xianyang, 712046, PR China; Key Laboratory of Pharmacodynamic Mechanism and Material Basis of Traditional Chinese Medicine, Shaanxi Administration of Traditional Chinese Medicine, Xianyang 712046, PR China. Electronic address:
Diabetic neuropathic pain (DNP) is a common complication of diabetes mellitus (DM) and is characterized by spontaneous pain and neuroinflammation. The Sigma-1 receptor (Sig-1R) has been proposed as a target for analgesic development. It is an important receptor with anti-inflammatory properties and has been found to regulate DNP.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!