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Cell-Active, Arginine-Targeting Irreversible Covalent Inhibitors for Non-Kinases and Kinases.
Angew Chem Int Ed Engl
January 2025
Sun Yat-sen University - Shenzhen Campus, School of Pharmaceutical Sciences (Shenzhen), CHINA.
Targeted covalent inhibitors (TCIs) play an essential role in the fields of kinase research and drug discovery. Most existing TCIs are however cysteine- or lysine-reactive, thus severely limiting their potential applications. New types of TCIs capable of covalently targeting other nucleophilic amino acids that are readily available in proteins are urgently needed.
View Article and Find Full Text PDFLysine acetylation and its role in the pathophysiology of acute pancreatitis.
Inflamm Res
January 2025
Department of Immunology, School of Basic Medicine, Qingdao University, No. 308 Ningxia Road, Qingdao, 266021, 266071, Shandong, People's Republic of China.
Acute pancreatitis (AP) represents a severe inflammatory condition of the exocrine pancreas, precipitating systemic organ dysfunction and potential failure. The global prevalence of acute pancreatitis is on an ascending trajectory. The condition carries a significant mortality rate during acute episodes.
View Article and Find Full Text PDFMETTL10 attenuates adriamycin-induced podocyte injury by targeting cell dedifferentiation.
Sci Rep
January 2025
Department of Nephrology, Ren Ji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China.
Chronic kidney disease (CKD) is a worldwide public health problem. Podocyte damage is a hallmark of glomerular diseases including focal segmental glomerulosclerosis (FSGS) and one of the leading causes of CKD. Lysine methylation is a crucial post-translational modification.
View Article and Find Full Text PDFUbiquitin-specific protease 25 ameliorates ulcerative colitis by regulating the degradation of phosphor-STAT3.
Cell Death Dis
January 2025
Department of Gastroenterology, Renmin Hospital of Wuhan University, Wuhan, 430060, China.
Ubiquitin-specific protease 25 (USP25), a member of the deubiquitination family, plays an important role in protein ubiquitination, degradation, inflammation, and immune regulation. However, the role and mechanism of USP25 in ulcerative colitis (UC) remain unclear. To study the role and mechanism of USP25 in UC, bioinformatics analysis and research are conducted on clinical patients with UC, Usp25 knockout (Usp25) mice, intestinal epithelial cell-specific knockout signal transducer and activator of transcription 3 (Stat3) (Villin-Cre Stat3) mice, and human colonic epithelial cells.
View Article and Find Full Text PDFPKM2 controls cochlear development through lactate-dependent transcriptional regulation.
Proc Natl Acad Sci U S A
January 2025
ENT Institute and Otorhinolaryngology Department of Eye & ENT Hospital, State Key Laboratory of Medical Neurobiology and MOE Frontiers Center for Brain Science, Fudan University, Shanghai 200031, China.
Understanding the role of metabolic processes during inner ear development is essential for identifying targets for hair cell (HC) regeneration, as metabolic choices play a crucial role in cell proliferation and differentiation. Among the metabolic processes, growing evidence shows that glucose metabolism is closely related to organ development. However, the role of glucose metabolism in mammalian inner ear development and HC regeneration remains unclear.
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